| DRUGS | RECEPTOR | CLINICAL INFORMATION | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| NAME |
INDICATION |
TARGET |
TARGET LEVEL |
CLASS |
FAMILY |
STATUS |
PHASE |
CLINICAL STATUS |
YEAR OF APPROVAL |
DRUG TYPE |
MECHANISM OF ACTION |
NHS |
REFERENCES |
| abaloparatide | Anti-Osteoporotic | pth1r_human | primary | B1 (Secretin) | Parathyroid hormone receptors | approved | 4 | - | 2017 | peptide | agonist | no | Refs |
| abarelix | Antineoplastic | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | approved | 4 | - | 2003 | peptide | antagonist | no | Refs |
| acamprosate | Antineoplastic | grm5_human | secondary | C (Glutamate) | Metabotropic glutamate receptors | approved | 4 | - | 2004 | small molecule | antagonist | yes | Refs |
| acebutolol | Antihypertensive | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1984 | small molecule | antagonist | yes | Refs |
| acepromazine | Antipsychotic | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| acepromazine | Antipsychotic | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| acepromazine | Antipsychotic | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| acepromazine | Antipsychotic | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| acepromazine | Hypnotics And Sedatives | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| acetophenazine | Schizophrenia | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1961 | small molecule | antagonist | no | Refs |
| acetophenazine | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1961 | small molecule | antagonist | no | Refs |
| acetylcholine | Antiglaucomic | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1973 | small molecule | agonist | yes | Refs |
| acipimox | Lipid-Lowering | hcar2_human | primary | A (Rhodopsin) | Hydroxycarboxylic acid receptors | approved | 4 | - | 2003 | small molecule | agonist | yes | Refs |
| agomelatine | Anti-Depressant | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| agomelatine | Anti-Depressant | mtr1a_human | primary | A (Rhodopsin) | Melatonin | approved | 4 | - | 2009 | small molecule | agonist | yes | Refs |
| agomelatine | Anti-Depressant | mtr1b_human | primary | A (Rhodopsin) | Melatonin | approved | 4 | - | 2009 | small molecule | agonist | yes | Refs |
| aclidinium | Bronchodilator | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2012 | small molecule | antagonist | yes | Refs |
| aclidinium | Bronchodilator | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2012 | small molecule | antagonist | yes | Refs |
| aclidinium | Bronchodilator | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2012 | small molecule | antagonist | yes | Refs |
| aclidinium | Bronchodilator | acm4_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2012 | small molecule | antagonist | yes | Refs |
| aclidinium | Bronchodilator | acm5_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2012 | small molecule | antagonist | yes | Refs |
| acrivastine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1994 | small molecule | antagonist | yes | Refs |
| adenosine | Analgesics | aa3r_human | primary | A (Rhodopsin) | Adenosine receptors | approved | 4 | - | 1989 | small molecule | agonist | yes | Refs |
| adenosine | Analgesics | aa2ar_human | primary | A (Rhodopsin) | Adenosine receptors | approved | 4 | - | 1989 | small molecule | agonist | yes | Refs |
| adenosine | Analgesics | aa2br_human | primary | A (Rhodopsin) | Adenosine receptors | approved | 4 | - | 1989 | small molecule | agonist | yes | Refs |
| adenosine | Analgesics | aa1r_human | primary | A (Rhodopsin) | Adenosine receptors | approved | 4 | - | 1989 | small molecule | agonist | yes | Refs |
| albiglutide | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | approved | 4 | - | 2014 | protein | agonist | yes | Refs |
| albuterol | Chronic Obstructive Pulmonary Disease (Copd) | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1981 | small molecule | agonist | no | Refs |
| alcaftadine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 2010 | small molecule | antagonist | no | Refs |
| alprenolol | Anti-Arrhythmia ; Antihypertensive | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1966 | small molecule | antagonist | no | Refs |
| alfentanil | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1986 | small molecule | agonist | yes | Refs |
| alfuzosin | Benign Prostatic Hyperplasia | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2003 | small molecule | agonist | yes | Refs |
| alfuzosin | Benign Prostatic Hyperplasia | ada1d_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2003 | small molecule | agonist | yes | Refs |
| alfuzosin | Benign Prostatic Hyperplasia | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2003 | small molecule | agonist | yes | Refs |
| almotriptan | Anti-Migraine | 5ht1b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2001 | small molecule | agonist | yes | Refs |
| almotriptan | Anti-Migraine | 5ht1d_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2001 | small molecule | agonist | yes | Refs |
| alprenolol | Anti-Arrhythmia ; Antihypertensive | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1966 | small molecule | antagonist | no | Refs |
| alprostadil | Sexual Dysfunction | pe2r2_human | primary | A (Rhodopsin) | Prostanoid receptors | approved | 4 | - | 1981 | small molecule | agonist | yes | Refs |
| alprostadil | Sexual Dysfunction | pe2r1_human | primary | A (Rhodopsin) | Prostanoid receptors | approved | 4 | - | 1981 | small molecule | agonist | yes | Refs |
| alverine | Antispasmodics | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2014 | small molecule | antagonist | yes | Refs |
| alvimopan | Opioid-Induced Bowel Dysfunction | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2008 | small molecule | antagonist | no | Refs |
| alvimopan | Opiate Antagonists | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2008 | small molecule | antagonist | no | Refs |
| amantadine hcl | Dyskinesias | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1968 | small molecule | antagonist | no | Refs |
| ambrisentan | Antihypertensive | ednra_human | primary | A (Rhodopsin) | Endothelin receptors | approved | 4 | - | 2007 | small molecule | antagonist | yes | Refs |
| amiodarone | Anti-Arrhythmia | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1985 | small molecule | antagonist | yes | Refs |
| amitriptyline | Analgesics | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1961 | small molecule | antagonist | yes | Refs |
| amoxapine | Unipolar Depression | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1980 | small molecule | antagonist | yes | Refs |
| amoxapine | Unipolar Depression | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1980 | small molecule | antagonist | yes | Refs |
| amoxapine | Unipolar Depression | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1980 | small molecule | antagonist | yes | Refs |
| amoxapine | Unipolar Depression | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1980 | small molecule | antagonist | yes | Refs |
| amphetamine | Cognitive Dysfunction; Adhd | taar1_human | secondary | A (Rhodopsin) | Trace amine receptors | approved | 4 | - | 1996 | small molecule | agonist | no | Refs |
| anileridine | Analgesics; Narcotics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1982 | small molecule | agonist | no | Refs |
| anisotropine methylbromide | Antispasmodics; Anti-Ulcer | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| anisotropine methylbromide | Antispasmodics; Anti-Ulcer | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| anisotropine methylbromide | Antispasmodics; Anti-Ulcer | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| antazoline | Atrial Fibrillation | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1994 | small molecule | antagonist | yes | Refs |
| apomorphine | Anti-Parkisonian | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2004 | small molecule | agonist | yes | Refs |
| apomorphine | Anti-Parkisonian | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2004 | small molecule | agonist | yes | Refs |
| apomorphine | Anti-Parkisonian | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2004 | small molecule | agonist | yes | Refs |
| atropine | Nerve Antidote | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1973 | small molecule | antagonist | yes | Refs |
| atropine | Nerve Antidote | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1973 | small molecule | antagonist | yes | Refs |
| atropine | Nerve Antidote | acm4_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1973 | small molecule | antagonist | yes | Refs |
| apraclonidine | Antiglaucomic | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1987 | small molecule | agonist | yes | Refs |
| apraclonidine | Antiglaucomic | ada2c_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1987 | small molecule | agonist | yes | Refs |
| apraclonidine | Antiglaucomic | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1987 | small molecule | agonist | yes | Refs |
| aprepitant | Antiemetics | nk1r_human | primary | A (Rhodopsin) | Tachykinin receptors | approved | 4 | - | 2003 | small molecule | antagonist | yes | Refs |
| arbutamine | Cardiotonic | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1997 | small molecule | agonist | no | Refs |
| arformoterol | Bronchodilator | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2006 | small molecule | agonist | no | Refs |
| aripiprazole | Schizophrenia | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2002 | small molecule | partial agonist | yes | Refs |
| aripiprazole | Psychosis | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2015 | small molecule | partial agonist | yes | Refs |
| aripiprazole | Schizophrenia | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2002 | small molecule | partial agonist | yes | Refs |
| aripiprazole | Psychosis | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2015 | small molecule | partial agonist | yes | Refs |
| aripiprazole | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2002 | small molecule | partial agonist | yes | Refs |
| aripiprazole | Psychosis | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2015 | small molecule | partial agonist | yes | Refs |
| asenapine | Schizophrenia | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| asenapine | Schizophrenia | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| asenapine | Schizophrenia | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| asenapine | Schizophrenia | 5ht6r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| atropine | Nerve Antidote | acm5_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1973 | small molecule | antagonist | yes | Refs |
| asenapine | Schizophrenia | 5ht1b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| asenapine | Schizophrenia | 5ht5a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| asenapine | Schizophrenia | 5ht7r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| asenapine | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| asfotase alfa | Hypophosphatasia | s1pr1_human | primary | A (Rhodopsin) | Lysophospholipid (S1P) receptors | approved | 4 | - | 2015 | enzyme | agonist | no | Refs |
| astemizole | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1988 | small molecule | antagonist | no | Refs |
| atenolol | Anti-Arrhythmia ; Antihypertensive | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1981 | small molecule | antagonist | yes | Refs |
| atosiban | Labor Repressant | oxyr_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | approved | 4 | - | 2013 | small molecule | antagonist | no | Refs |
| atropine | Nerve Antidote | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1973 | small molecule | antagonist | yes | Refs |
| azatadine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1977 | small molecule | antagonist | yes | Refs |
| baclofen | Anti-Spastic | gabr2_human | primary | C (Glutamate) | GABAB receptors | approved | 4 | - | 1977 | small molecule | agonist | yes | Refs |
| azelastine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| azelastine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 2012 | small molecule | antagonist | yes | Refs |
| azilsartan medoxomil | Antihypertensive | agtr1_human | primary | A (Rhodopsin) | Angiotensin receptors | approved | 4 | - | 2011 | small molecule | antagonist | yes | Refs |
| baclofen | Anti-Spastic | gabr1_human | primary | C (Glutamate) | GABAB receptors | approved | 4 | - | 1977 | small molecule | agonist | yes | Refs |
| benperidol | Antipsychotic | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2006 | small molecule | antagonist | yes | Refs |
| benzphetamine | Central Nervous System Stimulants | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1960 | small molecule | agonist | no | Refs |
| benzphetamine | Central Nervous System Stimulants | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1960 | small molecule | agonist | no | Refs |
| benztropine | Antiparkinson | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1954 | small molecule | antagonist | no | Refs |
| bepotastine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | no | Refs |
| betahistine | Vertigo | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1970 | small molecule | agonist | yes | Refs |
| betahistine | Vertigo | hrh3_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1970 | small molecule | antagonist | yes | Refs |
| betanechol | Antidiabetic | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1970 | small molecule | agonist | no | Refs |
| betaxolol | Antihypertensive | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1985 | small molecule | antagonist | yes | Refs |
| betazole | Diagnostic | hrh2_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1982 | small molecule | agonist | no | Refs |
| bethanechol | Eosinophilic Esophagitis | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1948 | small molecule | agonist | yes | Refs |
| bromocriptine | Antidiabetic | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1978 | small molecule | agonist | yes | Refs |
| bethanidine | Antihypertensive | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1982 | small molecule | agonist | no | Refs |
| bethanidine | Antihypertensive | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1982 | small molecule | agonist | no | Refs |
| bethanidine | Antihypertensive | ada1d_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1982 | small molecule | agonist | no | Refs |
| bromocriptine | Antidiabetic | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1978 | small molecule | agonist | yes | Refs |
| bethanidine | Antihypertensive | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1982 | small molecule | agonist | no | Refs |
| bethanidine | Antihypertensive | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1982 | small molecule | agonist | no | Refs |
| bethanidine | Antihypertensive | ada2c_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1982 | small molecule | agonist | no | Refs |
| bilastine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 2010 | small molecule | antagonist | yes | Refs |
| bimatoprost | Antiglaucomic | pf2r_human | primary | A (Rhodopsin) | Prostanoid receptors | approved | 4 | - | 2001 | small molecule | agonist | yes | Refs |
| bimatoprost | Antiglaucomic | pe2r1_human | primary | A (Rhodopsin) | Prostanoid receptors | approved | 4 | - | 2001 | small molecule | agonist | yes | Refs |
| bimatoprost | Antiglaucomic | pe2r3_human | primary | A (Rhodopsin) | Prostanoid receptors | approved | 4 | - | 2001 | small molecule | agonist | yes | Refs |
| biperiden | Antidyskinetics | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1959 | small molecule | antagonist | yes | Refs |
| bisoprolol | Antihypertensive | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1992 | small molecule | antagonist | yes | Refs |
| bitolterol | Obstructive Lung Disease | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1984 | small molecule | agonist | no | Refs |
| bopindolol | Antihypertensive | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | - | small molecule | partial agonist | no | Refs |
| bosentan | Antihypertensive | ednra_human | primary | A (Rhodopsin) | Endothelin receptors | approved | 4 | - | 2001 | small molecule | antagonist | yes | Refs |
| bosentan | Antihypertensive | ednrb_human | primary | A (Rhodopsin) | Endothelin receptors | approved | 4 | - | 2001 | small molecule | antagonist | yes | Refs |
| bromodiphenhydramine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1954 | small molecule | antagonist | no | Refs |
| brexpiprazole | Anti-Depressant | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2015 | small molecule | partial agonist | no | Refs |
| brexpiprazole | Anti-Depressant | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2015 | small molecule | partial agonist | no | Refs |
| brexpiprazole | Anti-Depressant | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2015 | small molecule | partial agonist | no | Refs |
| bromopride | Antiemetics | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| brimonidine | Antiglaucomic | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | agonist | yes | Refs |
| brimonidine | Antiglaucomic | ada2c_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | agonist | yes | Refs |
| brompheniramine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1957 | small molecule | antagonist | yes | Refs |
| brimonidine | Antiglaucomic | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | agonist | yes | Refs |
| buclizine | Antiemetics | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| buclizine | Antiemetics | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| bupranolol | Antihypertensive | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| buprenorphine | Anti-Depressant; Analgesics; Opioid Addiction | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1981 | small molecule | agonist | yes | Refs |
| buprenorphine | Anti-Depressant; Analgesics; Opioid Addiction | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2016 | small molecule | agonist | yes | Refs |
| buspirone | Anti-Anxiety | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1986 | small molecule | partial agonist | yes | Refs |
| buprenorphine | Anti-Depressant; Analgesics; Opioid Addiction | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2016 | small molecule | agonist | yes | Refs |
| butorphanol | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1978 | small molecule | partial agonist | no | Refs |
| butorphanol | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1978 | small molecule | partial agonist | no | Refs |
| buprenorphine | Anti-Depressant; Analgesics; Opioid Addiction | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1981 | small molecule | agonist | yes | Refs |
| buserelin | Lhrh Analogue | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | approved | 4 | - | - | peptide | not available | yes | Refs |
| buspirone | Anti-Anxiety | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1986 | small molecule | partial agonist | yes | Refs |
| butorphanol | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1978 | small molecule | partial agonist | no | Refs |
| butriptyline | Anti-Depressant | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1974 | small molecule | antagonist | no | Refs |
| butriptyline | Anti-Depressant | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1974 | small molecule | antagonist | no | Refs |
| cabergoline | Antiparkinson | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1996 | small molecule | agonist | yes | Refs |
| caffeine | Central Nervous System Stimulants | aa1r_human | primary | A (Rhodopsin) | Adenosine receptors | approved | 4 | - | 1999 | small molecule | antagonist | yes | Refs |
| caffeine | Central Nervous System Stimulants | aa2ar_human | primary | A (Rhodopsin) | Adenosine receptors | approved | 4 | - | 1999 | small molecule | antagonist | yes | Refs |
| calcitonin human | Parathyroid Disease | calcr_human | primary | B1 (Secretin) | Calcitonin receptors | approved | 4 | - | 1986 | peptide | agonist | no | Refs |
| calcitonin salmon recombinant | Paget'S Disease | calcr_human | primary | B1 (Secretin) | Calcitonin receptors | approved | 4 | - | 2005 | peptide | agonist | no | Refs |
| calcitonin salmon recombinant | Osteitis Deformans | calcr_human | primary | B1 (Secretin) | Calcitonin receptors | approved | 4 | - | 2005 | peptide | agonist | no | Refs |
| calcitonin salmon recombinant | Postmenopausal Osteoporosis | calcr_human | primary | B1 (Secretin) | Calcitonin receptors | approved | 4 | - | 1978 | peptide | agonist | no | Refs |
| candesartan cilexetil | Antihypertensive | agtr1_human | primary | A (Rhodopsin) | Angiotensin receptors | approved | 4 | - | 1998 | small molecule | antagonist | yes | Refs |
| cangrelor | Antithrombotic | p2y12_human | primary | A (Rhodopsin) | P2Y receptors | approved | 4 | - | 2015 | small molecule | antagonist | no | Refs |
| captodiame | Anxiolytic | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | - | small molecule | agonist | no | Refs |
| captodiame | Anxiolytic | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| carbachol | Antiglaucomic | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1972 | small molecule | agonist | no | Refs |
| carbachol | Antiglaucomic | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1972 | small molecule | agonist | no | Refs |
| carbinoxamine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 2003 | small molecule | antagonist | no | Refs |
| carboprost tromethamine | Abortifacient | pe2r1_human | primary | A (Rhodopsin) | Prostanoid receptors | approved | 4 | - | 1965 | small molecule | agonist | no | Refs |
| cariprazine | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2015 | small molecule | partial agonist | no | Refs |
| cariprazine | Schizophrenia | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2015 | small molecule | partial agonist | no | Refs |
| chlophedianol | Antitussive | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1987 | small molecule | antagonist | no | Refs |
| carphenazine | Schizophrenia | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| carphenazine | Schizophrenia | drd5_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| carphenazine | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| carteolol | Antiglaucomic | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1988 | small molecule | antagonist | yes | Refs |
| carteolol | Cardiovascular Disease | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1988 | small molecule | antagonist | yes | Refs |
| carvedilol | Cardiovascular Disease | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1995 | small molecule | antagonist | yes | Refs |
| carvedilol | Congestive Heart Failure | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1995 | small molecule | antagonist | yes | Refs |
| celiprolol | Antihypertensive | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | - | small molecule | agonist | yes | Refs |
| celiprolol | Antihypertensive | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | - | small molecule | antagonist | yes | Refs |
| ceruletide | Diagnostic | cckar_human | primary | A (Rhodopsin) | Cholecystokinin receptors | withdrawn | 4 | - | 1982 | small molecule | agonist | no | Refs |
| cetirizine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 2007 | small molecule | antagonist | yes | Refs |
| cetrorelix | Antineoplastic | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | approved | 4 | - | 2000 | peptide | antagonist | yes | Refs |
| cevimeline | Parasympathomimetics | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2000 | small molecule | agonist | no | Refs |
| cevimeline | Parasympathomimetics | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2000 | small molecule | agonist | no | Refs |
| chlorcyclizine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| chloropyramine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| chlorpheniramine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1950 | small molecule | antagonist | no | Refs |
| chlorpromazine | Psychosis | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1957 | small molecule | antagonist | yes | Refs |
| chlorpromazine | Psychosis | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1957 | small molecule | antagonist | yes | Refs |
| chlorprothixene | Schizophrenia | 5ht2b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1967 | small molecule | antagonist | yes | Refs |
| chlorprothixene | Schizophrenia | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1967 | small molecule | antagonist | yes | Refs |
| chorionic gonadotropin | Antineoplastic | lshr_human | primary | A (Rhodopsin) | Glycoprotein hormone receptors | approved | 4 | - | 1973 | protein | agonist | no | Refs |
| chlorprothixene | Schizophrenia | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1967 | small molecule | antagonist | yes | Refs |
| chlorprothixene | Schizophrenia | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1967 | small molecule | antagonist | yes | Refs |
| chlorprothixene | Schizophrenia | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1967 | small molecule | antagonist | yes | Refs |
| chlorprothixene | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1967 | small molecule | antagonist | yes | Refs |
| chorionic gonadotropin | Stroke | lshr_human | primary | A (Rhodopsin) | Glycoprotein hormone receptors | approved | 4 | - | 1973 | protein | agonist | no | Refs |
| chorionic gonadotropin | Fertility | lshr_human | primary | A (Rhodopsin) | Glycoprotein hormone receptors | approved | 4 | - | 1973 | protein | agonist | no | Refs |
| cimetidine | Antihistamines | hrh2_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1977 | small molecule | antagonist | yes | Refs |
| cimetidine | Gi Anti-Ulcer ; Antihistamines | hrh2_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1977 | small molecule | antagonist | yes | Refs |
| cinacalcet | Hyperparathyroidism | casr_human | primary | C (Glutamate) | Calcium-sensing receptors | approved | 4 | - | 2004 | small molecule | PAM | yes | Refs |
| cinacalcet | Calcimimetics | casr_human | primary | C (Glutamate) | Calcium-sensing receptors | approved | 4 | - | 2004 | small molecule | PAM | yes | Refs |
| cinitapride | Gastrointestinal Disorders | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| cinitapride | Gastrointestinal Disorders | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | - | small molecule | agonist | no | Refs |
| cinnarizine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1989 | small molecule | antagonist | yes | Refs |
| cisapride | Parasympathomimetics | 5ht4r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1993 | small molecule | agonist | no | Refs |
| clemastine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1977 | small molecule | antagonist | yes | Refs |
| clenbuterol | Bronchodilator | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | - | small molecule | agonist | no | Refs |
| kp201 | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| kp201 | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| kp201 | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| clidinium | Gi Anti-Ulcer ; Anticholinergic; Antispasmodics | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2013 | small molecule | antagonist | no | Refs |
| clofedanol | Antitussive | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1987 | small molecule | antagonist | no | Refs |
| cyclobenzaprine | Anti-Depressant | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1977 | small molecule | antagonist | no | Refs |
| clonidine | Diabetic Neuropathy; Adhd; Antimucositic | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1974 | small molecule | agonist | yes | Refs |
| clonidine | Diabetic Neuropathy; Adhd; Antimucositic | ada2c_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1974 | small molecule | agonist | yes | Refs |
| clonidine | Diabetic Neuropathy; Adhd; Antimucositic | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1974 | small molecule | agonist | yes | Refs |
| clopidogrel | Antiplatelet | p2y12_human | primary | A (Rhodopsin) | P2Y receptors | approved | 4 | - | 1997 | small molecule | antagonist | yes | Refs |
| clopidogrel | Antithrombotic | p2y12_human | primary | A (Rhodopsin) | P2Y receptors | approved | 4 | - | 1997 | small molecule | antagonist | yes | Refs |
| elsiglutide | Antidiuretic | glp2r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 2 | completed | - | peptide | agonist | no | |
| clozapine | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1989 | small molecule | antagonist | yes | Refs |
| clozapine | Schizophrenia | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1989 | small molecule | antagonist | yes | Refs |
| cocaine | Local Anesthetic | drd3_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1982 | small molecule | agonist | yes | Refs |
| cocaine | Local Anesthetic | oprk_human | secondary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1982 | small molecule | agonist | yes | Refs |
| codeine | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2009 | small molecule | agonist | yes | Refs |
| codeine | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2009 | small molecule | agonist | yes | Refs |
| codeine | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2009 | small molecule | agonist | yes | Refs |
| conivaptan | Hyponatremia | v2r_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | approved | 4 | - | 2005 | small molecule | antagonist | no | Refs |
| conivaptan | Hyponatremia | v1ar_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | approved | 4 | - | 2005 | small molecule | antagonist | no | Refs |
| corticorelin ovine triflutate | Diagnostic | crfr1_human | primary | B1 (Secretin) | Corticotropin-releasing factor receptors | approved | 4 | - | 1996 | small molecule | agonist | no | Refs |
| cosyntropin | Diagnostic | acthr_human | primary | A (Rhodopsin) | Melanocortin receptors | approved | 4 | - | 1970 | peptide | agonist | no | Refs |
| cromolyn sodium | Anti-Allergenic | gpr35_human | primary | A (Rhodopsin) | Class A orphans | approved | 4 | - | 2000 | small molecule | agonist | no | Refs |
| cyclizine | Antiemetics | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1982 | small molecule | antagonist | yes | Refs |
| cyclobenzaprine | Muscle Relaxants | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1977 | small molecule | antagonist | no | Refs |
| cyclopentolate | Mydriatics | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1974 | small molecule | antagonist | yes | Refs |
| cycrimine | Antiparkinson | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| cyproheptadine | Anti-Allergic ; Appetite Stimulant | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1961 | small molecule | antagonist | yes | Refs |
| cyproheptadine | Anti-Allergic ; Appetite Stimulant | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1961 | small molecule | antagonist | yes | Refs |
| danazol | Diabetic Macular Edema | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | approved | 4 | - | 1976 | small molecule | agonist | yes | Refs |
| danazol | Antiendometriosis ; Antineoplastic | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | approved | 4 | - | 1976 | small molecule | agonist | yes | Refs |
| dapiprazole | Opthalmological | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1990 | small molecule | antagonist | no | Refs |
| dapiprazole | Opthalmological | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1990 | small molecule | antagonist | no | Refs |
| dapiprazole | Opthalmological | ada1d_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1990 | small molecule | antagonist | no | Refs |
| darifenacin | Overactive Bladder | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2004 | small molecule | antagonist | yes | Refs |
| degarelix | Antineoplastic | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | approved | 4 | - | 2008 | small molecule | antagonist | yes | Refs |
| desipramine | Anti-Depressant | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1964 | small molecule | antagonist | no | Refs |
| desloratadine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 2001 | small molecule | antagonist | yes | Refs |
| desmopressin | Antidiuretic | v1ar_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | approved | 4 | - | 1978 | peptide | not available | yes | Refs |
| desmopressin | Antidiuretic | v1br_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | approved | 4 | - | 1978 | peptide | not available | yes | Refs |
| desmopressin | Antidiuretic | v2r_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | approved | 4 | - | 1978 | peptide | agonist | yes | Refs |
| dexbrompheniramine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1963 | small molecule | antagonist | no | Refs |
| dexchlorpheniramine | Sunburn | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1981 | small molecule | antagonist | no | Refs |
| dexmedetomidine | Analgesics | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1999 | small molecule | agonist | no | Refs |
| dexmedetomidine | Antineoplastic | ada2c_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1999 | small molecule | agonist | no | Refs |
| dexmedetomidine | Analgesics; Hypnotics And Sedatives | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1999 | small molecule | agonist | no | Refs |
| dezocine | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1989 | small molecule | partial agonist | no | Refs |
| dezocine | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1989 | small molecule | partial agonist | no | Refs |
| dicyclomine | Antispasmodics | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1950 | small molecule | antagonist | no | Refs |
| difenoxin | Recurrent Infection Of The Gastrointestinal Tract | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1978 | small molecule | agonist | no | Refs |
| dihydrocodeine | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1958 | small molecule | agonist | yes | Refs |
| dihydroergotamine | Anti-Migraine | 5ht1b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1997 | small molecule | agonist | no | Refs |
| dipivefrin | Antiglaucomic | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1980 | small molecule | agonist | yes | Refs |
| dihydroergotamine | Anti-Migraine | 5ht1d_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1997 | small molecule | agonist | no | Refs |
| dimenhydrinate | Antiemetics | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1972 | small molecule | antagonist | yes | Refs |
| dimetindene | Anti-Allergic | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| dimetindene | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| dinoprost tromethamine | Abortifacient | pi2r_human | primary | A (Rhodopsin) | Prostanoid receptors | approved | 4 | - | 1981 | small molecule | agonist | no | Refs |
| dinoprostone | Abortifacient | pe2r4_human | primary | A (Rhodopsin) | Prostanoid receptors | approved | 4 | - | 1977 | small molecule | agonist | yes | Refs |
| dinoprostone | Abortifacient | pe2r1_human | primary | A (Rhodopsin) | Prostanoid receptors | approved | 4 | - | 1977 | small molecule | agonist | yes | Refs |
| dinoprostone | Abortifacient | pe2r3_human | primary | A (Rhodopsin) | Prostanoid receptors | approved | 4 | - | 1977 | small molecule | agonist | yes | Refs |
| dinoprostone | Abortifacient | pe2r2_human | primary | A (Rhodopsin) | Prostanoid receptors | approved | 4 | - | 1977 | small molecule | agonist | yes | Refs |
| diphemanil | Bronchodilator | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1976 | small molecule | antagonist | no | Refs |
| diphenhydramine | Anti-Allergic ; Hypnotics And Sedatives; Antiemetics; Antipruritics; Antitussives | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1946 | small molecule | antagonist | yes | Refs |
| diphenidol | Antiemetics | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1967 | small molecule | antagonist | no | Refs |
| diphenidol | Antiemetics | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1967 | small molecule | antagonist | no | Refs |
| diphenidol | Antiemetics | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1967 | small molecule | antagonist | no | Refs |
| diphenoxylate | Antidiuretic | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1960 | small molecule | agonist | no | Refs |
| diphenylpyraline | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| dipivefrin | Opthalmological | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1980 | small molecule | agonist | yes | Refs |
| dipivefrin | Antiglaucomic | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1980 | small molecule | agonist | yes | Refs |
| dobutamine | Cardiotonic | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1978 | small molecule | agonist | no | Refs |
| dopamine | Hypotension | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1974 | small molecule | agonist | no | Refs |
| doxepin | Hypnotics And Sedatives | hrh2_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1969 | small molecule | antagonist | yes | Refs |
| doxacurium | Muscle Relaxants | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1991 | small molecule | antagonist | no | Refs |
| doxazosin | Anticholesteremic ; Antihypertensive ; Vasodilator | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1990 | small molecule | antagonist | yes | Refs |
| doxazosin | Anticholesteremic ; Antihypertensive ; Vasodilator | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1990 | small molecule | antagonist | yes | Refs |
| doxazosin | Anticholesteremic ; Antihypertensive ; Vasodilator | ada1d_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1990 | small molecule | antagonist | yes | Refs |
| doxepin | Hypnotics And Sedatives | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1969 | small molecule | antagonist | yes | Refs |
| doxepin | Hypnotics And Sedatives | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1969 | small molecule | antagonist | yes | Refs |
| doxepin | Hypnotics And Sedatives | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1969 | small molecule | antagonist | yes | Refs |
| doxepin | Hypnotics And Sedatives | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1969 | small molecule | antagonist | yes | Refs |
| doxepin | Hypnotics And Sedatives | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1969 | small molecule | antagonist | yes | Refs |
| doxepin | Hypnotics And Sedatives | acm4_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1969 | small molecule | antagonist | yes | Refs |
| doxepin | Hypnotics And Sedatives | acm5_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1969 | small molecule | antagonist | yes | Refs |
| doxylamine | Antihistamine; For Nausea And Vomiting Of Pregnancy | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1948 | small molecule | antagonist | no | Refs |
| doxepin | Hypnotics And Sedatives | 5ht2b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1969 | small molecule | antagonist | yes | Refs |
| doxepin | Hypnotics And Sedatives | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1969 | small molecule | antagonist | yes | Refs |
| doxylamine | Anti-Allergic ; Antiemetics; Antitussive ; Hypnotics And Sedatives | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1948 | small molecule | antagonist | no | Refs |
| dronabinol | Analgesics | cnr1_human | primary | A (Rhodopsin) | Cannabinoid receptors | approved | 4 | - | 1985 | small molecule | agonist | no | Refs |
| dronabinol | Appetite Stimulant | cnr1_human | primary | A (Rhodopsin) | Cannabinoid receptors | approved | 4 | - | 1985 | small molecule | agonist | no | Refs |
| droperidol | Psychosis | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1970 | small molecule | antagonist | no | Refs |
| dronedarone | Anti-Arrhythmia | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| dronedarone | Anti-Arrhythmia | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| droperidol | Adjuvants; Anesthesia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1970 | small molecule | antagonist | no | Refs |
| droxidopa | Orthostatic Hypotension | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2014 | small molecule | agonist | no | Refs |
| droxidopa | Orthostatic Hypotension | ada1d_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2014 | small molecule | agonist | no | Refs |
| droxidopa | Orthostatic Hypotension | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2014 | small molecule | agonist | no | Refs |
| droxidopa | Orthostatic Hypotension | adrb3_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2014 | small molecule | agonist | no | Refs |
| droxidopa | Orthostatic Hypotension | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2014 | small molecule | agonist | no | Refs |
| droxidopa | Orthostatic Hypotension | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2014 | small molecule | agonist | no | Refs |
| droxidopa | Orthostatic Hypotension | ada2c_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2014 | small molecule | agonist | no | Refs |
| droxidopa | Orthostatic Hypotension | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2014 | small molecule | agonist | no | Refs |
| droxidopa | Orthostatic Hypotension | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2014 | small molecule | agonist | no | Refs |
| dulaglutide | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | approved | 4 | - | 2014 | protein | agonist | yes | Refs |
| eletriptan | Anti-Migraine | 5ht1b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2002 | small molecule | agonist | yes | Refs |
| eletriptan | Anti-Migraine | 5ht1f_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2002 | small molecule | agonist | yes | Refs |
| eletriptan | Anti-Migraine | 5ht1d_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2002 | small molecule | agonist | yes | Refs |
| eluxadoline | Irritable Bowel Syndrome | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2015 | small molecule | agonist | no | Refs |
| eluxadoline | Irritable Bowel Syndrome | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2015 | small molecule | agonist | no | Refs |
| emedastine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1997 | small molecule | antagonist | yes | Refs |
| ephedrine | Central Nervous System Stimulants | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1963 | small molecule | not available | yes | Refs |
| epinastine | Anti-Allergic | hrh2_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 2003 | small molecule | antagonist | yes | Refs |
| epinastine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 2003 | small molecule | antagonist | yes | Refs |
| epinephrine | Anesthetics | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1976 | small molecule | agonist | yes | Refs |
| epinephrine | Anesthetics | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1976 | small molecule | agonist | yes | Refs |
| epinephrine | Anesthetics | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1976 | small molecule | agonist | yes | Refs |
| epinephrine | Anesthetics | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1976 | small molecule | agonist | yes | Refs |
| epinephrine | Anesthetics | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1976 | small molecule | agonist | yes | Refs |
| epinephrine | Anesthetics | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1976 | small molecule | agonist | yes | Refs |
| epoprostenol | Antihypertensive ; Platelet Aggregation Inhibitors | pi2r_human | primary | A (Rhodopsin) | Prostanoid receptors | approved | 4 | - | 1995 | small molecule | agonist | yes | Refs |
| eprosartan | Antihypertensive | agtr1_human | primary | A (Rhodopsin) | Angiotensin receptors | approved | 4 | - | 1997 | small molecule | antagonist | yes | Refs |
| ergotamine | Anti-Migraine | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1960 | small molecule | agonist | yes | Refs |
| ergotamine | Anti-Migraine | ada1d_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1960 | small molecule | agonist | yes | Refs |
| ergotamine | Anti-Migraine | ada2c_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1960 | small molecule | agonist | yes | Refs |
| ergoloid | Cardiovascular Disease | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1953 | small molecule | agonist | yes | Refs |
| ergoloid | Cardiovascular Disease | ada1d_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1953 | small molecule | agonist | yes | Refs |
| ergoloid | Cardiovascular Disease | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1953 | small molecule | agonist | yes | Refs |
| ergoloid | Cardiovascular Disease | ada2c_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1953 | small molecule | agonist | yes | Refs |
| ergotamine | Anti-Migraine | 5ht1b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1960 | small molecule | agonist | yes | Refs |
| ergoloid | Nootropic ; Vasodilator | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1953 | small molecule | agonist | yes | Refs |
| ergoloid | Nootropic ; Vasodilator | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1953 | small molecule | agonist | yes | Refs |
| ergonovine | Antihaemorrhagic | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1946 | small molecule | agonist | yes | Refs |
| ergotamine | Anti-Migraine | 5ht1d_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1960 | small molecule | agonist | yes | Refs |
| ergotamine | Anti-Migraine | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1960 | small molecule | agonist | yes | Refs |
| etelcalcetide | Parathyroid Disorders | casr_human | primary | C (Glutamate) | Calcium-sensing receptors | approved | 4 | - | 2017 | peptide | agonist | no | Refs |
| ergotamine | Anti-Migraine | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1960 | small molecule | agonist | yes | Refs |
| ergotamine | Anti-Migraine | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1960 | small molecule | agonist | yes | Refs |
| esmolol | Anti-Arrhythmia | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1986 | small molecule | antagonist | no | Refs |
| ethopropazine | Antidyskinetics | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| ethylmorphine | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | - | small molecule | agonist | no | Refs |
| etomidate | Anesthetics; Intravenous | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1982 | small molecule | PAM | yes | Refs |
| exenatide | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | approved | 4 | - | 2005 | peptide | agonist | yes | Refs |
| exendin-4 | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | approved | 4 | - | 2005 | peptide | agonist | no | Refs |
| famotidine | Gastric Ulcer And Gastroesophageal Reflux | hrh2_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1986 | small molecule | antagonist | yes | Refs |
| famotidine | Acid Reducer | hrh2_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1986 | small molecule | antagonist | yes | Refs |
| mkc-253 | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 1 | discontinued | - | protein | agonist | no | |
| naronapride | Constipation | 5ht4r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| fenoldopam | Antihypertensive | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1997 | small molecule | agonist | no | Refs |
| fenoldopam | Antihypertensive | drd5_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1997 | small molecule | agonist | no | Refs |
| fenoterol | Bronchodilator ; Tocolytic | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | withdrawn | - | small molecule | agonist | yes | Refs |
| fingolimod | Multiple Sclerosis | s1pr5_human | primary | A (Rhodopsin) | Lysophospholipid (S1P) receptors | approved | 4 | - | 2010 | small molecule | agonist | yes | Refs |
| fentanyl | Adjuvant To Anesthesia | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1968 | small molecule | agonist | yes | Refs |
| flavoxate | Antispasmodics | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1970 | small molecule | antagonist | yes | Refs |
| flavoxate | Antispasmodics | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1970 | small molecule | antagonist | yes | Refs |
| flibanserin | Sexual Dysfunction | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2015 | small molecule | agonist | no | Refs |
| flunarizine | Anticonvulsants; Vasodilator | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1968 | small molecule | antagonist | yes | Refs |
| fentanyl | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1968 | small molecule | agonist | yes | Refs |
| fentanyl | Adjuvant To Anesthesia | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1968 | small molecule | agonist | yes | Refs |
| flupentixol | Antipsychotic | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1965 | small molecule | antagonist | yes | Refs |
| nn9924 | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 3 | ongoing | - | protein | agonist | no | |
| flupentixol | Antipsychotic | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1965 | small molecule | antagonist | yes | Refs |
| flupentixol | Antipsychotic | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1965 | small molecule | antagonist | yes | Refs |
| flupentixol | Antipsychotic | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1965 | small molecule | antagonist | yes | Refs |
| fentanyl | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1968 | small molecule | agonist | yes | Refs |
| fesoterodine | Prostate Adenocarcinoma | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2007 | small molecule | antagonist | yes | Refs |
| fesoterodine | Overactive Bladder Syndrome | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2007 | small molecule | antagonist | yes | Refs |
| fexofenadine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| fingolimod | Multiple Sclerosis | s1pr1_human | primary | A (Rhodopsin) | Lysophospholipid (S1P) receptors | approved | 4 | - | 2010 | small molecule | agonist | yes | Refs |
| fluphenazine | Schizophrenia | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1959 | small molecule | antagonist | yes | Refs |
| fluphenazine | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1959 | small molecule | antagonist | yes | Refs |
| fluphenazine decanoate | Psychosis | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1972 | small molecule | antagonist | yes | Refs |
| fluphenazine enanthate | Psychosis | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1967 | small molecule | antagonist | no | Refs |
| fluspirilene | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1977 | small molecule | antagonist | no | Refs |
| forasartan | Antihypertensive | agtr1_human | primary | A (Rhodopsin) | Angiotensin receptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| follitropin | Fertility | fshr_human | primary | A (Rhodopsin) | Glycoprotein hormone receptors | approved | 4 | - | 1997 | protein | agonist | yes | Refs |
| formoterol | Chronic Obstructive Pulmonary Disease (Copd) | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2016 | small molecule | agonist | yes | Refs |
| formoterol | Anti-Asthmatic | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2001 | small molecule | agonist | yes | Refs |
| formoterol | Chronic Obstructive Pulmonary Disease (Copd) | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2001 | small molecule | agonist | yes | Refs |
| formoterol | Bronchodilator | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2001 | small molecule | agonist | yes | Refs |
| formoterol | Anti-Asthmatic | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2010 | small molecule | agonist | yes | Refs |
| formoterol | Anti-Asthmatic ; Copd | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2001 | small molecule | agonist | yes | Refs |
| frovatriptan | Anti-Migraine | 5ht1d_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2001 | small molecule | agonist | yes | Refs |
| frovatriptan | Anti-Migraine | 5ht1b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2001 | small molecule | agonist | yes | Refs |
| gamma hydroxybutyric acid | Hypnotics And Sedatives | gabr1_human | primary | C (Glutamate) | GABAB receptors | approved | 4 | - | 2002 | small molecule | agonist | no | Refs |
| gamma hydroxybutyric acid | Hypnotics And Sedatives | gabr2_human | primary | C (Glutamate) | GABAB receptors | approved | 4 | - | 2002 | small molecule | agonist | no | Refs |
| ganirelix acetate | For Prevention Of Premature Ovulation In Fertility Treatment | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | approved | 4 | - | 1999 | small molecule | antagonist | no | Refs |
| ganirelix acetate | Fertility | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | approved | 4 | - | 1999 | small molecule | antagonist | no | Refs |
| glucagon | For Prevention Of Hypoglycemia | glr_human | primary | B1 (Secretin) | Glucagon receptor family | approved | 4 | - | 1960 | peptide | agonist | yes | Refs |
| glucagon | Hypoglycemia | glr_human | primary | B1 (Secretin) | Glucagon receptor family | approved | 4 | - | 1998 | peptide | agonist | yes | Refs |
| glucagon | Antidiabetic | glr_human | primary | B1 (Secretin) | Glucagon receptor family | approved | 4 | - | 1960 | peptide | agonist | yes | Refs |
| glucagon | Antihypoglycemic | glr_human | primary | B1 (Secretin) | Glucagon receptor family | approved | 4 | - | 1960 | peptide | agonist | yes | Refs |
| glycopyrrolate | Antineoplastic | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1961 | small molecule | antagonist | no | Refs |
| hyoscyamine | Antispasmodics | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| glycopyrrolate | Chronic Obstructive Pulmonary Disease (Copd) | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1961 | small molecule | antagonist | no | Refs |
| glycopyrronium | Chronic Obstructive Pulmonary Disease (Copd) | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1961 | small molecule | antagonist | yes | Refs |
| gonadorelin | Fertility | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | approved | 4 | - | 1982 | small molecule | agonist | yes | Refs |
| goserelin | Antineoplastic | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | approved | 4 | - | 1989 | peptide | agonist | yes | Refs |
| goserelin | Antineoplastic S; Hormonal | lshr_human | primary | A (Rhodopsin) | Glycoprotein hormone receptors | approved | 4 | - | 1989 | peptide | agonist | yes | Refs |
| guanabenz | Antihypertensive | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1982 | small molecule | agonist | no | Refs |
| guanfacine | Adhd | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1986 | small molecule | agonist | yes | Refs |
| haloperidol | Psychosis | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1986 | small molecule | antagonist | yes | Refs |
| haloperidol | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1967 | small molecule | antagonist | yes | Refs |
| hexocyclium | Digestive System Disease | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| hexocyclium | Digestive System Disease | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| histamine | Anti-Migraine | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1939 | small molecule | agonist | no | Refs |
| lanreotide | Antineoplastic | ssr2_human | primary | A (Rhodopsin) | Somatostatin receptors | approved | 4 | - | 2007 | peptide | agonist | yes | Refs |
| histamine | For Diagnosis Of Gastric Acid Secretory Function | hrh2_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1939 | small molecule | agonist | no | Refs |
| histrelin | Antineoplastic | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | approved | 4 | - | 1991 | small molecule | agonist | yes | Refs |
| homatropine methylbromide | Gi Anti-Ulcer ; Antimuscarinics | acm5_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| homatropine methylbromide | Gi Anti-Ulcer ; Antimuscarinics | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| homatropine methylbromide | Gi Anti-Ulcer ; Antimuscarinics | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| homatropine methylbromide | Gi Anti-Ulcer ; Antimuscarinics | acm4_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| homatropine methylbromide | Gi Anti-Ulcer ; Antimuscarinics | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| hyoscyamine | Antispasmodics | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| hydrocodone | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1943 | small molecule | agonist | no | Refs |
| icatibant | Hereditary Angioedema | bkrb2_human | primary | A (Rhodopsin) | Bradykinin receptors | approved | 4 | - | 2008 | small molecule | antagonist | yes | Refs |
| icosapent | Hypertriglyceridemia | ffar1_human | secondary | A (Rhodopsin) | Free fatty acid receptors | approved | 4 | - | - | small molecule | agonist | no | Refs |
| hydrocodone | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1943 | small molecule | agonist | no | Refs |
| hydromorphone | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1984 | small molecule | agonist | yes | Refs |
| hydromorphone | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1984 | small molecule | agonist | yes | Refs |
| hydromorphone | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1984 | small molecule | agonist | yes | Refs |
| hydroxyzine | Antipruritics; Anxiolytics Sedatives And Hypnotics | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1956 | small molecule | antagonist | yes | Refs |
| iloprost | Antihypertensive | pe2r1_human | primary | A (Rhodopsin) | Prostanoid receptors | approved | 4 | - | 2004 | small molecule | agonist | yes | Refs |
| iloperidone | Antipsychotic ; Atypical | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | no | Refs |
| iloperidone | Antipsychotic ; Atypical | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | no | Refs |
| iloprost | Antihypertensive | pd2r2_human | primary | A (Rhodopsin) | Prostanoid receptors | approved | 4 | - | 2004 | small molecule | agonist | yes | Refs |
| iloprost | Antihypertensive | pi2r_human | primary | A (Rhodopsin) | Prostanoid receptors | approved | 4 | - | 2004 | small molecule | agonist | yes | Refs |
| indacaterol | Bronchodilator | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2009 | small molecule | agonist | yes | Refs |
| ipratropium | Chronic Obstructive Pulmonary Disease (Copd) | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1986 | small molecule | antagonist | yes | Refs |
| ipratropium | Chronic Obstructive Pulmonary Disease (Copd) | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1986 | small molecule | antagonist | yes | Refs |
| ipratropium | Chronic Obstructive Pulmonary Disease (Copd) | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1986 | small molecule | antagonist | yes | Refs |
| indoramin | Antihypertensive | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1993 | small molecule | not available | yes | Refs |
| indoramin | Antihypertensive | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1993 | small molecule | not available | yes | Refs |
| indoramin | Antihypertensive | ada1d_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1993 | small molecule | not available | yes | Refs |
| isoetharine | Anti-Asthmatic | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1979 | small molecule | antagonist | no | Refs |
| irbesartan | Antihypertensive | agtr1_human | primary | A (Rhodopsin) | Angiotensin receptors | approved | 4 | - | 1997 | small molecule | antagonist | yes | Refs |
| isoetharine | Bronchodilator | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1979 | small molecule | agonist | no | Refs |
| isometheptene | Migraines | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | - | small molecule | agonist | yes | Refs |
| isometheptene | Anti-Migraine | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1962 | small molecule | agonist | yes | Refs |
| isopropamide | Digestive System Disease | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1957 | small molecule | antagonist | no | Refs |
| isopropamide | Digestive System Disease | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1957 | small molecule | antagonist | no | Refs |
| isoproterenol | Cardiovascular ; Anti-Asthmatic | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1956 | small molecule | agonist | no | Refs |
| isoproterenol | Bronchodilator ; Cardiotonic | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1956 | small molecule | agonist | no | Refs |
| isoproterenol | Cardiovascular ; Anti-Asthmatic | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1956 | small molecule | agonist | no | Refs |
| isoproterenol | Bronchodilator ; Cardiotonic | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1956 | small molecule | agonist | no | Refs |
| isothipendyl | Antipruritic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| itraconazole | Antineoplastic | smo_human | primary | F (Frizzled) | Frizzled | approved | 4 | - | 1992 | small molecule | antagonist | yes | Refs |
| ketobemidone | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | - | small molecule | agonist | no | Refs |
| ketobemidone | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | - | small molecule | agonist | no | Refs |
| ketobemidone | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | - | small molecule | agonist | no | Refs |
| ketotifen | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1999 | small molecule | antagonist | yes | Refs |
| leuprolide | Alzheimer'S Disease | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | approved | 4 | - | 1985 | peptide | agonist | no | Refs |
| labetalol | Cardiovascular Disease | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1984 | small molecule | antagonist | yes | Refs |
| labetalol | Cardiovascular Disease | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1984 | small molecule | antagonist | yes | Refs |
| labetalol | Cardiovascular Disease | ada2c_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1984 | small molecule | antagonist | yes | Refs |
| labetalol | Antihypertensive | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1984 | small molecule | antagonist | yes | Refs |
| labetalol | Antihypertensive | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1984 | small molecule | antagonist | yes | Refs |
| levallorphan | Opiate Antagonists | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| labetalol | Cardiovascular Disease | ada1d_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1984 | small molecule | antagonist | yes | Refs |
| labetalol | Cardiovascular Disease | adrb3_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1984 | small molecule | antagonist | yes | Refs |
| labetalol | Antihypertensive | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1984 | small molecule | antagonist | yes | Refs |
| labetalol | Antihypertensive | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1984 | small molecule | antagonist | yes | Refs |
| lanreotide | Acromegaly | ssr1_human | primary | A (Rhodopsin) | Somatostatin receptors | approved | 4 | - | 2007 | peptide | agonist | yes | Refs |
| lanreotide | Acromegaly | ssr5_human | primary | A (Rhodopsin) | Somatostatin receptors | approved | 4 | - | 2007 | peptide | agonist | yes | Refs |
| levobunolol | Antiglaucomic | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1985 | small molecule | antagonist | yes | Refs |
| levobunolol | Antiglaucomic | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1985 | small molecule | antagonist | yes | Refs |
| latanoprost | Antiglaucomic | pf2r_human | primary | A (Rhodopsin) | Prostanoid receptors | approved | 4 | - | 1996 | small molecule | agonist | yes | Refs |
| leuprolide | Antineoplastic | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | approved | 4 | - | 1985 | peptide | agonist | no | Refs |
| levocabastine | Anti-Allergic | ntr2_human | primary | A (Rhodopsin) | Neurotensin receptors | approved | 4 | - | 1993 | small molecule | antagonist | yes | Refs |
| leuprolide | Antineoplastic ; Endometriosis | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | approved | 4 | - | 1985 | peptide | agonist | no | Refs |
| levocabastine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1993 | small molecule | antagonist | yes | Refs |
| levocetirizine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 2007 | small molecule | antagonist | yes | Refs |
| levodopa | Antiparkinson | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1993 | small molecule | agonist | yes | Refs |
| levodopa | Antiparkinson | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2015 | small molecule | agonist | yes | Refs |
| levonordefrin | Nasal Decongestant | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1960 | small molecule | agonist | no | Refs |
| levodopa | Antiparkinson | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2015 | small molecule | agonist | yes | Refs |
| levodopa | Antiparkinson | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2015 | small molecule | agonist | yes | Refs |
| levodopa | Antiparkinson | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2015 | small molecule | agonist | yes | Refs |
| levodopa | Antiparkinson | drd5_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2015 | small molecule | agonist | yes | Refs |
| levodopa | Antiparkinson | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1993 | small molecule | agonist | yes | Refs |
| levodopa | Antiparkinson | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1993 | small molecule | agonist | yes | Refs |
| levodopa | Antiparkinson | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1993 | small molecule | agonist | yes | Refs |
| levodopa | Antiparkinson | drd5_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1993 | small molecule | agonist | yes | Refs |
| levorphanol | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1953 | small molecule | agonist | no | Refs |
| levomepromazine | Psychosis | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1982 | small molecule | antagonist | yes | Refs |
| levomepromazine | Psychosis | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1982 | small molecule | antagonist | yes | Refs |
| levomepromazine | Psychosis | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1982 | small molecule | antagonist | yes | Refs |
| levomepromazine | Schizophrenia | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1982 | small molecule | antagonist | yes | Refs |
| levomepromazine | Schizophrenia | 5ht2b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1982 | small molecule | antagonist | yes | Refs |
| levomethadyl acetate | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1993 | small molecule | agonist | no | Refs |
| levonordefrin | Decongestant | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1960 | small molecule | agonist | no | Refs |
| levosalbutamol | Anti-Asthmatic | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1999 | small molecule | agonist | no | Refs |
| liraglutide | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | approved | 4 | - | 2010 | protein | agonist | yes | Refs |
| liraglutide | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | approved | 4 | - | 2009 | protein | agonist | yes | Refs |
| lisdexamfetamine | Central Nervous System Stimulants | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2007 | small molecule | antagonist | yes | Refs |
| lisdexamfetamine | Central Nervous System Stimulants | taar1_human | primary | A (Rhodopsin) | Trace amine receptors | approved | 4 | - | 2007 | small molecule | antagonist | yes | Refs |
| lisuride | Antiparkinson | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2011 | small molecule | agonist | no | Refs |
| lisuride | Antiparkinson | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2011 | small molecule | agonist | no | Refs |
| lisuride | Antiparkinson | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2011 | small molecule | agonist | no | Refs |
| lixisenatide | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | approved | 4 | - | 2016 | small molecule | agonist | yes | Refs |
| lofexidine | Opiate Withdrawal | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2006 | small molecule | agonist | yes | Refs |
| lofexidine | Opiate Withdrawal | ada2c_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2006 | small molecule | agonist | yes | Refs |
| lofexidine | Opiate Withdrawal | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2006 | small molecule | agonist | yes | Refs |
| loperamide | Antidiuretic | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1976 | small molecule | agonist | yes | Refs |
| loratadine | Anti-Asthmatic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1993 | small molecule | antagonist | yes | Refs |
| lorcaserin | Anti-Obesity | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2012 | small molecule | agonist | no | Refs |
| losartan | Antihypertensive ; For Diabetic Neuropathy | agtr1_human | primary | A (Rhodopsin) | Angiotensin receptors | approved | 4 | - | 1995 | small molecule | antagonist | yes | Refs |
| losartan | Antihypertensive | agtr1_human | primary | A (Rhodopsin) | Angiotensin receptors | approved | 4 | - | 1995 | small molecule | antagonist | yes | Refs |
| loxapine | Schizophrenia | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1975 | small molecule | antagonist | yes | Refs |
| loxapine | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1975 | small molecule | antagonist | yes | Refs |
| mepenzolate | Digestive System Disease | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1956 | small molecule | antagonist | yes | Refs |
| mepenzolate | Digestive System Disease | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1956 | small molecule | antagonist | yes | Refs |
| lurasidone | Schizophrenia | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2010 | small molecule | antagonist | yes | Refs |
| lurasidone | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2010 | small molecule | antagonist | yes | Refs |
| lutropin alfa | Fertility | lshr_human | primary | A (Rhodopsin) | Glycoprotein hormone receptors | approved | 4 | - | 2004 | peptide | agonist | yes | Refs |
| macitentan | Cardiovascular Disease | ednra_human | primary | A (Rhodopsin) | Endothelin receptors | approved | 4 | - | 2013 | small molecule | antagonist | yes | Refs |
| macitentan | Cardiovascular Disease | ednrb_human | primary | A (Rhodopsin) | Endothelin receptors | approved | 4 | - | 2013 | small molecule | antagonist | yes | Refs |
| maraviroc | Antiviral ; Hiv | ccr5_human | primary | A (Rhodopsin) | Chemokine receptors | approved | 4 | - | 2007 | small molecule | antagonist | yes | Refs |
| marinol | Antiemetics | cnr1_human | primary | A (Rhodopsin) | Cannabinoid receptors | approved | 4 | - | 1985 | small molecule | agonist | no | Refs |
| meclizine | Antiemetics | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1957 | small molecule | antagonist | no | Refs |
| melatonin | Hypnotics And Sedatives | mtr1a_human | primary | A (Rhodopsin) | Melatonin | approved | 4 | - | 2005 | small molecule | agonist | yes | Refs |
| melatonin | Hypnotics And Sedatives | mtr1b_human | primary | A (Rhodopsin) | Melatonin | approved | 4 | - | 2005 | small molecule | agonist | yes | Refs |
| meperidine | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1942 | small molecule | agonist | yes | Refs |
| metaraminol | Antihypotensive ; Vasoconstrictor | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1954 | small molecule | agonist | no | Refs |
| melevodopa | Antiparkinson | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2000 | small molecule | agonist | no | Refs |
| melevodopa | Antiparkinson | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2000 | small molecule | agonist | no | Refs |
| melevodopa | Antiparkinson | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2000 | small molecule | agonist | no | Refs |
| melevodopa | Antiparkinson | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2000 | small molecule | agonist | no | Refs |
| melevodopa | Antiparkinson | drd5_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2000 | small molecule | agonist | no | Refs |
| menotropins | Fertility | lshr_human | primary | A (Rhodopsin) | Glycoprotein hormone receptors | approved | 4 | - | 1975 | protein | agonist | yes | Refs |
| menotropins | Fertility | fshr_human | primary | A (Rhodopsin) | Glycoprotein hormone receptors | approved | 4 | - | 1975 | protein | agonist | yes | Refs |
| methacholine | Anti-Asthmatic | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1986 | small molecule | agonist | no | Refs |
| methadone | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1947 | small molecule | agonist | yes | Refs |
| methadyl acetate | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1993 | small molecule | agonist | no | Refs |
| mephentermine | Cardiovascular Disease | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1951 | small molecule | agonist | no | Refs |
| mephentermine | Cardiovascular Disease | ada1d_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1951 | small molecule | agonist | no | Refs |
| mephentermine | Cardiovascular Disease | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1951 | small molecule | agonist | no | Refs |
| mephentermine | Cardiovascular Disease | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1951 | small molecule | agonist | no | Refs |
| mephentermine | Cardiovascular Disease | ada2c_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1951 | small molecule | agonist | no | Refs |
| mephentermine | Cardiovascular Disease | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1951 | small molecule | agonist | no | Refs |
| mephentermine | Cardiovascular Disease | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1951 | small molecule | agonist | no | Refs |
| mephentermine | Cardiovascular Disease | adrb3_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1951 | small molecule | agonist | no | Refs |
| mephentermine | Antihypotensive ; Vasoconstrictor | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1951 | small molecule | agonist | no | Refs |
| mequitazine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| mesoridazine | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1970 | small molecule | antagonist | no | Refs |
| mesoridazine | Schizophrenia | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1970 | small molecule | antagonist | no | Refs |
| metaproterenol | Anti-Asthmatic | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1973 | small molecule | agonist | yes | Refs |
| methamphetamine | Neuroprotectant | taar1_human | secondary | A (Rhodopsin) | Trace amine receptors | approved | 4 | - | 1943 | small molecule | agonist | no | Refs |
| methantheline | Digestive System Disease | hrh2_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1951 | small molecule | antagonist | no | Refs |
| methamphetamine | Neuroprotectant | ada2b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1943 | small molecule | agonist | no | Refs |
| methamphetamine | Neuroprotectant | ada2c_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1943 | small molecule | agonist | no | Refs |
| methamphetamine | Neuroprotectant | ada2a_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1943 | small molecule | agonist | no | Refs |
| methantheline | Gi Anti-Ulcer ; Anticholinergic; Antispasmodics | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1951 | small molecule | antagonist | no | Refs |
| methdilazine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| methoxamine | Cardiovascular Disease | ada1d_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1982 | small molecule | agonist | no | Refs |
| methoxamine | Antihypotensive ; Vasoconstrictor | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1982 | small molecule | agonist | no | Refs |
| methoxamine | Antihypotensive ; Vasoconstrictor | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1982 | small molecule | agonist | no | Refs |
| methyldopa | Antihypertensive | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1962 | small molecule | agonist | yes | Refs |
| methylergonovine | Abortifacient | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1946 | small molecule | partial agonist | no | Refs |
| methylnaltrexone | Opioid-Induced Constipation | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2008 | small molecule | antagonist | yes | Refs |
| methylnaltrexone | Oic Treatment | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2008 | small molecule | antagonist | yes | Refs |
| methylscopolamine | Anti-Ulcer | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1953 | small molecule | antagonist | no | Refs |
| methylscopolamine | Antispasmodics | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1953 | small molecule | antagonist | no | Refs |
| methylscopolamine | Anti-Ulcer | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1953 | small molecule | antagonist | no | Refs |
| methysergide | Anti-Migraine | 5ht2b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1962 | small molecule | antagonist | yes | Refs |
| methysergide | Anti-Migraine S; Vasoconstrictor | 5ht7r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1962 | small molecule | antagonist | yes | Refs |
| methysergide | Anti-Migraine S; Vasoconstrictor | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1962 | small molecule | antagonist | yes | Refs |
| methysergide | Anti-Migraine S; Vasoconstrictor | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1962 | small molecule | antagonist | yes | Refs |
| methysergide | Anti-Migraine S; Vasoconstrictor | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1962 | small molecule | antagonist | yes | Refs |
| metiamide | Acid Reducer | hrh2_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| metipranolol | Anti-Arrhythmia ; Antihypertensive ; Anti-Glaucoma | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1989 | small molecule | antagonist | yes | Refs |
| metipranolol | Anti-Arrhythmia ; Antihypertensive ; Anti-Glaucoma | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1989 | small molecule | antagonist | yes | Refs |
| metixene | Antiparkinson | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| mianserin | Anti-Depressant | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| mianserin | Anti-Depressant | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| metixene | Antiparkinson | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| metixene | Antiparkinson | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| metixene | Antiparkinson | acm4_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| metixene | Antiparkinson | acm5_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| metoclopramide | Motilitant; Gastroesophageal Reflux Disease | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1979 | small molecule | antagonist | yes | Refs |
| metoclopramide | Antiemetics | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1979 | small molecule | antagonist | yes | Refs |
| metoclopramide | Motilitant; Gastroesophageal Reflux Disease | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1979 | small molecule | agonist | yes | Refs |
| metoclopramide | Antiemetics | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1979 | small molecule | agonist | yes | Refs |
| metoprolol | Antihypertensive | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1978 | small molecule | antagonist | yes | Refs |
| metoprolol | Anti-Arrhythmia ; Antihypertensive | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1978 | small molecule | antagonist | yes | Refs |
| mirtazapine | Unipolar Depression | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| mianserin | Anti-Depressant | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| mianserin | Anti-Depressant | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| midodrine | Cardiovascular Disease | ada1d_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | agonist | yes | Refs |
| midodrine | Antihypotensive ; Vasoconstrictor | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | agonist | yes | Refs |
| midodrine | Antihypotensive ; Vasoconstrictor | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | agonist | yes | Refs |
| minaprine | Anti-Depressant | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | withdrawn | 1984 | small molecule | antagonist | no | Refs |
| minaprine | Anti-Depressant | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | withdrawn | 1984 | small molecule | antagonist | no | Refs |
| minaprine | Anti-Depressant | 5ht2b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | withdrawn | 1984 | small molecule | antagonist | no | Refs |
| mirabegron | Incontinence | adrb3_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2012 | small molecule | agonist | yes | Refs |
| mirtazapine | Anti-Depressant | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| mirtazapine | Anti-Depressant | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| misoprostol | Hemorrhage | pe2r2_human | primary | A (Rhodopsin) | Prostanoid receptors | approved | 4 | - | 1988 | small molecule | agonist | yes | Refs |
| misoprostol | Hemorrhage | pe2r3_human | primary | A (Rhodopsin) | Prostanoid receptors | approved | 4 | - | 1988 | small molecule | agonist | yes | Refs |
| mivacurium | Muscle Relaxants | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1992 | small molecule | antagonist | yes | Refs |
| molindone | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1974 | small molecule | antagonist | no | Refs |
| montelukast | Anti-Asthmatic | cltr1_human | primary | A (Rhodopsin) | Leukotriene receptors | approved | 4 | - | 1998 | small molecule | antagonist | yes | Refs |
| morphine | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1984 | small molecule | agonist | yes | Refs |
| morphine | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2002 | small molecule | agonist | yes | Refs |
| morphine | Analgesics; Opioid Addiction | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1984 | small molecule | agonist | yes | Refs |
| morphine | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1984 | small molecule | agonist | yes | Refs |
| morphine | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2002 | small molecule | agonist | yes | Refs |
| morphine | Analgesics; Opioid Addiction | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1984 | small molecule | agonist | yes | Refs |
| morphine | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1984 | small molecule | agonist | yes | Refs |
| morphine | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2002 | small molecule | agonist | yes | Refs |
| morphine | Analgesics; Opioid Addiction | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1984 | small molecule | agonist | yes | Refs |
| nabilone | Antiemetics | cnr2_human | primary | A (Rhodopsin) | Cannabinoid receptors | approved | 4 | - | 1985 | small molecule | agonist | yes | Refs |
| nabilone | Antiemetics | cnr1_human | primary | A (Rhodopsin) | Cannabinoid receptors | approved | 4 | - | 1985 | small molecule | agonist | yes | Refs |
| nadolol | Anti-Arrhythmia ; Antihypertensive | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1979 | small molecule | antagonist | yes | Refs |
| nadolol | Anti-Arrhythmia ; Antihypertensive | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1979 | small molecule | antagonist | yes | Refs |
| nafarelin | Antiendometriosis | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | approved | 4 | - | 1990 | small molecule | agonist | yes | Refs |
| nalbuphine | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1979 | small molecule | agonist | yes | Refs |
| nalbuphine | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1979 | small molecule | agonist | yes | Refs |
| nalbuphine | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1979 | small molecule | agonist | yes | Refs |
| naldemedine | Opioid-Induced Constipation | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2017 | small molecule | antagonist | no | Refs |
| nalmefene | Smoking-Cessation ; Addiction | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2013 | small molecule | antagonist | yes | Refs |
| nalmefene | Pruritus | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1995 | small molecule | antagonist | yes | Refs |
| nalmefene | Smoking-Cessation ; Addiction | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2013 | small molecule | antagonist | yes | Refs |
| nalmefene | Smoking-Cessation ; Addiction | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2013 | small molecule | antagonist | yes | Refs |
| nalmefene | Pruritus | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1995 | small molecule | antagonist | yes | Refs |
| nalmefene | Pruritus | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1995 | small molecule | antagonist | yes | Refs |
| naloxegol | Opioid-Induced Constipation | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2014 | small molecule | antagonist | yes | Refs |
| naloxone | Analgesics; Opioid Addiction | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1971 | small molecule | antagonist | yes | Refs |
| naloxone | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1971 | small molecule | antagonist | yes | Refs |
| naloxone | Analgesics; Opioid Addiction | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1971 | small molecule | antagonist | yes | Refs |
| naloxone | Analgesics; Overdose/Drug Toxicity | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1971 | small molecule | antagonist | yes | Refs |
| naloxone | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2006 | small molecule | antagonist | yes | Refs |
| naltrexone | Appetite Suppressant | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1998 | small molecule | antagonist | yes | Refs |
| naloxone | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1971 | small molecule | antagonist | yes | Refs |
| naloxone | Analgesics; Overdose/Drug Toxicity | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1971 | small molecule | antagonist | yes | Refs |
| naloxone | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2006 | small molecule | antagonist | yes | Refs |
| naltrexone | Addiction | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2016 | small molecule | antagonist | yes | Refs |
| naloxone | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1971 | small molecule | antagonist | yes | Refs |
| naloxone | Analgesics; Opioid Addiction | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1971 | small molecule | antagonist | yes | Refs |
| naloxone | Analgesics; Overdose/Drug Toxicity | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1971 | small molecule | antagonist | yes | Refs |
| naloxone | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2006 | small molecule | antagonist | yes | Refs |
| naltrexone | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1998 | small molecule | antagonist | yes | Refs |
| naltrexone | Substance Abuse | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1998 | small molecule | antagonist | yes | Refs |
| naltrexone | Analgesics; For Type 1A Charcot-Marie-Tooth Disease | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1998 | small molecule | antagonist | yes | Refs |
| naltrexone | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1998 | small molecule | antagonist | yes | Refs |
| naltrexone | Appetite Suppressant | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1998 | small molecule | antagonist | yes | Refs |
| naltrexone | Substance Abuse | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1998 | small molecule | antagonist | yes | Refs |
| naltrexone | Addiction | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2016 | small molecule | antagonist | yes | Refs |
| naltrexone | Analgesics; For Type 1A Charcot-Marie-Tooth Disease | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1998 | small molecule | antagonist | yes | Refs |
| naltrexone | Appetite Suppressant | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1998 | small molecule | antagonist | yes | Refs |
| naltrexone | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1998 | small molecule | antagonist | yes | Refs |
| naltrexone | Substance Abuse | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1998 | small molecule | antagonist | yes | Refs |
| naltrexone | Addiction | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2016 | small molecule | antagonist | yes | Refs |
| naltrexone | Analgesics; For Type 1A Charcot-Marie-Tooth Disease | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1998 | small molecule | antagonist | yes | Refs |
| naphazoline | Nasal Obstruction | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1971 | small molecule | agonist | yes | Refs |
| naphazoline | Eye Allergy | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1971 | small molecule | agonist | yes | Refs |
| naratriptan | Anti-Migraine | 5ht1d_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1998 | small molecule | agonist | yes | Refs |
| naratriptan | Anti-Migraine | 5ht1f_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1998 | small molecule | agonist | yes | Refs |
| naratriptan | Anti-Migraine | 5ht1b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1998 | small molecule | agonist | yes | Refs |
| naratriptan | Anti-Migraine | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1998 | small molecule | agonist | yes | Refs |
| nebivolol | Antihypertensive | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2007 | small molecule | antagonist | yes | Refs |
| nebivolol | Antihypertensive | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2007 | small molecule | antagonist | yes | Refs |
| nedocromil | Anti-Allergic ; Anti-Asthmatic | cltr2_human | primary | A (Rhodopsin) | Leukotriene receptors | approved | 4 | - | 1992 | small molecule | antagonist | yes | Refs |
| nedocromil | Anti-Allergic ; Anti-Asthmatic | cltr1_human | primary | A (Rhodopsin) | Leukotriene receptors | approved | 4 | - | 1992 | small molecule | antagonist | yes | Refs |
| nefazodone | Anti-Depressant | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1994 | small molecule | antagonist | yes | Refs |
| nefazodone | Anti-Depressant | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1994 | small molecule | unknown | yes | Refs |
| nefazodone | Unipolar Depression | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1994 | small molecule | antagonist | yes | Refs |
| nefazodone | Anti-Depressant | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1994 | small molecule | antagonist | yes | Refs |
| netupitant | Antiemetics | nk1r_human | primary | A (Rhodopsin) | Tachykinin receptors | approved | 4 | - | 2014 | small molecule | antagonist | yes | Refs |
| niacin | Antihyperlipidemic | hcar2_human | primary | A (Rhodopsin) | Hydroxycarboxylic acid receptors | approved | 4 | - | 1997 | small molecule | agonist | no | Refs |
| niacin | Antihyperlipidemic | hcar3_human | primary | A (Rhodopsin) | Hydroxycarboxylic acid receptors | approved | 4 | - | 1997 | small molecule | agonist | no | Refs |
| nicergoline | Nootropic ; Vasodilator | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| nizatidine | Gi Anti-Ulcer ; Antihistamines | hrh2_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1988 | small molecule | antagonist | yes | Refs |
| norepinephrine | For Prevention Of Dermatitis During Radiotherapy | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1950 | small molecule | agonist | no | Refs |
| norepinephrine | Antihypotensive ; Vasoconstrictor | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1950 | small molecule | agonist | no | Refs |
| norepinephrine | For Prevention Of Dermatitis During Radiotherapy | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1950 | small molecule | agonist | no | Refs |
| norepinephrine | Antihypotensive ; Vasoconstrictor | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1950 | small molecule | agonist | no | Refs |
| norepinephrine | For Prevention Of Dermatitis During Radiotherapy | ada1d_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1950 | small molecule | agonist | no | Refs |
| norepinephrine | Antihypotensive ; Vasoconstrictor | ada1d_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1950 | small molecule | agonist | no | Refs |
| norepinephrine | For Prevention Of Dermatitis During Radiotherapy | ada2c_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1950 | small molecule | agonist | no | Refs |
| norepinephrine | Antihypotensive ; Vasoconstrictor | ada2c_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1950 | small molecule | agonist | no | Refs |
| norepinephrine | For Prevention Of Dermatitis During Radiotherapy | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1950 | small molecule | agonist | no | Refs |
| norepinephrine | Antihypotensive ; Vasoconstrictor | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1950 | small molecule | agonist | no | Refs |
| norepinephrine | For Prevention Of Dermatitis During Radiotherapy | adrb3_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1950 | small molecule | agonist | no | Refs |
| norepinephrine | Antihypotensive ; Vasoconstrictor | adrb3_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1950 | small molecule | agonist | no | Refs |
| norepinephrine | For Prevention Of Dermatitis During Radiotherapy | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1950 | small molecule | agonist | no | Refs |
| norepinephrine | Antihypotensive ; Vasoconstrictor | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1950 | small molecule | agonist | no | Refs |
| phenylephrine | Incontinence | ada1d_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1952 | small molecule | agonist | yes | Refs |
| norepinephrine | For Prevention Of Dermatitis During Radiotherapy | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1950 | small molecule | agonist | no | Refs |
| norepinephrine | Antihypotensive ; Vasoconstrictor | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1950 | small molecule | agonist | no | Refs |
| norepinephrine | For Prevention Of Dermatitis During Radiotherapy | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1950 | small molecule | agonist | no | Refs |
| norepinephrine | Antihypotensive ; Vasoconstrictor | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1950 | small molecule | agonist | no | Refs |
| octreotide | Growth Hormone Excess | ssr3_human | primary | A (Rhodopsin) | Somatostatin receptors | approved | 4 | - | 1988 | peptide | agonist | yes | Refs |
| octreotide | Growth Hormone Excess | ssr4_human | primary | A (Rhodopsin) | Somatostatin receptors | approved | 4 | - | 1988 | peptide | agonist | yes | Refs |
| octreotide | Antineoplastic | ssr1_human | primary | A (Rhodopsin) | Somatostatin receptors | approved | 4 | - | 1988 | peptide | agonist | yes | Refs |
| octreotide | Antihypertensive | ssr1_human | primary | A (Rhodopsin) | Somatostatin receptors | approved | 4 | - | 1988 | peptide | agonist | yes | Refs |
| olanzapine | Anti-Depressant | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olmesartan medoxomil | Cardiovascular Disease | agtr1_human | primary | A (Rhodopsin) | Angiotensin receptors | approved | 4 | - | 2002 | small molecule | antagonist | yes | Refs |
| octreotide | Antineoplastic | ssr5_human | primary | A (Rhodopsin) | Somatostatin receptors | approved | 4 | - | 1988 | peptide | agonist | yes | Refs |
| octreotide | Antihypertensive | ssr5_human | primary | A (Rhodopsin) | Somatostatin receptors | approved | 4 | - | 1988 | peptide | agonist | yes | Refs |
| olanzapine | Schizophrenia | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Schizophrenia | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| octreotide | Antineoplastic | ssr2_human | primary | A (Rhodopsin) | Somatostatin receptors | approved | 4 | - | 1988 | peptide | agonist | yes | Refs |
| octreotide | Antihypertensive | ssr2_human | primary | A (Rhodopsin) | Somatostatin receptors | approved | 4 | - | 1988 | peptide | agonist | yes | Refs |
| olanzapine | Anti-Depressant | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Schizophrenia | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Anti-Depressant | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Anti-Depressant | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Schizophrenia | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Anti-Depressant | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Anti-Depressant | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Anti-Depressant | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Schizophrenia | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olodaterol | Chronic Obstructive Pulmonary Disease (Copd) | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2014 | small molecule | agonist | yes | Refs |
| olanzapine | Anti-Depressant | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Schizophrenia | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Schizophrenia | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Anti-Depressant | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Schizophrenia | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olopatadine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olmesartan medoxomil | Antiglaucomic | agtr1_human | primary | A (Rhodopsin) | Angiotensin receptors | approved | 4 | - | 2002 | small molecule | antagonist | yes | Refs |
| olmesartan medoxomil | Antihypertensive | agtr1_human | primary | A (Rhodopsin) | Angiotensin receptors | approved | 4 | - | 2002 | small molecule | antagonist | yes | Refs |
| orphenadrine | Antiparkinson S; Muscle Relaxants; Central | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1957 | small molecule | antagonist | yes | Refs |
| oxprenolol | Antihypertensive ; Anti-Arrhythmia | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1983 | small molecule | antagonist | yes | Refs |
| oxprenolol | Antihypertensive ; Anti-Arrhythmia | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1983 | small molecule | antagonist | yes | Refs |
| oxybutynin | Overactive Bladder | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1975 | small molecule | antagonist | yes | Refs |
| oxybutynin | Incontinence | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1975 | small molecule | antagonist | yes | Refs |
| oxybutynin | Overactive Bladder | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1975 | small molecule | antagonist | yes | Refs |
| oxybutynin | Incontinence | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1975 | small molecule | antagonist | yes | Refs |
| oxybutynin | Incontinence | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1975 | small molecule | antagonist | yes | Refs |
| oxybutynin | Overactive Bladder | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1975 | small molecule | antagonist | yes | Refs |
| oxytocin | Analgesics | oxyr_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | approved | 4 | - | 1980 | peptide | agonist | yes | Refs |
| oxycodone | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2011 | small molecule | agonist | yes | Refs |
| oxycodone | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1998 | small molecule | agonist | yes | Refs |
| oxycodone | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2016 | small molecule | agonist | yes | Refs |
| oxycodone | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2006 | small molecule | agonist | yes | Refs |
| oxytocin | Autism | oxyr_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | approved | 4 | - | 1980 | peptide | agonist | yes | Refs |
| oxycodone | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2011 | small molecule | agonist | yes | Refs |
| oxycodone | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1998 | small molecule | agonist | yes | Refs |
| oxycodone | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2016 | small molecule | agonist | yes | Refs |
| oxycodone | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2006 | small molecule | agonist | yes | Refs |
| paliperidone | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2006 | small molecule | antagonist | yes | Refs |
| oxycodone | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2011 | small molecule | agonist | yes | Refs |
| oxycodone | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1998 | small molecule | agonist | yes | Refs |
| oxycodone | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2016 | small molecule | agonist | yes | Refs |
| oxycodone | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2006 | small molecule | agonist | yes | Refs |
| oxymetazoline | Analgesics | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1986 | small molecule | agonist | yes | Refs |
| oxymetazoline | Analgesics | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1986 | small molecule | agonist | yes | Refs |
| oxymorphone | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1959 | small molecule | agonist | no | Refs |
| paliperidone | Schizophrenia | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2006 | small molecule | antagonist | yes | Refs |
| oxyphencyclimine | Gi Anti-Ulcer ; Anticholinergic; Antispasmodics | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| oxyphencyclimine | Gi Anti-Ulcer ; Anticholinergic; Antispasmodics | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| oxyphencyclimine | Gi Anti-Ulcer ; Anticholinergic; Antispasmodics | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| oxyphenonium | Mydriatics | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| parathyroid hormone | Anti-Osteoporotic | pth1r_human | primary | B1 (Secretin) | Parathyroid hormone receptors | approved | 4 | - | 2015 | protein | agonist | yes | Refs |
| parathyroid hormone | Anti-Osteoporotic | pth2r_human | primary | B1 (Secretin) | Parathyroid hormone receptors | approved | 4 | - | 2015 | protein | agonist | yes | Refs |
| parathyroid hormone | Hypoparathyroidism | pth1r_human | primary | B1 (Secretin) | Parathyroid hormone receptors | approved | 4 | - | 2015 | protein | agonist | yes | Refs |
| parathyroid hormone | Control Hypocalcemia | pth1r_human | primary | B1 (Secretin) | Parathyroid hormone receptors | approved | 4 | - | 2015 | protein | agonist | yes | Refs |
| pentagastrin | Diagnostic | gasr_human | primary | A (Rhodopsin) | Cholecystokinin receptors | approved | 4 | - | 1974 | small molecule | agonist | no | Refs |
| pentazocine | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1967 | small molecule | agonist | yes | Refs |
| pasireotide | Antineoplastic ; Acromegaly | ssr1_human | primary | A (Rhodopsin) | Somatostatin receptors | approved | 4 | - | 2012 | peptide | agonist | yes | Refs |
| pasireotide | Antineoplastic ; Acromegaly | ssr2_human | primary | A (Rhodopsin) | Somatostatin receptors | approved | 4 | - | 2012 | peptide | agonist | yes | Refs |
| pasireotide | Antineoplastic ; Acromegaly | ssr3_human | primary | A (Rhodopsin) | Somatostatin receptors | approved | 4 | - | 2012 | peptide | agonist | yes | Refs |
| pasireotide | Antineoplastic ; Acromegaly | ssr5_human | primary | A (Rhodopsin) | Somatostatin receptors | approved | 4 | - | 2012 | peptide | agonist | yes | Refs |
| pemirolast | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1999 | small molecule | antagonist | no | Refs |
| penbutolol | Antihypertensive | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1987 | small molecule | antagonist | no | Refs |
| penbutolol | Antihypertensive | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1987 | small molecule | antagonist | no | Refs |
| pentazocine | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1967 | small molecule | antagonist | yes | Refs |
| pergolide | Antiparkinson | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1988 | small molecule | agonist | yes | Refs |
| perphenazine | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1957 | small molecule | antagonist | yes | Refs |
| perphenazine | Schizophrenia | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1957 | small molecule | antagonist | yes | Refs |
| phendimetrazine | Appetite Suppressant | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1976 | small molecule | agonist | no | Refs |
| phendimetrazine | Appetite Suppressant | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1976 | small molecule | agonist | no | Refs |
| phenindamine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1949 | small molecule | antagonist | no | Refs |
| pheniramine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1994 | small molecule | antagonist | no | Refs |
| phenoxybenzamine | Cardiovascular Disease | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1953 | small molecule | antagonist | yes | Refs |
| phenoxybenzamine | Anticonvulsants; Hypnotics And Sedatives | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1953 | small molecule | antagonist | yes | Refs |
| phentolamine | Sexual Dysfunction | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1952 | small molecule | antagonist | yes | Refs |
| phentolamine | Antihypertensive | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1952 | small molecule | antagonist | yes | Refs |
| phentolamine | Sexual Dysfunction | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1952 | small molecule | antagonist | yes | Refs |
| phenylephrine | Incontinence | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1952 | small molecule | agonist | yes | Refs |
| phenylephrine | Incontinence | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1952 | small molecule | agonist | yes | Refs |
| phenylpropanolamine | Appetite Depressants; Nasal Decongestants | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1958 | small molecule | agonist | yes | Refs |
| phenylpropanolamine | Appetite Depressants; Nasal Decongestants | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1958 | small molecule | agonist | yes | Refs |
| pilocarpine | Incontinence | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1974 | small molecule | agonist | yes | Refs |
| pilocarpine | Incontinence | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1974 | small molecule | agonist | yes | Refs |
| pilocarpine | Incontinence | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1974 | small molecule | agonist | yes | Refs |
| pimavanserin | Antiparkinson | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2016 | small molecule | inverse agonist | no | Refs |
| pimozide | Psychosis | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1984 | small molecule | antagonist | yes | Refs |
| pimozide | Antidyskinetics; Antipsychotic | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1984 | small molecule | antagonist | yes | Refs |
| pindolol | Antihypertensive | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1982 | small molecule | partial agonist | yes | Refs |
| pindolol | Antihypertensive | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1982 | small molecule | partial agonist | yes | Refs |
| pipotiazine | Antipsychotic | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1980 | small molecule | antagonist | yes | Refs |
| pipotiazine | Antipsychotic | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1980 | small molecule | antagonist | yes | Refs |
| pipotiazine | Antipsychotic | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1980 | small molecule | antagonist | yes | Refs |
| pipotiazine | Antipsychotic | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1980 | small molecule | antagonist | yes | Refs |
| pirbuterol | Obstructive Lung Disease | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1986 | small molecule | agonist | no | Refs |
| pirenzepine | Gi Anti-Ulcer ; Anticholinergic; Antispasmodics | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | - | small molecule | antagonist | yes | Refs |
| plerixafor | Antineoplastic | cxcr4_human | primary | A (Rhodopsin) | Chemokine receptors | approved | 4 | - | 2008 | small molecule | partial agonist | no | Refs |
| practolol | Anti-Arrhythmia | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| pramipexole | Antiparkinson | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1997 | small molecule | agonist | yes | Refs |
| pramlintide acetate | Antidiabetic | calcr_human | primary | B1 (Secretin) | Calcitonin receptors | approved | 4 | - | 2005 | peptide | agonist | no | Refs |
| pramipexole | Antiparkinson | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1997 | small molecule | agonist | yes | Refs |
| pramipexole | Antiparkinson | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1997 | small molecule | agonist | yes | Refs |
| pranlukast | Anti-Asthmatic | cltr1_human | primary | A (Rhodopsin) | Leukotriene receptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| prasugrel | Antithrombotic | p2y12_human | primary | A (Rhodopsin) | P2Y receptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| prazosin | Antihypertensive ; Antispasmodics | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1976 | small molecule | antagonist | yes | Refs |
| prazosin | Antihypertensive ; Antispasmodics | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1976 | small molecule | antagonist | yes | Refs |
| prazosin | Antihypertensive ; Antispasmodics | ada1d_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1976 | small molecule | antagonist | yes | Refs |
| prochlorperazine | Antiemetics | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1956 | small molecule | antagonist | yes | Refs |
| procyclidine | Antidyskinetics; Antiparkinson S | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1955 | small molecule | antagonist | yes | Refs |
| procyclidine | Antidyskinetics; Antiparkinson S | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1955 | small molecule | antagonist | yes | Refs |
| procyclidine | Antidyskinetics; Antiparkinson S | acm4_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1955 | small molecule | antagonist | yes | Refs |
| progabide | Anticonvulsants | gabr1_human | primary | C (Glutamate) | GABAB receptors | approved | 4 | - | - | small molecule | agonist | no | Refs |
| promazine | Psychosis | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1956 | small molecule | antagonist | yes | Refs |
| promazine | Antiemetics; Antipsychotic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1956 | small molecule | antagonist | yes | Refs |
| promazine | Antiemetics; Antipsychotic | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1956 | small molecule | antagonist | yes | Refs |
| promazine | Antiemetics; Antipsychotic | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1956 | small molecule | antagonist | yes | Refs |
| promazine | Antiemetics; Antipsychotic | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1956 | small molecule | antagonist | yes | Refs |
| promazine | Antiemetics; Antipsychotic | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1956 | small molecule | antagonist | yes | Refs |
| promazine | Antiemetics; Antipsychotic | acm4_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1956 | small molecule | antagonist | yes | Refs |
| promazine | Antiemetics; Antipsychotic | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1956 | small molecule | antagonist | yes | Refs |
| promazine | Antiemetics; Antipsychotic | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1956 | small molecule | antagonist | yes | Refs |
| promazine | Antiemetics; Antipsychotic | ada1d_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1956 | small molecule | antagonist | yes | Refs |
| promazine | Antiemetics; Antipsychotic | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1956 | small molecule | antagonist | yes | Refs |
| promazine | Antiemetics; Antipsychotic | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1956 | small molecule | antagonist | yes | Refs |
| promazine | Antiemetics; Antipsychotic | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1956 | small molecule | antagonist | yes | Refs |
| promazine | Antiemetics; Antipsychotic | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1956 | small molecule | antagonist | yes | Refs |
| promethazine | Hypnotics And Sedatives; Anti-Anxiety S; Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1951 | small molecule | antagonist | yes | Refs |
| promazine | Antiemetics; Antipsychotic | acm5_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1956 | small molecule | antagonist | yes | Refs |
| propantheline | Gi Anti-Ulcer ; Anticholinergic; Antispasmodics | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1953 | small molecule | antagonist | yes | Refs |
| propericiazine | Schizophrenia | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| propiomazine | Hypnotics And Sedatives | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1960 | small molecule | antagonist | no | Refs |
| propiomazine | Hypnotics And Sedatives | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1960 | small molecule | antagonist | no | Refs |
| propiomazine | Hypnotics And Sedatives | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1960 | small molecule | antagonist | no | Refs |
| propiomazine | Hypnotics And Sedatives | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1960 | small molecule | antagonist | no | Refs |
| propiomazine | Hypnotics And Sedatives | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1960 | small molecule | antagonist | no | Refs |
| propiomazine | Hypnotics And Sedatives | acm4_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1960 | small molecule | antagonist | no | Refs |
| propiomazine | Hypnotics And Sedatives | acm5_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1960 | small molecule | antagonist | no | Refs |
| propiomazine | Hypnotics And Sedatives | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1960 | small molecule | antagonist | no | Refs |
| propiomazine | Hypnotics And Sedatives | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1960 | small molecule | antagonist | no | Refs |
| propiomazine | Hypnotics And Sedatives | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1960 | small molecule | antagonist | no | Refs |
| propiomazine | Hypnotics And Sedatives | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1960 | small molecule | antagonist | no | Refs |
| propoxyphene | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1957 | small molecule | agonist | yes | Refs |
| propoxyphene | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1957 | small molecule | agonist | yes | Refs |
| propoxyphene | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1957 | small molecule | agonist | yes | Refs |
| propranolol | Cancer Cachexia | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1967 | small molecule | antagonist | yes | Refs |
| protirelin | Diagnostic | trfr_human | primary | A (Rhodopsin) | Thyrotropin-releasing hormone receptors | approved | 4 | - | 1976 | small molecule | agonist | no | Refs |
| prucalopride | Motilitant | 5ht4r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2009 | small molecule | agonist | yes | Refs |
| pseudoephedrine | Anti-Allergic | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1975 | small molecule | agonist | yes | Refs |
| pseudoephedrine | Anti-Allergic | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1975 | small molecule | agonist | yes | Refs |
| pyrilamine | Pruritus | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1973 | small molecule | antagonist | no | Refs |
| quetiapine | Antipsychotic ; Anti-Depressant | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1997 | small molecule | antagonist | yes | Refs |
| quetiapine | Antipsychotic ; Anti-Depressant | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1997 | small molecule | antagonist | yes | Refs |
| ramelteon | Insomnia | mtr1a_human | primary | A (Rhodopsin) | Melatonin | approved | 4 | - | 2005 | small molecule | agonist | no | Refs |
| ramelteon | Insomnia | mtr1b_human | primary | A (Rhodopsin) | Melatonin | approved | 4 | - | 2005 | small molecule | agonist | no | Refs |
| rizatriptan | Anti-Migraine | 5ht1d_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1998 | small molecule | agonist | yes | Refs |
| ranitidine | Antiulcer | hrh2_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1977 | small molecule | antagonist | yes | Refs |
| rizatriptan | Anti-Migraine | 5ht1b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1998 | small molecule | agonist | yes | Refs |
| rocuronium | Muscle Relaxants | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2008 | small molecule | antagonist | no | Refs |
| rauwolfia serpentina | Antihypertensive | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| rauwolfia serpentina | Antihypertensive | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| rauwolfia serpentina | Antihypertensive | ada1d_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| rauwolfia serpentina | Antihypertensive | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| rauwolfia serpentina | Antihypertensive | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| rauwolfia serpentina | Antihypertensive | ada2c_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| regadenoson | Diagnostic | aa2ar_human | primary | A (Rhodopsin) | Adenosine receptors | approved | 4 | - | 2008 | small molecule | agonist | no | Refs |
| remifentanil | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1996 | small molecule | agonist | yes | Refs |
| remoxipride | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1990 | small molecule | antagonist | no | Refs |
| ridogrelum | For The Prevention Of Systemic Thrombo-Embolism; Adjunctive To Thrombolytic Therapy | ta2r_human | primary | A (Rhodopsin) | Prostanoid receptors | approved | 4 | - | - | small molecule | antagonist | no | Refs |
| rimonabant | Anti-Obesity | cnr1_human | primary | A (Rhodopsin) | Cannabinoid receptors | withdrawn | 4 | - | 2007 | small molecule | antagonist | yes | Refs |
| rolapitant | Antiemetics | nk1r_human | primary | A (Rhodopsin) | Tachykinin receptors | approved | 4 | - | 2015 | small molecule | antagonist | no | Refs |
| risperidone | Schizophrenia | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1993 | small molecule | antagonist | yes | Refs |
| risperidone | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1993 | small molecule | antagonist | yes | Refs |
| ritodrine | Tocolytic | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1987 | small molecule | agonist | yes | Refs |
| ropinirole | Antiparkinson | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1997 | small molecule | agonist | yes | Refs |
| ropinirole | Antiparkinson | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1997 | small molecule | agonist | yes | Refs |
| ropinirole | Antiparkinson | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1997 | small molecule | agonist | yes | Refs |
| salbutamol | Symptomatic Exophthalmos Associated With Thyroid-Related Eye Disease | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1981 | small molecule | agonist | yes | Refs |
| rotigotine | Antiparkinson | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2006 | small molecule | agonist | yes | Refs |
| rotigotine | Antiparkinson | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2006 | small molecule | agonist | yes | Refs |
| rotigotine | Antiparkinson | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2006 | small molecule | agonist | yes | Refs |
| rupatadine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 2016 | small molecule | antagonist | yes | Refs |
| rupatadine | Anti-Allergic | ptafr_human | primary | A (Rhodopsin) | Platelet-activating factor receptors | approved | 4 | - | 2016 | small molecule | antagonist | yes | Refs |
| sermorelin | Hormone Replacement | ghrhr_human | primary | B1 (Secretin) | Glucagon receptor family | approved | 4 | - | 1990 | peptide | agonist | no | Refs |
| salbutamol | Chronic Obstructive Pulmonary Disease (Copd) | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1981 | small molecule | agonist | yes | Refs |
| salbutamol | Bronchodilator | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1981 | small molecule | agonist | yes | Refs |
| amiodarone | Anti-Arrhythmia | ada1a_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1985 | small molecule | antagonist | yes | Refs |
| salmeterol | Bronchodilator | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1994 | small molecule | agonist | yes | Refs |
| scopolamine | Adjuvants; Anesthesia; Antispasmodics; Mydriatics | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1953 | small molecule | antagonist | no | Refs |
| secretin | Diagnostic | sctr_human | primary | B1 (Secretin) | Glucagon receptor family | approved | 4 | - | 2002 | peptide | agonist | no | Refs |
| selexipag | Antihypertensive | pi2r_human | primary | A (Rhodopsin) | Prostanoid receptors | approved | 4 | - | 2015 | small molecule | agonist | no | Refs |
| silodosin | Bph-Related Urinary Symptoms | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2008 | small molecule | antagonist | no | Refs |
| solifenacin | Incontinence | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2004 | small molecule | antagonist | yes | Refs |
| sitaxentan | Antihypertensive | ednra_human | primary | A (Rhodopsin) | Endothelin receptors | approved | 4 | - | 2006 | small molecule | antagonist | yes | Refs |
| sonidegib | Antineoplastic | smo_human | primary | F (Frizzled) | Frizzled | approved | 4 | - | 2015 | small molecule | antagonist | no | Refs |
| sotalol | Cardiovascular Disease | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1992 | small molecule | antagonist | yes | Refs |
| sotalol | Atrial Fibrillation | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1992 | small molecule | antagonist | yes | Refs |
| succinylcholine | Muscle Relaxants; Skeletal | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1952 | small molecule | agonist | no | Refs |
| sufentanil | Analgesics; Adjuvant To Anesthesia | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1984 | small molecule | agonist | no | Refs |
| sumatriptan | Anti-Migraine | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2008 | small molecule | agonist | yes | Refs |
| sumatriptan | Anti-Migraine | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1992 | small molecule | agonist | yes | Refs |
| sumatriptan | Anti-Migraine | 5ht1f_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2008 | small molecule | agonist | yes | Refs |
| tapentadol | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2008 | small molecule | agonist | yes | Refs |
| sumatriptan | Anti-Migraine | 5ht1f_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1992 | small molecule | agonist | yes | Refs |
| sumatriptan | Anti-Migraine | 5ht1b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2008 | small molecule | agonist | yes | Refs |
| tetrahydrozoline | Eye Allergy | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1979 | small molecule | agonist | no | Refs |
| tasimelteon | Hypnotics And Sedatives | mtr1a_human | primary | A (Rhodopsin) | Melatonin | approved | 4 | - | 2014 | small molecule | agonist | no | Refs |
| tasimelteon | Hypnotics And Sedatives | mtr1b_human | primary | A (Rhodopsin) | Melatonin | approved | 4 | - | 2014 | small molecule | agonist | no | Refs |
| sumatriptan | Anti-Migraine | 5ht1b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1992 | small molecule | agonist | yes | Refs |
| sumatriptan | Anti-Migraine | 5ht1d_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2008 | small molecule | agonist | yes | Refs |
| teduglutide | Short Bowel Syndrome | glp2r_human | primary | B1 (Secretin) | Glucagon receptor family | approved | 4 | - | 2012 | peptide | agonist | no | Refs |
| sumatriptan | Anti-Migraine | 5ht1d_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1992 | small molecule | agonist | yes | Refs |
| suramin | African Trypanosomiasis | p2ry2_human | primary | A (Rhodopsin) | P2Y receptors | approved | 4 | - | 1916 | small molecule | antagonist | no | Refs |
| tegaserod | Motilitant | 5ht4r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2002 | small molecule | partial agonist | no | Refs |
| suvorexant | Hypnotics And Sedatives | ox1r_human | primary | A (Rhodopsin) | Orexin receptors | approved | 4 | - | 2014 | small molecule | antagonist | no | Refs |
| suvorexant | Hypnotics And Sedatives | ox2r_human | primary | A (Rhodopsin) | Orexin receptors | approved | 4 | - | 2014 | small molecule | antagonist | no | Refs |
| tafluprost | Reduce Intraocular Pressure | pf2r_human | primary | A (Rhodopsin) | Prostanoid receptors | approved | 4 | - | 2012 | small molecule | agonist | yes | Refs |
| tamsulosin | Urinary Symptoms Associated With Bph | ada1d_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1997 | small molecule | antagonist | yes | Refs |
| tamsulosin | Benign Prostatic Hyperplasia | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1997 | small molecule | antagonist | yes | Refs |
| tamsulosin | Urinary Symptoms Associated With Bph | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1997 | small molecule | antagonist | yes | Refs |
| tamsulosin | Urinary Symptoms Associated With Bph | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1997 | small molecule | antagonist | yes | Refs |
| telmisartan | Antihypertensive | agtr1_human | primary | A (Rhodopsin) | Angiotensin receptors | approved | 4 | - | 1998 | small molecule | antagonist | yes | Refs |
| terazosin | Antineoplastic S; Antihypertensive | ada1d_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1987 | small molecule | antagonist | yes | Refs |
| terazosin | Antineoplastic S; Antihypertensive | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1987 | small molecule | antagonist | yes | Refs |
| terazosin | Antineoplastic S; Antihypertensive | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1987 | small molecule | antagonist | yes | Refs |
| terbutaline | Bronchodilator ; Tocolytic | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1974 | small molecule | agonist | yes | Refs |
| terfenadine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1985 | small molecule | antagonist | yes | Refs |
| teriparatide | Anti-Osteoporotic | pth1r_human | primary | B1 (Secretin) | Parathyroid hormone receptors | approved | 4 | - | 1987 | peptide | agonist | yes | Refs |
| terlipressin | Hepatorenal Syndrome | v2r_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | approved | 4 | - | 2003 | small molecule | agonist | yes | Refs |
| terlipressin | Hepatorenal Syndrome | v1br_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | approved | 4 | - | 2003 | small molecule | agonist | yes | Refs |
| terlipressin | Hepatorenal Syndrome | v1ar_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | approved | 4 | - | 2003 | small molecule | agonist | yes | Refs |
| tesamorelin | Hiv-Associated Lipodystrophy | ghrhr_human | primary | B1 (Secretin) | Glucagon receptor family | approved | 4 | - | 2010 | peptide | agonist | no | Refs |
| tetrahydrocannabinol | Analgesics; Neuropathic Pain; Restlegs Legs Syndrome | cnr1_human | primary | A (Rhodopsin) | Cannabinoid receptors | approved | 4 | - | 1985 | plant extract | agonist | no | Refs |
| tetrahydrocannabinol | Analgesics; Neuropathic Pain; Restlegs Legs Syndrome | cnr2_human | primary | A (Rhodopsin) | Cannabinoid receptors | approved | 4 | - | 1985 | plant extract | agonist | no | Refs |
| tetryzoline | For Eye Irritation, Decongestant | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1982 | small molecule | agonist | no | Refs |
| theophylline | Bronchodilator | aa2br_human | primary | A (Rhodopsin) | Adenosine receptors | approved | 4 | - | 1976 | small molecule | antagonist | yes | Refs |
| theophylline | Bronchodilator | aa1r_human | primary | A (Rhodopsin) | Adenosine receptors | approved | 4 | - | 1976 | small molecule | antagonist | yes | Refs |
| theophylline | Bronchodilator | aa2ar_human | primary | A (Rhodopsin) | Adenosine receptors | approved | 4 | - | 1976 | small molecule | antagonist | yes | Refs |
| thiethylperazine | Antiemetics | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1961 | small molecule | antagonist | no | Refs |
| thiethylperazine | Antiemetics | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1961 | small molecule | antagonist | no | Refs |
| thiethylperazine | Antiemetics | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1961 | small molecule | antagonist | no | Refs |
| thiethylperazine | Antiemetics | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1961 | small molecule | antagonist | no | Refs |
| thiethylperazine | Antiemetics | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1961 | small molecule | antagonist | no | Refs |
| thiethylperazine | Antiemetics | acm4_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1961 | small molecule | antagonist | no | Refs |
| thiethylperazine | Antiemetics | acm5_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1961 | small molecule | antagonist | no | Refs |
| thiethylperazine | Antiemetics | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1961 | small molecule | antagonist | no | Refs |
| thiethylperazine | Antiemetics | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1961 | small molecule | antagonist | no | Refs |
| thiethylperazine | Antiemetics | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1961 | small molecule | antagonist | no | Refs |
| thiethylperazine | Antiemetics | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1961 | small molecule | antagonist | no | Refs |
| thioproperazine | Antipsychotic | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1962 | small molecule | antagonist | no | Refs |
| thioproperazine | Antipsychotic | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1962 | small molecule | antagonist | no | Refs |
| thioproperazine | Antipsychotic | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1962 | small molecule | antagonist | no | Refs |
| thioproperazine | Antipsychotic | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1962 | small molecule | antagonist | no | Refs |
| thioridazine | Schizophrenia | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1962 | small molecule | antagonist | yes | Refs |
| thioridazine | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1962 | small molecule | antagonist | yes | Refs |
| thioridazine | Schizophrenia | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1962 | small molecule | antagonist | yes | Refs |
| thioridazine | Schizophrenia | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1962 | small molecule | antagonist | yes | Refs |
| thiothixene | Psychosis | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1967 | small molecule | antagonist | no | Refs |
| thiothixene | Psychosis | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1967 | small molecule | antagonist | no | Refs |
| thyrotropin alfa | Diagnostic | tshr_human | primary | A (Rhodopsin) | Glycoprotein hormone receptors | approved | 4 | - | 1998 | protein | agonist | yes | Refs |
| ticagrelor | Antithrombotic | p2y12_human | primary | A (Rhodopsin) | P2Y receptors | approved | 4 | - | 2010 | small molecule | NAM | yes | Refs |
| ticlopidine | Platelet Aggregation Inhibitors | p2y12_human | primary | A (Rhodopsin) | P2Y receptors | approved | 4 | - | 1991 | small molecule | antagonist | yes | Refs |
| tramadol | Analgesics | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1995 | small molecule | agonist | yes | Refs |
| timolol | Antiglaucomic | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1981 | small molecule | antagonist | yes | Refs |
| tizanidine | Muscle Relaxants | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | agonist | yes | Refs |
| tizanidine | Muscle Relaxants | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | agonist | yes | Refs |
| tizanidine | Muscle Relaxants | ada2c_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | agonist | yes | Refs |
| timolol | Antiglaucomic | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1981 | small molecule | antagonist | yes | Refs |
| tiotropium | Cystic Fibrosis; Chronic Obstructive Pulmonary Disorder (Copd) | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2004 | small molecule | antagonist | yes | Refs |
| tiotropium | Chronic Obstructive Pulmonary Disease (Copd) | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2004 | small molecule | antagonist | yes | Refs |
| tiotropium | Cystic Fibrosis; Chronic Obstructive Pulmonary Disorder (Copd) | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2004 | small molecule | antagonist | yes | Refs |
| tiotropium | Chronic Obstructive Pulmonary Disease (Copd) | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2004 | small molecule | antagonist | yes | Refs |
| tiotropium | Cystic Fibrosis; Chronic Obstructive Pulmonary Disorder (Copd) | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2004 | small molecule | antagonist | yes | Refs |
| tiotropium | Chronic Obstructive Pulmonary Disease (Copd) | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2004 | small molecule | antagonist | yes | Refs |
| tolazoline | Antihypertensive | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1948 | small molecule | agonist | no | Refs |
| tizanidine | Skeletal Muscular Spasticity | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | agonist | yes | Refs |
| tizanidine | Skeletal Muscular Spasticity | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | agonist | yes | Refs |
| tizanidine | Skeletal Muscular Spasticity | ada2c_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | agonist | yes | Refs |
| tolterodine | Incontinence | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1998 | small molecule | antagonist | yes | Refs |
| tolterodine | Incontinence | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1998 | small molecule | antagonist | yes | Refs |
| tolterodine | Incontinence | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1998 | small molecule | antagonist | yes | Refs |
| tolvaptan | Antihypertensive | v2r_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| travoprost | Antiglaucomic | pf2r_human | primary | A (Rhodopsin) | Prostanoid receptors | approved | 4 | - | 2001 | small molecule | agonist | yes | Refs |
| tramadol | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1995 | small molecule | agonist | yes | Refs |
| trazodone | Anti-Depressant | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1981 | small molecule | partial agonist | yes | Refs |
| tramadol | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1995 | small molecule | agonist | yes | Refs |
| trazodone | Anti-Depressant | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1981 | small molecule | antagonist | yes | Refs |
| trazodone | Anti-Depressant | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1981 | small molecule | antagonist | yes | Refs |
| trifluoperazine | Psychosis | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1959 | small molecule | antagonist | yes | Refs |
| treprostinil | Antihypertensive | p2y12_human | primary | A (Rhodopsin) | P2Y receptors | approved | 4 | - | 2002 | small molecule | agonist | no | Refs |
| treprostinil | Antihypertensive ; Antithrombotic | p2y12_human | primary | A (Rhodopsin) | P2Y receptors | approved | 4 | - | 2002 | small molecule | agonist | no | Refs |
| treprostinil | Antihypertensive | pi2r_human | primary | A (Rhodopsin) | Prostanoid receptors | approved | 4 | - | 2002 | small molecule | agonist | no | Refs |
| trifluoperazine | Antiemetics; Antipsychotic | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1959 | small molecule | antagonist | yes | Refs |
| tridihexethyl | Gi Anti-Ulcer ; Anticholinergic; Antispasmodics | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1954 | small molecule | antagonist | no | Refs |
| tridihexethyl | Gi Anti-Ulcer ; Anticholinergic; Antispasmodics | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1954 | small molecule | antagonist | no | Refs |
| tridihexethyl | Gi Anti-Ulcer ; Anticholinergic; Antispasmodics | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1954 | small molecule | antagonist | no | Refs |
| trifluoperazine | Psychosis | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1959 | small molecule | antagonist | yes | Refs |
| trifluoperazine | Antiemetics; Antipsychotic | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1959 | small molecule | antagonist | yes | Refs |
| triflupromazine | Antiemetics; Antipsychotic | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1957 | small molecule | antagonist | no | Refs |
| triflupromazine | Antiemetics; Antipsychotic | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1957 | small molecule | antagonist | no | Refs |
| triflupromazine | Antiemetics; Antipsychotic | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1957 | small molecule | antagonist | no | Refs |
| triflupromazine | Antiemetics; Antipsychotic | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1957 | small molecule | antagonist | no | Refs |
| triflupromazine | Antiemetics; Antipsychotic | 5ht2b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1957 | small molecule | antagonist | no | Refs |
| trihexyphenidyl | Antiparkinson | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1949 | small molecule | antagonist | yes | Refs |
| trimeprazine | Antipruritics | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| zolmitriptan | Anti-Migraine | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1997 | small molecule | agonist | yes | Refs |
| vilanterol | Chronic Obstructive Pulmonary Disease (Copd) | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2013 | small molecule | agonist | yes | Refs |
| trimipramine | Unipolar Depression | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1979 | small molecule | antagonist | yes | Refs |
| trimipramine | Unipolar Depression | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1979 | small molecule | antagonist | yes | Refs |
| trimipramine | Unipolar Depression | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1979 | small molecule | antagonist | yes | Refs |
| trimipramine | Unipolar Depression | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1979 | small molecule | antagonist | yes | Refs |
| trimipramine | Unipolar Depression | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1979 | small molecule | antagonist | yes | Refs |
| trimipramine | Unipolar Depression | ada1d_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1979 | small molecule | antagonist | yes | Refs |
| trimipramine | Unipolar Depression | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1979 | small molecule | antagonist | yes | Refs |
| tripelennamine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1948 | small molecule | antagonist | no | Refs |
| triprolidine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| triptorelin | Antineoplastic | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | approved | 4 | - | 2001 | small molecule | agonist | yes | Refs |
| triptorelin | Palliiative Treatment Of Advanced Prostate Cancer | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | approved | 4 | - | 2001 | small molecule | agonist | yes | Refs |
| tropicamide | Diagnostic | acm4_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1960 | small molecule | antagonist | yes | Refs |
| trospium | Incontinence | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2004 | small molecule | antagonist | yes | Refs |
| vilazodone | Anti-Depressant | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2011 | small molecule | agonist | no | Refs |
| umeclidinium | Bronchodilator ; Copd | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2013 | small molecule | antagonist | yes | Refs |
| umeclidinium | Bronchodilator ; Copd | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2013 | small molecule | antagonist | yes | Refs |
| umeclidinium | Chronic Obstructive Pulmonary Disease (Copd) | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2013 | small molecule | antagonist | yes | Refs |
| umeclidinium | Chronic Obstructive Pulmonary Disease (Copd) | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2013 | small molecule | antagonist | yes | Refs |
| urofollitropin | Fertility | fshr_human | primary | A (Rhodopsin) | Glycoprotein hormone receptors | approved | 4 | - | 1986 | protein | agonist | yes | Refs |
| vismodegib | Antineoplastic | smo_human | primary | F (Frizzled) | Frizzled | approved | 4 | - | 2012 | small molecule | antagonist | no | Refs |
| valsartan | Antihypertensive | agtr1_human | primary | A (Rhodopsin) | Angiotensin receptors | approved | 4 | - | 2012 | small molecule | antagonist | yes | Refs |
| vapreotide | Liver Cirrhosis-Related Variceal Bleeding | ssr2_human | primary | A (Rhodopsin) | Somatostatin receptors | approved | 4 | - | - | small molecule | agonist | no | Refs |
| vapreotide | Liver Cirrhosis-Related Variceal Bleeding | ssr5_human | primary | A (Rhodopsin) | Somatostatin receptors | approved | 4 | - | - | small molecule | agonist | no | Refs |
| vasopressin | Antidiuretic | v2r_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | approved | 4 | - | 1982 | peptide | agonist | no | Refs |
| vasopressin | Antidiuretic | v1br_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | approved | 4 | - | 1982 | peptide | agonist | no | Refs |
| vasopressin | Antidiuretic | v1ar_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | approved | 4 | - | 1982 | peptide | agonist | no | Refs |
| vigabatrin | Addiction | gabr1_human | primary | C (Glutamate) | GABAB receptors | approved | 4 | - | 2009 | small molecule | agonist | yes | Refs |
| vorapaxar | Cardiovascular Disease | par1_human | primary | A (Rhodopsin) | Proteinase-activated receptors | approved | 4 | - | 2014 | small molecule | antagonist | no | Refs |
| zolmitriptan | Anti-Migraine | 5ht1d_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1997 | small molecule | agonist | yes | Refs |
| vortioxetine | Anti-Depressant | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2013 | small molecule | agonist | yes | Refs |
| vortioxetine | Anti-Depressant | 5ht1b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2013 | small molecule | agonist | yes | Refs |
| vortioxetine | Anti-Depressant | 5ht7r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2013 | small molecule | agonist | yes | Refs |
| xylometazoline | Decongestant | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1959 | small molecule | agonist | yes | Refs |
| xylometazoline | Decongestant | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1959 | small molecule | agonist | yes | Refs |
| xylometazoline | Decongestant | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1959 | small molecule | agonist | yes | Refs |
| zafirlukast | Anti-Asthmatic | cltr1_human | primary | A (Rhodopsin) | Leukotriene receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| ziprasidone | Schizophrenia | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2001 | small molecule | antagonist | yes | Refs |
| ziprasidone | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2001 | small molecule | antagonist | yes | Refs |
| zolmitriptan | Anti-Migraine | 5ht1b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1997 | small molecule | agonist | yes | Refs |
| zolmitriptan | Anti-Migraine | 5ht1f_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1997 | small molecule | agonist | yes | Refs |
| zuclopenthixol | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1962 | small molecule | antagonist | yes | Refs |
| zuclopenthixol | Schizophrenia | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1962 | small molecule | antagonist | yes | Refs |
| zuclopenthixol | Schizophrenia | drd5_human | primary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1962 | small molecule | antagonist | yes | Refs |
| agomelatine | Anti-Depressant | 5ht2b_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| ambrisentan | Antihypertensive | ednrb_human | secondary | A (Rhodopsin) | Endothelin receptors | approved | 4 | - | 2007 | small molecule | antagonist | yes | Refs |
| asenapine | Schizophrenia | drd4_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| asenapine | Schizophrenia | 5ht2b_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| asenapine | Schizophrenia | drd1_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| asenapine | Schizophrenia | hrh1_human | secondary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| asenapine | Schizophrenia | hrh2_human | secondary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| asenapine | Schizophrenia | ada1a_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| asenapine | Schizophrenia | ada2a_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| asenapine | Schizophrenia | ada2b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| asenapine | Schizophrenia | ada2c_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| asenapine | Schizophrenia | drd3_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | yes | Refs |
| bethanechol | Eosinophilic Esophagitis | acm3_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1948 | small molecule | agonist | yes | Refs |
| bethanechol | Parasympathomimetics | acm1_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1948 | small molecule | agonist | yes | Refs |
| brexpiprazole | Anti-Depressant | 5ht7r_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2015 | small molecule | partial agonist | no | Refs |
| bromocriptine | Growth Hormone Excess | drd4_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1978 | small molecule | agonist | yes | Refs |
| buserelin | Lhrh Analogue | lshr_human | secondary | A (Rhodopsin) | Glycoprotein hormone receptors | approved | 4 | - | - | peptide | not available | yes | Refs |
| caffeine | Coronary Artery Disease | aa2br_human | secondary | A (Rhodopsin) | Adenosine receptors | approved | 4 | - | 1999 | small molecule | antagonist | yes | Refs |
| carbachol | Antiglaucomic | acm3_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1972 | small molecule | agonist | no | Refs |
| carbinoxamine | Anti-Allergic | acm1_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2003 | small molecule | antagonist | no | Refs |
| carteolol | Antiglaucomic | adrb3_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1988 | small molecule | antagonist | yes | Refs |
| carvedilol | Antihypertensive | ada1b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1995 | small molecule | antagonist | yes | Refs |
| carvedilol | Antihypertensive | adrb3_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1995 | small molecule | antagonist | yes | Refs |
| carvedilol | Cardiovascular Disease | adrb2_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1995 | small molecule | antagonist | yes | Refs |
| carvedilol | Antihypertensive | ada1d_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1995 | small molecule | antagonist | yes | Refs |
| chlorpromazine | Psychosis | drd3_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1957 | small molecule | antagonist | yes | Refs |
| chlorpromazine | Psychosis | drd4_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1957 | small molecule | antagonist | yes | Refs |
| chlorprothixene | Schizophrenia | hrh1_human | secondary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1967 | small molecule | antagonist | yes | Refs |
| chorionic gonadotropin | Fertility | fshr_human | secondary | A (Rhodopsin) | Glycoprotein hormone receptors | approved | 4 | - | 1973 | protein | agonist | no | Refs |
| clozapine | Schizophrenia | drd1_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1989 | small molecule | antagonist | yes | Refs |
| clozapine | Schizophrenia | drd4_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1989 | small molecule | antagonist | yes | Refs |
| clozapine | Schizophrenia | hrh1_human | secondary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1989 | small molecule | antagonist | yes | Refs |
| clozapine | Schizophrenia | 5ht1a_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1989 | small molecule | antagonist | yes | Refs |
| clozapine | Schizophrenia | 5ht2c_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1989 | small molecule | antagonist | yes | Refs |
| cyclobenzaprine | Spasticity | 5ht2c_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1977 | small molecule | antagonist | no | Refs |
| cyclopentolate | Cycloplegia | acm3_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1974 | small molecule | antagonist | yes | Refs |
| darifenacin | Overactive Bladder | acm2_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2004 | small molecule | antagonist | yes | Refs |
| desipramine | Anti-Depressant | adrb2_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1964 | small molecule | antagonist | no | Refs |
| desipramine | Anti-Depressant | adrb1_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1964 | small molecule | unknown | no | Refs |
| desipramine | Anti-Depressant | acm1_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1964 | small molecule | antagonist | no | Refs |
| desipramine | Anti-Depressant | acm2_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1964 | small molecule | antagonist | no | Refs |
| dicyclomine | Digestive System Disease | acm3_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1950 | small molecule | antagonist | no | Refs |
| diphemanil | Digestive System Disease | acm1_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| epinephrine | Anesthetics | ada1d_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1976 | small molecule | agonist | yes | Refs |
| dipivefrin | Antiglaucomic | ada1b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1980 | small molecule | agonist | yes | Refs |
| dipivefrin | Antiglaucomic | ada1d_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1980 | small molecule | agonist | yes | Refs |
| dipivefrin | Antiglaucomic | ada2b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1980 | small molecule | agonist | yes | Refs |
| dipivefrin | Antiglaucomic | ada2c_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1980 | small molecule | agonist | yes | Refs |
| esmolol | Tinnitus | adrb2_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1986 | small molecule | antagonist | no | Refs |
| dipivefrin | Antiglaucomic | adrb1_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1980 | small molecule | agonist | yes | Refs |
| dipivefrin | Antiglaucomic | adrb3_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1980 | small molecule | agonist | yes | Refs |
| dobutamine | Heart Failure | adrb2_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1978 | small molecule | agonist | no | Refs |
| dronabinol | Analgesics | cnr2_human | secondary | A (Rhodopsin) | Cannabinoid receptors | approved | 4 | - | 1985 | small molecule | agonist | no | Refs |
| dronabinol | Appetite Stimulant | cnr2_human | secondary | A (Rhodopsin) | Cannabinoid receptors | approved | 4 | - | 1985 | small molecule | agonist | no | Refs |
| droperidol | Vomiting | drd3_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1970 | small molecule | antagonist | no | Refs |
| droperidol | Psychosis | drd4_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1970 | small molecule | antagonist | no | Refs |
| ergoloid | Cardiovascular Disease | drd1_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1953 | small molecule | agonist | yes | Refs |
| ergoloid | Cardiovascular Disease | drd2_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1953 | small molecule | agonist | yes | Refs |
| ergoloid | Cardiovascular Disease | 5ht1a_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1953 | small molecule | agonist | yes | Refs |
| flibanserin | Sexual Dysfunction | 5ht2a_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2015 | small molecule | antagonist | no | Refs |
| ergoloid | Cardiovascular Disease | 5ht1b_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1953 | small molecule | agonist | yes | Refs |
| ergoloid | Cardiovascular Disease | drd3_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1953 | small molecule | agonist | yes | Refs |
| ergoloid | Cardiovascular Disease | drd4_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1953 | small molecule | agonist | yes | Refs |
| ergoloid | Cardiovascular Disease | drd5_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1953 | small molecule | agonist | yes | Refs |
| fluoxetine | Autism | 5ht2b_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1987 | small molecule | antagonist | yes | Refs |
| glycopyrrolate | Obstructive Lung Disease | acm3_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1961 | small molecule | antagonist | no | Refs |
| glycopyrronium | Chronic Obstructive Pulmonary Disease (Copd) | acm1_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1961 | small molecule | antagonist | yes | Refs |
| guanabenz | Antineoplastic | ada2c_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1982 | small molecule | agonist | no | Refs |
| guanfacine | Attention Deficit Hyperactivity Disorder | ada2b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1986 | small molecule | agonist | yes | Refs |
| guanfacine | Obstructive Sleep Apnea | ada2c_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1986 | small molecule | agonist | yes | Refs |
| haloperidol | Conduct Disorder | 5ht2a_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1967 | small molecule | antagonist | yes | Refs |
| haloperidol | Psychosis | drd3_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1986 | small molecule | antagonist | yes | Refs |
| haloperidol | Gastroparesis | drd3_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1967 | small molecule | antagonist | yes | Refs |
| haloperidol | Schizophrenia | drd4_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1967 | small molecule | antagonist | yes | Refs |
| haloperidol | Psychosis | 5ht2a_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1986 | small molecule | antagonist | yes | Refs |
| hydrocodone | Analgesics | oprk_human | secondary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 2013 | small molecule | agonist | no | Refs |
| icatibant | Hereditary Angioedema | bkrb1_human | secondary | A (Rhodopsin) | Bradykinin receptors | approved | 4 | - | 2008 | small molecule | antagonist | yes | Refs |
| meperidine | Analgesics | oprm_human | secondary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1942 | small molecule | agonist | yes | Refs |
| metaraminol | Cardiovascular Disease | ada1b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1954 | small molecule | agonist | no | Refs |
| metaraminol | Cardiovascular Disease | ada1d_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1954 | small molecule | agonist | no | Refs |
| iloperidone | Antipsychotic ; Atypical | 5ht1a_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | no | Refs |
| iloperidone | Antipsychotic ; Atypical | 5ht6r_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | no | Refs |
| iloperidone | Antipsychotic ; Atypical | 5ht7r_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | no | Refs |
| iloperidone | Antipsychotic ; Atypical | drd1_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | no | Refs |
| iloperidone | Antipsychotic ; Atypical | hrh1_human | secondary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | no | Refs |
| iloperidone | Antipsychotic ; Atypical | ada1a_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2009 | small molecule | antagonist | no | Refs |
| iloperidone | Antipsychotic ; Atypical | ada2c_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2009 | small molecule | antagonist | no | Refs |
| iloperidone | Antipsychotic ; Atypical | drd3_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 2009 | small molecule | antagonist | no | Refs |
| isoetharine | Obstructive Lung Disease | adrb2_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1979 | small molecule | agonist | no | Refs |
| isoproterenol | Cardiovascular ; Anti-Asthmatic | adrb3_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1956 | small molecule | agonist | no | Refs |
| isoproterenol | Anti-Asthmatic | adrb3_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1956 | small molecule | agonist | no | Refs |
| methyldopa | Antihypertensive | ada2b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1962 | small molecule | agonist | yes | Refs |
| methyldopa | Antihypertensive | ada2c_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1962 | small molecule | agonist | yes | Refs |
| levomepromazine | Schizophrenia | ada1a_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1982 | small molecule | antagonist | yes | Refs |
| levomepromazine | Schizophrenia | ada1b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1982 | small molecule | antagonist | yes | Refs |
| levomepromazine | Schizophrenia | ada1d_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1982 | small molecule | antagonist | yes | Refs |
| methylergonovine | Hemorrhage | 5ht2b_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1946 | small molecule | partial agonist | no | Refs |
| metoclopramide | Pregnancy | 5ht4r_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1979 | small molecule | antagonist | yes | Refs |
| olanzapine | Anti-Depressant | ada1b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| levomepromazine | Schizophrenia | acm1_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | yes | Refs |
| levomepromazine | Schizophrenia | acm2_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | yes | Refs |
| levomepromazine | Schizophrenia | acm3_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | yes | Refs |
| levomepromazine | Schizophrenia | acm4_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | yes | Refs |
| levomepromazine | Schizophrenia | acm5_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | yes | Refs |
| levomepromazine | Schizophrenia | hrh1_human | secondary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1982 | small molecule | antagonist | yes | Refs |
| loxapine | Psychosis | drd3_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1975 | small molecule | antagonist | yes | Refs |
| loxapine | Psychosis | drd4_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1975 | small molecule | antagonist | yes | Refs |
| loxapine | Psychosis | 5ht2c_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1975 | small molecule | antagonist | yes | Refs |
| minaprine | Anti-Depressant | drd1_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | withdrawn | 1984 | small molecule | antagonist | no | Refs |
| minaprine | Anti-Depressant | drd2_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | withdrawn | 1984 | small molecule | antagonist | no | Refs |
| mirtazapine | Unipolar Depression | ada2b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| mirtazapine | Unipolar Depression | ada2c_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| lurasidone | Schizophrenia | 5ht1a_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2010 | small molecule | antagonist | yes | Refs |
| lurasidone | Schizophrenia | 5ht7r_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2010 | small molecule | antagonist | yes | Refs |
| lurasidone | Schizophrenia | ada2c_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 2010 | small molecule | antagonist | yes | Refs |
| mepenzolate | Antispasmodics | hcar2_human | secondary | A (Rhodopsin) | Hydroxycarboxylic acid receptors | approved | 4 | - | 1956 | small molecule | antagonist | yes | Refs |
| molindone | Schizophrenia | 5ht2a_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1974 | small molecule | antagonist | no | Refs |
| naphazoline | Eye Allergy | ada1d_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1971 | small molecule | agonist | yes | Refs |
| oxymetazoline | Dry Eye | ada2c_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1986 | small molecule | agonist | yes | Refs |
| naphazoline | Nasal Obstruction | ada1b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1971 | small molecule | agonist | yes | Refs |
| naphazoline | Nasal Obstruction | ada2b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1971 | small molecule | agonist | yes | Refs |
| naphazoline | Nasal Obstruction | ada2c_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1971 | small molecule | agonist | yes | Refs |
| olanzapine | Schizophrenia | ada1b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| oxymetazoline | Dry Eye | ada2b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1986 | small molecule | agonist | yes | Refs |
| oxymetazoline | Allergic Conjunctivitis | ada1d_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1986 | small molecule | agonist | yes | Refs |
| oxymetazoline | Antiglaucomic | ada1b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1986 | small molecule | agonist | yes | Refs |
| olanzapine | Anti-Depressant | 5ht1a_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Anti-Depressant | 5ht1b_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Anti-Depressant | 5ht1d_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Anti-Depressant | 5ht1e_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Anti-Depressant | 5ht6r_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Anti-Depressant | 5ht7r_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Anti-Depressant | ada2a_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Anti-Depressant | ada2b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Anti-Depressant | ada2c_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| oxymorphone | Analgesics | oprd_human | secondary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1959 | small molecule | agonist | no | Refs |
| oxyphenonium | Digestive System Disease | acm3_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1982 | small molecule | antagonist | no | Refs |
| olanzapine | Anti-Depressant | acm2_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Anti-Depressant | acm3_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Anti-Depressant | acm4_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Anti-Depressant | acm5_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Anti-Depressant | drd5_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Schizophrenia | 5ht1a_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Schizophrenia | 5ht1b_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Schizophrenia | 5ht1d_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Schizophrenia | 5ht1e_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Schizophrenia | 5ht6r_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Schizophrenia | 5ht7r_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Schizophrenia | ada2a_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Schizophrenia | ada2b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Schizophrenia | ada2c_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| pentoxifylline | Amyotrophic Lateral Sclerosis (Als) | aa2ar_human | secondary | A (Rhodopsin) | Adenosine receptors | approved | 4 | - | 1984 | small molecule | antagonist | yes | Refs |
| olanzapine | Schizophrenia | acm2_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Schizophrenia | acm3_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Schizophrenia | acm4_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Schizophrenia | acm5_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| olanzapine | Schizophrenia | drd5_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1996 | small molecule | antagonist | yes | Refs |
| pentoxifylline | Irritable Bowel Syndrome | aa2br_human | secondary | A (Rhodopsin) | Adenosine receptors | approved | 4 | - | 1984 | small molecule | antagonist | yes | Refs |
| pergolide | Antiparkinson | drd3_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1988 | small molecule | agonist | yes | Refs |
| pergolide | Antiparkinson | drd4_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1988 | small molecule | agonist | yes | Refs |
| pergolide | Antiparkinson | drd5_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1988 | small molecule | agonist | yes | Refs |
| pergolide | Antiparkinson | drd1_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1988 | small molecule | agonist | yes | Refs |
| phenoxybenzamine | Cardiovascular Disease | ada2b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1953 | small molecule | antagonist | yes | Refs |
| phenoxybenzamine | Adrenal Gland Pheochromocytoma | ada1b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1953 | small molecule | antagonist | yes | Refs |
| phenoxybenzamine | Adrenal Gland Pheochromocytoma | ada1d_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1953 | small molecule | antagonist | yes | Refs |
| phenoxybenzamine | Adrenal Gland Pheochromocytoma | ada2c_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1953 | small molecule | antagonist | yes | Refs |
| phentolamine | Cardiovascular Disease | ada1b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1952 | small molecule | antagonist | yes | Refs |
| phentolamine | Cardiovascular Disease | ada1d_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1952 | small molecule | antagonist | yes | Refs |
| phentolamine | Cardiovascular Disease | ada2b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1952 | small molecule | antagonist | yes | Refs |
| phentolamine | Cardiovascular Disease | ada2c_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1952 | small molecule | antagonist | yes | Refs |
| pimozide | Psychosis | drd1_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1984 | small molecule | antagonist | yes | Refs |
| pimozide | Psychosis | drd5_human | secondary | A (Rhodopsin) | Dopamine receptors | approved | 4 | - | 1984 | small molecule | antagonist | yes | Refs |
| thioridazine | Psychosis | 5ht2c_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1962 | small molecule | antagonist | yes | Refs |
| tolazoline | Cardiovascular Disease | hrh1_human | secondary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1948 | small molecule | agonist | no | Refs |
| promethazine | Hypnotics And Sedatives; Anti-Anxiety S; Anti-Allergic | acm1_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1951 | small molecule | antagonist | yes | Refs |
| promethazine | Hypnotics And Sedatives; Anti-Anxiety S; Anti-Allergic | acm2_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1951 | small molecule | antagonist | yes | Refs |
| promethazine | Hypnotics And Sedatives; Anti-Anxiety S; Anti-Allergic | acm3_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1951 | small molecule | antagonist | yes | Refs |
| promethazine | Hypnotics And Sedatives; Anti-Anxiety S; Anti-Allergic | acm4_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1951 | small molecule | antagonist | yes | Refs |
| promethazine | Hypnotics And Sedatives; Anti-Anxiety S; Anti-Allergic | acm5_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1951 | small molecule | antagonist | yes | Refs |
| propafenone | Cardiac Arrhythmia | adrb1_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1989 | small molecule | antagonist | yes | Refs |
| propafenone | Atrial Fibrillation | adrb2_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1989 | small molecule | antagonist | yes | Refs |
| propantheline | Digestive System Disease | acm2_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1953 | small molecule | antagonist | yes | Refs |
| propantheline | Digestive System Disease | acm3_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1953 | small molecule | antagonist | yes | Refs |
| tolazoline | Arthralgia | ada2b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1948 | small molecule | agonist | no | Refs |
| tolazoline | Arthralgia | ada2c_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1948 | small molecule | agonist | no | Refs |
| propiomazine | Hypnotics And Sedatives | ada1a_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1960 | small molecule | antagonist | no | Refs |
| propiomazine | Hypnotics And Sedatives | ada1b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1960 | small molecule | antagonist | no | Refs |
| propiomazine | Hypnotics And Sedatives | ada1d_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1960 | small molecule | antagonist | no | Refs |
| propranolol | Antihypertensive | adrb2_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1967 | small molecule | antagonist | yes | Refs |
| quetiapine | Antipsychotic ; Anti-Depressant | 5ht2c_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1997 | small molecule | antagonist | yes | Refs |
| risperidone | Schizophrenia | 5ht2c_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1993 | small molecule | antagonist | yes | Refs |
| solifenacin | Incontinence | acm4_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2004 | small molecule | antagonist | yes | Refs |
| solifenacin | Incontinence | acm5_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2004 | small molecule | antagonist | yes | Refs |
| solifenacin | Incontinence | acm1_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2004 | small molecule | antagonist | yes | Refs |
| solifenacin | Incontinence | acm2_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2004 | small molecule | antagonist | yes | Refs |
| sufentanil | Analgesics; Adjuvant To Anesthesia | oprd_human | secondary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1984 | small molecule | agonist | no | Refs |
| sufentanil | Analgesics; Adjuvant To Anesthesia | oprk_human | secondary | A (Rhodopsin) | Opioid receptors | approved | 4 | - | 1984 | small molecule | agonist | no | Refs |
| tolazoline | Cardiovascular Disease | ada2a_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1948 | small molecule | agonist | no | Refs |
| tetrahydrozoline | Eye Allergy | ada2a_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1979 | small molecule | agonist | no | Refs |
| tolazoline | Arthralgia | hrh2_human | secondary | A (Rhodopsin) | Histamine receptors | approved | 4 | - | 1948 | small molecule | agonist | no | Refs |
| tetrahydrozoline | Nasal Obstruction | ada1b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1979 | small molecule | agonist | no | Refs |
| tetrahydrozoline | Nasal Obstruction | ada1d_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1979 | small molecule | agonist | no | Refs |
| tetrahydrozoline | Nasal Obstruction | ada2b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1979 | small molecule | agonist | no | Refs |
| tetrahydrozoline | Nasal Obstruction | ada2c_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1979 | small molecule | agonist | no | Refs |
| theophylline | Anti-Asthmatic | aa3r_human | secondary | A (Rhodopsin) | Adenosine receptors | approved | 4 | - | 1976 | small molecule | antagonist | yes | Refs |
| thioproperazine | Antipsychotic | ada1b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1962 | small molecule | antagonist | no | Refs |
| abediterol | Anti-Asthmatic | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| tolazoline | Cardiovascular Disease | ada1b_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1948 | small molecule | agonist | no | Refs |
| tolazoline | Cardiovascular Disease | ada1d_human | secondary | A (Rhodopsin) | Adrenoceptors | approved | 4 | - | 1948 | small molecule | agonist | no | Refs |
| tolterodine | Incontinence | acm4_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1998 | small molecule | antagonist | yes | Refs |
| tolterodine | Incontinence | acm5_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1998 | small molecule | antagonist | yes | Refs |
| ac-100 | Dental Ossificant | pe2r1_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 1 | discontinued | - | peptide | not available | no | |
| trifluoperazine | Psychosis | 5ht2a_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1959 | small molecule | antagonist | yes | Refs |
| trifluoperazine | Psychosis | 5ht2c_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 1959 | small molecule | antagonist | yes | Refs |
| tropicamide | Myopia | acm3_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 1960 | small molecule | antagonist | yes | Refs |
| trospium | Incontinence | acm2_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2004 | small molecule | antagonist | yes | Refs |
| trospium | Incontinence | acm3_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2004 | small molecule | antagonist | yes | Refs |
| ACT-774312 | Anti-Allergic | pd2r2_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 1 | ongoing | - | small molecule | antagonist | no | |
| trospium | Incontinence | acm4_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2004 | small molecule | antagonist | yes | Refs |
| trospium | Incontinence | acm5_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | approved | 4 | - | 2004 | small molecule | antagonist | yes | Refs |
| ziprasidone | Schizophrenia | 5ht2c_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | approved | 4 | - | 2001 | small molecule | antagonist | yes | Refs |
| acp-104 | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | discontinued | - | small molecule | partial agonist | no | |
| acp-104 | Schizophrenia | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | discontinued | - | small molecule | partial agonist | no | |
| ac-100 | Periodontal Ossificant | pe2r2_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 1 | discontinued | - | peptide | not available | no | |
| ac-100 | Periodontal Ossificant | pe2r3_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 1 | discontinued | - | peptide | not available | no | |
| ac-100 | Periodontal Ossificant | pe2r4_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 1 | discontinued | - | peptide | not available | no | |
| acp-104 | Schizophrenia | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | discontinued | - | small molecule | inverse agonist | no | |
| ACT-246475 | Cardiovascular Diseases; Myocardial Infarction | p2y12_human | primary | A (Rhodopsin) | P2Y receptors | in trial | 1 | completed | - | small molecule | antagonist | no | |
| aclidinium | Chronic Obstructive Pulmonary Disease (Copd) | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | recruiting | - | small molecule | antagonist | yes | |
| aclidinium | Chronic Obstructive Pulmonary Disease (Copd) | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | recruiting | - | small molecule | antagonist | yes | |
| aclidinium | Chronic Obstructive Pulmonary Disease (Copd) | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | recruiting | - | small molecule | antagonist | yes | |
| aclidinium | Chronic Obstructive Pulmonary Disease (Copd) | acm4_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | recruiting | - | small molecule | antagonist | yes | |
| aclidinium | Chronic Obstructive Pulmonary Disease (Copd) | acm5_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | recruiting | - | small molecule | antagonist | yes | |
| acp-104 | Schizophrenia | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| ACT-539313 | Anti-Anxiety | ox1r_human | primary | A (Rhodopsin) | Orexin receptors | in trial | 1 | ongoing | - | small molecule | antagonist | no | |
| ACT-541468 | Insomnia | ox1r_human | primary | A (Rhodopsin) | Orexin receptors | in trial | 2 | ongoing | - | small molecule | antagonist | no | |
| ACT-541468 | Insomnia | ox2r_human | primary | A (Rhodopsin) | Orexin receptors | in trial | 2 | ongoing | - | small molecule | antagonist | no | |
| adl5747 | Osteoarthritis | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| adl5859 | Osteoarthritis | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| adl5945 | Motilitant | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | terminated | - | small molecule | agonist | no | |
| adl7445 | Motilitant | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 1 | terminated | - | small molecule | agonist | no | |
| adx10059 | Anti-Migraine ; Gastroesophageal Reflux Disease | grm5_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 2 | discontinued | - | small molecule | NAM | no | |
| adx415 | Antihypertensive | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | completed | - | small molecule | NAM | no | |
| adx-48621 | Antiparkinson | grm5_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 2 | completed | - | small molecule | NAM | no | |
| adx-71149 | Antipsychotic ; Anti-Depressant; Anxiolytic | grm2_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 2 | completed | - | small molecule | PAM | no | |
| afamelanotide | Dermatological | mshr_human | primary | A (Rhodopsin) | Melanocortin receptors | in trial | 3 | completed | - | small molecule | agonist | no | Refs |
| aiko-150 | Opioid Antagonist | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 1 | completed | - | small molecule | antagonist | no | |
| ajulemic acid | Analgesics;Neuropathic Pain | cnr1_human | primary | A (Rhodopsin) | Cannabinoid receptors | in trial | 2 | not open yet | - | small molecule | agonist | no | |
| ajulemic acid | Analgesics;Neuropathic Pain | cnr2_human | primary | A (Rhodopsin) | Cannabinoid receptors | in trial | 2 | not open yet | - | small molecule | agonist | no | |
| akl-0707 | Hormone Replacement | ghrhr_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| akp-11 | Psoriasis | s1pr1_human | primary | A (Rhodopsin) | Lysophospholipid (S1P) receptors | in trial | 1 | completed | - | small molecule | PAM | no | |
| alb-127158(a) | Anti-Obesity | mshr_human | primary | A (Rhodopsin) | Melanocortin receptors | in trial | 1 | discontinued | - | small molecule | antagonist | no | |
| alx1-11 | Anti-Osteoporotic | pth1r_human | primary | B1 (Secretin) | Parathyroid hormone receptors | in trial | 3 | completed | - | protein | agonist | no | |
| alx1-11 | Anti-Osteoporotic | pth2r_human | primary | B1 (Secretin) | Parathyroid hormone receptors | in trial | 3 | completed | - | protein | agonist | no | |
| alks 33 | Alcohol Dependance; Anti-Depressant | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 1 | discontinued | - | small molecule | antagonist | no | |
| alks 33 | Alcohol Dependance; Anti-Depressant | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 1 | discontinued | - | small molecule | antagonist | no | |
| alks 33 | Alcohol Dependance; Anti-Depressant | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| alks 33 | Alcohol Dependance; Anti-Depressant | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| am1030 | Anti-Inflammatory ; Atopic Dermatitis | 5ht2b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| alks 33 | Alcohol Dependance; Anti-Depressant | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | completed | - | small molecule | antagonist | no | |
| alks 33 | Alcohol Dependance; Anti-Depressant | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | completed | - | small molecule | antagonist | no | |
| alks 33 | Anti-Obesity | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| alks 33 | Anti-Obesity | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| am-152 | Anti-Inflammatory ; Antifibrotic | lpar1_human | primary | A (Rhodopsin) | Lysophospholipid (LPA) receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| alks 37 | Motilitant | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| alks 37 | Motilitant | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| almorexant | Sleep Disorder Treatment | ox1r_human | primary | A (Rhodopsin) | Orexin receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| almorexant | Sleep Disorder Treatment | ox2r_human | primary | A (Rhodopsin) | Orexin receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| alprostadil | Sexual Dysfunction | pe2r2_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| alprostadil | Sexual Dysfunction | pe2r2_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 3 | suspended | - | small molecule | agonist | yes | Refs |
| alprostadil | Sexual Dysfunction | pe2r2_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| alprostadil | Raynaud'S Disease | pe2r2_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| alprostadil | Sexual Dysfunction | pe2r1_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| alprostadil | Sexual Dysfunction | pe2r1_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 3 | suspended | - | small molecule | agonist | yes | Refs |
| alprostadil | Sexual Dysfunction | pe2r1_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| alprostadil | Raynaud'S Disease | pe2r1_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| alx- 0651 | Antineoplastic | cxcr4_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 1 | terminated | - | antibody | antagonist | no | |
| am-211 | Anti-Inflammatory ; Antiallergy | pd2r2_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 1 | unknown | - | small molecule | antagonist | no | |
| am-461 | Anti-Inflammatory | pd2r_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 1 | unknown | - | small molecule | antagonist | no | |
| amisulpride | Antiemetics | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | completed | - | small molecule | antagonist | no | Refs |
| amisulpride | Antiemetics | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | completed | - | small molecule | antagonist | no | Refs |
| am-831 | Antipsychotic ; Schizophrenia | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 1 | discontinued | - | small molecule | antagonist | no | |
| am-831 | Antipsychotic ; Schizophrenia | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 1 | discontinued | - | small molecule | antagonist | no | |
| am-831 | Antipsychotic ; Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 1 | discontinued | - | small molecule | antagonist | no | |
| amphetamine | Cognitive Dysfunction; Adhd | taar1_human | secondary | A (Rhodopsin) | Trace amine receptors | in trial | 2 | completed | - | small molecule | agonist | no | Refs |
| amap102 | Anti-Inflammatory ; Dmard | 5ht2b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| amap102 | Anti-Inflammatory ; Dmard | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| amd-070 | Antiviral ; Hiv | cxcr4_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| amelubant | Chronic Obstructive Pulmonary Disease (Copd) | lt4r1_human | primary | A (Rhodopsin) | Leukotriene receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| amibegron | Anti-Depressant | adrb3_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 3 | discontinued | - | small molecule | agonist | no | |
| amisulpride | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 1 | discontinued | - | small molecule | antagonist | no | Refs |
| amisulpride | Schizophrenia | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 1 | discontinued | - | small molecule | antagonist | no | Refs |
| amphetamine | Cognitive Dysfunction; Adhd | taar1_human | secondary | A (Rhodopsin) | Trace amine receptors | in trial | 2 | completed | - | small molecule | agonist | no | Refs |
| amphetamine | Cognitive Dysfunction; Adhd | taar1_human | secondary | A (Rhodopsin) | Trace amine receptors | in trial | 2 | ongoing | - | small molecule | agonist | no | Refs |
| anamorelin | Appetite Stimulant | ghsr_human | primary | A (Rhodopsin) | Ghrelin receptors | in trial | 3 | completed | - | small molecule | agonist | no | |
| anatibant | Traumatic Brain Injury | bkrb2_human | primary | A (Rhodopsin) | Bradykinin receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | Refs |
| Anti-CXCR2 biparatopic nanobody‰ | Anti-Inflammatory | cxcr2_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 1 | ongoing | - | antibody | antagonist | no | |
| apd125 | Insomnia | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| ap1030 | Anti-Obesity | mshr_human | primary | A (Rhodopsin) | Melanocortin receptors | in trial | 1 | completed | - | small molecule | PAM | no | |
| ap1030 | Anti-Obesity | mc4r_human | primary | A (Rhodopsin) | Melanocortin receptors | in trial | 1 | completed | - | small molecule | PAM | no | |
| ap214 | Post-Surgical Kidney Injury | mshr_human | primary | A (Rhodopsin) | Melanocortin receptors | in trial | 2 | discontinued | - | peptide | agonist | no | |
| ap214 | Post-Surgical Kidney Injury | mc3r_human | primary | A (Rhodopsin) | Melanocortin receptors | in trial | 2 | discontinued | - | peptide | agonist | no | |
| ap214 | Post-Surgical Kidney Injury | mc4r_human | primary | A (Rhodopsin) | Melanocortin receptors | in trial | 2 | discontinued | - | peptide | agonist | no | |
| ap214 | Post-Surgical Kidney Injury | mc5r_human | primary | A (Rhodopsin) | Melanocortin receptors | in trial | 2 | discontinued | - | peptide | agonist | no | |
| apadenoson | Atrial Fibrillation | aa2ar_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | Refs |
| apd125 | Dementia With Lewy Bodies | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | recruiting | - | small molecule | agonist | no | |
| apd334 | For Autoimmune Disorders | s1pr1_human | primary | A (Rhodopsin) | Lysophospholipid (S1P) receptors | in trial | 2 | recruiting | - | small molecule | agonist | no | |
| apd597 | Antidiabetic | gp119_human | primary | A (Rhodopsin) | GPR18, GPR55 and GPR119 | in trial | 1 | discontinued | - | small molecule | agonist | no | |
| apd668 | Antidiabetic | gp119_human | primary | A (Rhodopsin) | GPR18, GPR55 and GPR119 | in trial | 1 | discontinued | - | small molecule | agonist | no | |
| apd791 | Antithrombotic | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 1 | completed | - | small molecule | agonist | no | |
| apd811 | Antihypertensive | pi2r_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 2 | ongoing | - | small molecule | agonist | no | |
| apd916 | Sleep Disorders; Narcolepsy | hrh3_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 1 | completed | - | small molecule | agonist | no | |
| apelin | Cardiovascular Disorders; Insulin Sensitivity | apj_human | primary | A (Rhodopsin) | Apelin receptors | in trial | 1 | completed | - | peptide | not available | no | |
| api246 | Treatment Of Affective And Anger Disorders | v1ar_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| aplindore | Antiparkinson ; Restlegs Legs Syndrome | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | discontinued | - | small molecule | partial agonist | no | |
| apomorphine | Erectile Dysfunction | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 1 | discontinued | - | small molecule | agonist | yes | Refs |
| apomorphine | Sexual Dysfunction In Women; Erectile Dysfunction; Antiparkinson | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| apomorphine | Sexual Dysfunction In Women; Erectile Dysfunction; Antiparkinson | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| apomorphine | Antiparkinson | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 1 | completed | - | small molecule | agonist | yes | Refs |
| apomorphine | Erectile Dysfunction | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 1 | discontinued | - | small molecule | agonist | yes | Refs |
| apomorphine | Sexual Dysfunction In Women; Erectile Dysfunction; Antiparkinson | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| apomorphine | Sexual Dysfunction In Women; Erectile Dysfunction; Antiparkinson | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| apomorphine | Antiparkinson | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 1 | completed | - | small molecule | agonist | yes | Refs |
| apomorphine | Erectile Dysfunction | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 1 | discontinued | - | small molecule | agonist | yes | Refs |
| apomorphine | Sexual Dysfunction In Women; Erectile Dysfunction; Antiparkinson | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| apomorphine | Sexual Dysfunction In Women; Erectile Dysfunction; Antiparkinson | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| apomorphine | Antiparkinson | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 1 | completed | - | small molecule | agonist | yes | Refs |
| aprocitentan | Hypertension | ednra_human | primary | A (Rhodopsin) | Endothelin receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| aprocitentan | Hypertension | ednrb_human | primary | A (Rhodopsin) | Endothelin receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| arbaclofen | Fragile X Syndrome | gabr2_human | primary | C (Glutamate) | GABAB receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | Refs |
| arbaclofen | Gastrointestinal Reflux Disease | gabr2_human | primary | C (Glutamate) | GABAB receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | Refs |
| arbaclofen | Fragile X Syndrome | gabr1_human | primary | C (Glutamate) | GABAB receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | Refs |
| arbaclofen | Gastrointestinal Reflux Disease | gabr1_human | primary | C (Glutamate) | GABAB receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | Refs |
| ari-3037mo | Vitamin B Analog; For Treatment For Hyperlipidemia | hcar2_human | primary | A (Rhodopsin) | Hydroxycarboxylic acid receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| ari-3037mo | Vitamin B Analog; For Treatment For Hyperlipidemia | hcar3_human | primary | A (Rhodopsin) | Hydroxycarboxylic acid receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| arry-502 | Anti-Allergic | pd2r2_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| asimadoline | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | |
| asm-024 | Anti-Asthmatic ; Copd | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| athx-105 | Anti-Obesity | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| ati-7505 | Parasympathomimetic | 5ht4r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| atrasentan | Antineoplastic | ednra_human | primary | A (Rhodopsin) | Endothelin receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| ati-9242 | Schizophrenia | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 1 | ongoing | - | small molecule | not available | no | |
| ati-9242 | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 1 | ongoing | - | small molecule | not available | no | |
| atopaxar | Acute Coronary Syndrome | par1_human | primary | A (Rhodopsin) | Proteinase-activated receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| atrasentan | Diabetic Nephropathy | ednra_human | primary | A (Rhodopsin) | Endothelin receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| ATX2417 | Anti-Asthmatic | pd2r2_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 1 | completed | - | small molecule | antagonist | no | |
| av608 | Anti-Depressant; Irritable Bowel Syndrome; Antispasmodic | nk1r_human | primary | A (Rhodopsin) | Tachykinin receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| ave-1625 | Anti-Obesity ; Alzheimer'S Disease | cnr1_human | primary | A (Rhodopsin) | Cannabinoid receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| avicine | Antineoplastic | lshr_human | primary | A (Rhodopsin) | Glycoprotein hormone receptors | in trial | 1 | discontinued | - | vaccine | not available | no | |
| avn-101 | Alzheimer'S Disease | 5ht6r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 1 | completed | - | small molecule | antagonist | no | |
| avn-211 | Schizophrenia | 5ht6r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | unknown | - | small molecule | antagonist | no | |
| avn-322 | Alzheimer'S Disease | 5ht6r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 1 | discontinued | - | small molecule | antagonist | no | |
| avn-397 | Alzheimer'S Disease | 5ht6r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | discontinued | - | small molecule | unknown | no | |
| avosentan | Diabetic Nephropathy | ednra_human | primary | A (Rhodopsin) | Endothelin receptors | in trial | 3 | terminated | - | small molecule | antagonist | no | |
| azd1981 | Anti-Asthmatic | pd2r2_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| azd2066 | Analgesics; Gastroesophageal Reflux Disease | grm5_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| azd2423 | Chronic Obstructive Pulmonary Disorder;Analgesics; Neuropathic Pain | ccr2_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| azd2820 | Anti-Obesity | mc4r_human | primary | A (Rhodopsin) | Melanocortin receptors | in trial | 1 | discontinued | - | small molecule | agonist | no | |
| azd3199 | Chronic Obstructive Pulmonary Disease (Copd) | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| betahistine | Dizzy/Fainting Spells | hrh3_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 1 | ongoing | - | small molecule | antagonist | yes | Refs |
| bevantolol | Antihypertensive | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | Refs |
| AZD8871 | Anti-Asthmatic | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 1 | completed | - | small molecule | agonist | no | |
| AZD8871 | Anti-Asthmatic | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 1 | completed | - | small molecule | agonist | no | |
| AZD8871 | Anti-Asthmatic | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 1 | completed | - | small molecule | agonist | no | |
| AZD8871 | Anti-Asthmatic | acm4_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 1 | completed | - | small molecule | agonist | no | |
| AZD8871 | Anti-Asthmatic | acm5_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 1 | completed | - | small molecule | agonist | no | |
| AZD8871 | Anti-Asthmatic | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 1 | completed | - | small molecule | agonist | no | |
| azelastine | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 2 | completed | - | small molecule | antagonist | yes | Refs |
| azp-531 | Antidiabetic | ghsr_human | primary | A (Rhodopsin) | Ghrelin receptors | in trial | 1 | ongoing | - | peptide | agonist | no | |
| baclofen | Alcohol Dependance | gabr2_human | primary | C (Glutamate) | GABAB receptors | in trial | 1 | discontinued | - | small molecule | agonist | yes | Refs |
| baclofen | For Type 1A Charcot-Marie-Tooth Disease | gabr2_human | primary | C (Glutamate) | GABAB receptors | in trial | 3 | recruiting | - | small molecule | agonist | yes | Refs |
| baclofen | Alcohol Dependance | gabr1_human | primary | C (Glutamate) | GABAB receptors | in trial | 1 | discontinued | - | small molecule | agonist | yes | Refs |
| baclofen | For Type 1A Charcot-Marie-Tooth Disease | gabr1_human | primary | C (Glutamate) | GABAB receptors | in trial | 3 | recruiting | - | small molecule | agonist | yes | Refs |
| barusiban | Fertility | oxyr_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | in trial | 2 | completed | - | protein | antagonist | no | |
| basimglurant | Fragile X Syndrome | grm5_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 2 | completed | - | small molecule | NAM | no | |
| bf-1 | Anti-Migraine | 5ht2b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 1 | ongoing | - | small molecule | antagonist | no | |
| batefenterol | Chronic Obstructive Pulmonary Disease (Copd) | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 2 | completed | - | small molecule | agonist | no | |
| batefenterol | Chronic Obstructive Pulmonary Disease (Copd) | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 2 | completed | - | small molecule | agonist | no | |
| batefenterol | Chronic Obstructive Pulmonary Disease (Copd) | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| bavisant | Attention Deficit Hyperactivity Disorder | hrh3_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 2 | withdrawn | - | small molecule | antagonist | no | |
| bci-838 | Anti-Depressant | grm2_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 1 | completed | - | small molecule | antagonist | no | |
| bci-838 | Anti-Depressant | grm3_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 1 | completed | - | small molecule | antagonist | no | |
| bedoradrine | Anti-Asthmatic | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| beraprost | Antihypertensive | pi2r_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 3 | withdrawn | - | small molecule | agonist | no | Refs |
| betahistine | Anti-Obesity | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| betahistine | Dizzy/Fainting Spells | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 1 | ongoing | - | small molecule | agonist | yes | Refs |
| betahistine | Anti-Obesity | hrh3_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | yes | Refs |
| bg-9928 | Congestive Heart Failure | aa1r_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 2 | terminated | - | small molecule | antagonist | no | |
| bgc20-1531 | Anti-Migraine | pe2r4_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| BI 665088‰ | Kidney Disease | cx3c1_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 1 | ongoing | - | antibody | antagonist | no | |
| bifeprunox | Antipsychotic ; Antiparkinson | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | discontinued | - | small molecule | partial agonist | no | Refs |
| bifeprunox | Antipsychotic ; Antiparkinson | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | discontinued | - | small molecule | partial agonist | no | Refs |
| bifeprunox | Antipsychotic ; Antiparkinson | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| bl-1020 | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | terminated | - | small molecule | antagonist | no | |
| bifeprunox | Antipsychotic ; Antiparkinson | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | |
| bifeprunox | Antipsychotic ; Antiparkinson | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | |
| bifeprunox | Antipsychotic ; Antiparkinson | 5ht7r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | |
| biib014 | Antiparkinson | aa2ar_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| bim23a760 | Antineoplastic ; Treatment For Acromegaly | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| bim23a760 | Antineoplastic ; Treatment For Acromegaly | ssr2_human | primary | A (Rhodopsin) | Somatostatin receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| bim23a760 | Antineoplastic ; Treatment For Acromegaly | ssr5_human | primary | A (Rhodopsin) | Somatostatin receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| bimatoprost | Antiglaucomic | pf2r_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| bimatoprost | Antiglaucomic | pe2r1_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| bimatoprost | Antiglaucomic | pe2r3_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| binodenoson | Diagnostic | aa2ar_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 3 | completed | - | small molecule | agonist | no | Refs |
| bl-1020 | Schizophrenia | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | terminated | - | small molecule | agonist | no | |
| bl-1020 | Schizophrenia | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 3 | terminated | - | small molecule | agonist | no | |
| bl-8040 | Antineoplastic | cxcr4_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 2 | recruiting | - | peptide | antagonist | no | |
| BNC-101‰ | Antineoplastic | lgr5_human | primary | A (Rhodopsin) | Class A orphans | in trial | 1 | ongoing | - | antibody | antagonist | no | |
| boxaban | Treatment Of Asystemic Scleroderma; Hepatorenal Syndrome; Asthma | ta2r_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 2 | not open yet | - | small molecule | antagonist | no | |
| bremelanotide | Sexual Dysfunction | mc3r_human | primary | A (Rhodopsin) | Melanocortin receptors | in trial | 3 | ongoing | - | protein | agonist | no | |
| bremelanotide | Sexual Dysfunction | mshr_human | primary | A (Rhodopsin) | Melanocortin receptors | in trial | 3 | ongoing | - | peptide | agonist | no | |
| bremelanotide | Sexual Dysfunction | mc4r_human | primary | A (Rhodopsin) | Melanocortin receptors | in trial | 3 | ongoing | - | peptide | agonist | no | |
| brimonidine | Erythema | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| brimonidine | Erythema | ada2c_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| brimonidine | Erythema | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| BTX-1503 | Skin Disorder Therapies | cnr1_human | primary | A (Rhodopsin) | Cannabinoid receptors | in trial | 1 | ongoing | - | small molecule | antagonist | no | |
| BTX-1503 | Skin Disorder Therapies | cnr2_human | primary | A (Rhodopsin) | Cannabinoid receptors | in trial | 1 | ongoing | - | small molecule | antagonist | no | |
| bucindolol | Heart Failure | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| bucindolol | Heart Failure | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| budiodarone | Anti-Arrhythmia | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| buprenorphine | Anti-Depressant; Analgesics; Opioid Addiction | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 1 | completed | - | small molecule | agonist | yes | Refs |
| buprenorphine | Anti-Depressant; Analgesics; Opioid Addiction | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | recruiting | - | small molecule | agonist | yes | Refs |
| buprenorphine | Anti-Depressant; Analgesics; Opioid Addiction | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| buprenorphine | Anti-Depressant; Analgesics; Opioid Addiction | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | completed | - | small molecule | agonist | yes | Refs |
| buprenorphine | Anti-Depressant; Analgesics; Opioid Addiction | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 1 | completed | - | small molecule | agonist | yes | Refs |
| buprenorphine | Anti-Depressant; Analgesics; Opioid Addiction | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | recruiting | - | small molecule | agonist | yes | Refs |
| buprenorphine | Anti-Depressant; Analgesics; Opioid Addiction | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| buprenorphine | Anti-Depressant; Analgesics; Opioid Addiction | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | completed | - | small molecule | agonist | yes | Refs |
| buprenorphine | Anti-Depressant; Analgesics; Opioid Addiction | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| bupropion/trazodone | Anti-Depressant; For Hypoactive Sexual Desire Disorder And Female Sexual Dysfunction | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | completed | - | small molecule | partial agonist | no | |
| bupropion/trazodone | Anti-Depressant; For Hypoactive Sexual Desire Disorder And Female Sexual Dysfunction | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| bupropion/trazodone | Anti-Depressant; For Hypoactive Sexual Desire Disorder And Female Sexual Dysfunction | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| bvt.115959 | Analgesics | aa2ar_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| bvt.28949 | Antiglaucomic | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | unknown | - | small molecule | antagonist | no | |
| cal-1 | Antiviral ; Hiv | ccr5_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 2 | ongoing | - | cell therapy | not available | no | |
| calcitonin human | Anti-Osteoporotic | calcr_human | primary | B1 (Secretin) | Calcitonin receptors | in trial | 2 | completed | - | peptide | agonist | no | |
| calcitonin human | Anti-Osteoporotic | calcr_human | primary | B1 (Secretin) | Calcitonin receptors | in trial | 1 | completed | - | peptide | agonist | no | |
| calcitonin salmon recombinant | Anti-Osteoporotic | calcr_human | primary | B1 (Secretin) | Calcitonin receptors | in trial | 3 | discontinued | - | peptide | agonist | no | Refs |
| camicinal | Gastroparesis | mtlr_human | primary | A (Rhodopsin) | Motilin receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| cannabidiol | Schizophrenia | gpr55_human | primary | A (Rhodopsin) | GPR18, GPR55 and GPR119 | in trial | 2 | completed | - | small molecule | agonist | no | |
| cannabidiol | Epilepsy | cnr1_human | primary | A (Rhodopsin) | Cannabinoid receptors | in trial | 2 | ongoing | - | small molecule | antagonist | no | |
| cannabidiol | Epilepsy | cnr2_human | primary | A (Rhodopsin) | Cannabinoid receptors | in trial | 2 | ongoing | - | small molecule | antagonist | no | |
| cannabidiol | Epilepsy | gpr55_human | primary | A (Rhodopsin) | GPR18, GPR55 and GPR119 | in trial | 2 | ongoing | - | small molecule | agonist | no | |
| cannabidiol | Graft Versus Host Disease | gpr55_human | primary | A (Rhodopsin) | GPR18, GPR55 and GPR119 | in trial | 2 | completed | - | small molecule | agonist | no | |
| cannabidiol | Epilepsy | gpr55_human | primary | A (Rhodopsin) | GPR18, GPR55 and GPR119 | in trial | 3 | not open yet | - | small molecule | agonist | no | |
| cannabidiol | Epilepsy | gpr55_human | primary | A (Rhodopsin) | GPR18, GPR55 and GPR119 | in trial | 3 | recruiting | - | small molecule | agonist | no | |
| cannabidivarin | Epilepsy | gpr55_human | primary | A (Rhodopsin) | GPR18, GPR55 and GPR119 | in trial | 2 | recruiting | - | small molecule | agonist | no | |
| carbetocin | Labor Inducing | oxyr_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | in trial | 3 | completed | - | small molecule | agonist | no | Refs |
| carmoterol | Chronic Obstructive Pulmonary Disease (Copd) | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| casopitant | Antiemetics | nk1r_human | primary | A (Rhodopsin) | Tachykinin receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| ccl2-lpm | Anti-Inflammatory | ccr2_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 1 | terminated | - | protein | antagonist | no | |
| ccx025 | Anti-Inflammatory | ccr9_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 1 | unknown | - | small molecule | antagonist | no | |
| ccx140 | Anti-Inflammatory ; Antidiabetic | ccr2_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| ccx168 | Anti-Inflammatory | c5ar1_human | primary | A (Rhodopsin) | Complement peptide receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| ccx282 | Anti-Inflammatory ; Crohn'S Disease; Ulceraite Colitis | ccr9_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 3 | terminated | - | small molecule | antagonist | no | |
| ccx354 | Anti-Inflammatory ; Dmard | ccr1_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| ccx507 | Ulcerative Colitis; Inflammatory Bowel Disease | ccr9_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 1 | completed | - | small molecule | antagonist | no | |
| ccx832 | Anti-Inflammatory ; For Treatment For Autoimmune Disease | cml1_human | primary | A (Rhodopsin) | Chemerin receptor | in trial | 1 | discontinued | - | small molecule | antagonist | no | |
| ccx872 | Antineoplastic ; Pancreatic Cancer | ccr2_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 1 | ongoing | - | small molecule | antagonist | no | |
| cebranopadol | Diabetic Neuropathy | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | recruiting | - | small molecule | agonist | no | |
| cebranopadol | Diabetic Neuropathy | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | recruiting | - | small molecule | agonist | no | |
| cebranopadol | Osteoarthritis, Knee | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | recruiting | - | small molecule | agonist | no | |
| cebranopadol | Analgesics | oprx_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | recruiting | - | small molecule | agonist | no | |
| cenerimod | Systemic Lupus Erythematosus | s1pr1_human | primary | A (Rhodopsin) | Lysophospholipid (S1P) receptors | in trial | 2 | ongoing | - | small molecule | agonist | no | |
| cenicriviroc | Antiviral ; Hiv | ccr2_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| cenicriviroc | Antiviral ; Hiv | ccr5_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| cer627 | Dyslipidemia With Low Hdl | hcar2_human | primary | A (Rhodopsin) | Hydroxycarboxylic acid receptors | in trial | 1 | discontinued | - | small molecule: combination | agonist | no | |
| cer627 | Dyslipidemia With Low Hdl | hcar3_human | primary | A (Rhodopsin) | Hydroxycarboxylic acid receptors | in trial | 1 | discontinued | - | small molecule: combination | agonist | no | |
| cerc-501 | Substance Use Disorders | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| cerlapirdine | Alzheimer'S Disease | 5ht6r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| cf101 | Keratoconjunctivitis Sicca | aa3r_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 3 | not open yet | - | small molecule | agonist | no | |
| cf-101 | Anti-Inflammatory ; Dmard | aa3r_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 3 | not open yet | - | small molecule | agonist | no | |
| cf-102 | Antineoplastic | aa3r_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 2 | recruiting | - | small molecule | agonist | no | |
| cf602 | Sexual Dysfunction | aa3r_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 1 | not open yet | - | small molecule | agonist | no | |
| cgrp | Anti-Asthmatic | calrl_human | primary | B1 (Secretin) | Calcitonin receptors | in trial | 2 | discontinued | - | peptide | agonist | no | |
| chorionic gonadotropin | Antineoplastic | lshr_human | primary | A (Rhodopsin) | Glycoprotein hormone receptors | in trial | 3 | not open yet | - | protein | agonist | no | Refs |
| cinalukast | Anti-Asthmatic | cltr1_human | primary | A (Rhodopsin) | Leukotriene receptors | in trial | 1 | discontinued | - | small molecule | antagonist | no | Refs |
| cis-uca eye drops | For Ocular Surface Inflammation | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| clazosentan | Vasospasm | ednra_human | primary | A (Rhodopsin) | Endothelin receptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| clonidine | Diabetic Neuropathy; Adhd; Antimucositic | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 3 | discontinued | - | small molecule | agonist | yes | Refs |
| clonidine | Diabetic Neuropathy; Adhd; Antimucositic | ada2c_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 3 | discontinued | - | small molecule | agonist | yes | Refs |
| cr845 | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | recruiting | - | small molecule | agonist | no | |
| clonidine | Diabetic Neuropathy; Adhd; Antimucositic | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| clonidine | Diabetic Neuropathy; Adhd; Antimucositic | ada2c_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| clonidine | Diabetic Neuropathy; Adhd; Antimucositic | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 3 | discontinued | - | small molecule | agonist | yes | Refs |
| clonidine | Diabetic Neuropathy; Adhd; Antimucositic | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| CNTX-0290 | Analgesics | ssr4_human | primary | A (Rhodopsin) | Somatostatin receptors | in trial | 1 | completed | - | small molecule | agonist | no | |
| CNTX-6970 | Analgesics | ccr2_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 1 | completed | - | small molecule | antagonist | no | |
| corifollitropin alfa | Fertility | fshr_human | primary | A (Rhodopsin) | Glycoprotein hormone receptors | in trial | 3 | recruiting | - | protein | agonist | no | |
| corticotropin-releasing factor | Peritumoral Brain Edema | crfr1_human | primary | B1 (Secretin) | Corticotropin-releasing factor receptors | in trial | 3 | discontinued | - | peptide | agonist | no | |
| cpb-307 | Autoimmune Diseases | s1pr1_human | primary | A (Rhodopsin) | Lysophospholipid (S1P) receptors | in trial | 1 | completed | - | small molecule | agonist | no | |
| cr665 | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| cromolyn sodium | Autoimmune Diseases | gpr35_human | primary | A (Rhodopsin) | Class A orphans | in trial | 2 | completed | - | small molecule | agonist | no | |
| ctce-9908 | Antineoplastic | cxcr4_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 2 | discontinued | - | protein | antagonist | no | |
| ctp-499 | Diabetic Nephropathy | aa1r_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 2 | completed | - | small molecule | not available | no | |
| ctp-499 | Diabetic Nephropathy | aa2ar_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 2 | completed | - | small molecule | not available | no | |
| cur-61414 | Antineoplastic | smo_human | primary | F (Frizzled) | Frizzled | in trial | 1 | completed | - | small molecule | antagonist | no | |
| cvt-3619 | Antihyperlipidemic | aa1r_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 1 | completed | - | small molecule | partial agonist | no | |
| cvt-6883 | Anti-Asthmatic | aa2br_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 1 | completed | - | small molecule | antagonist | no | |
| cyclobenzaprine | Fibromyalgia, Ptsd | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | Refs |
| dac:glp-1 | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 2 | discontinued | - | peptide | agonist | no | |
| dac:grf | Hormone Replacement | ghrhr_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 2 | discontinued | - | peptide | agonist | no | |
| danirixin | Chronic Obstructive Pulmonary Disease (Copd) | cxcr2_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| darusentan | Antihypertensive | ednra_human | primary | A (Rhodopsin) | Endothelin receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | Refs |
| davalintide | Anti-Obesity | calcr_human | primary | B1 (Secretin) | Calcitonin receptors | in trial | 2 | discontinued | - | protein | agonist | no | |
| decoglurant | Unipolar Depression | grm2_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 2 | discontinued | - | small molecule | NAM | no | |
| decoglurant | Unipolar Depression | grm3_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 2 | discontinued | - | small molecule | NAM | no | |
| denufosol | Cystic Fibrosis | p2ry2_human | primary | A (Rhodopsin) | P2Y receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | Refs |
| Denufosol | Rhegmatogenous Retinal Detachment | p2ry2_human | primary | A (Rhodopsin) | P2Y receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | Refs |
| Denufosol | Cystic Fibrosis; Perennial Allergic Rhinitis | p2ry2_human | primary | A (Rhodopsin) | P2Y receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | Refs |
| deuterium containing analog of sodium oxybate | Sleep Disorders; Narcolepsy | gabr1_human | primary | C (Glutamate) | GABAB receptors | in trial | 1 | completed | - | small molecule | agonist | no | |
| deuterium containing analog of sodium oxybate | Sleep Disorders; Narcolepsy | gabr2_human | primary | C (Glutamate) | GABAB receptors | in trial | 1 | completed | - | small molecule | agonist | no | |
| dexloxiglumide | Motilitant | cckar_human | primary | A (Rhodopsin) | Cholecystokinin receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | Refs |
| dg041 | Platelet Aggregation Inhibitor | pe2r3_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| dipraglurant | Antiparkinson | grm5_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 2 | completed | - | small molecule | NAM | no | |
| dg3173 | Hormone Replacement | ssr2_human | primary | A (Rhodopsin) | Somatostatin receptors | in trial | 2 | ongoing | - | small molecule | agonist | no | |
| dg3173 | Hormone Replacement | ssr4_human | primary | A (Rhodopsin) | Somatostatin receptors | in trial | 2 | ongoing | - | small molecule | agonist | no | |
| dg3173 | Hormone Replacement | ssr5_human | primary | A (Rhodopsin) | Somatostatin receptors | in trial | 2 | ongoing | - | small molecule | agonist | no | |
| diquafosol | Opthalmological | p2ry2_human | primary | A (Rhodopsin) | P2Y receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | |
| domperidone | Antiemetics | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | Refs |
| DP1038 | Growth Hormone Deficiency | ssr1_human | primary | A (Rhodopsin) | Somatostatin receptors | in trial | 1 | completed | - | peptide | agonist | no | |
| DP1039 | Growth Hormone Deficiency | ssr2_human | primary | A (Rhodopsin) | Somatostatin receptors | in trial | 1 | completed | - | peptide | agonist | no | |
| DP1040 | Growth Hormone Deficiency | ssr3_human | primary | A (Rhodopsin) | Somatostatin receptors | in trial | 1 | completed | - | peptide | agonist | no | |
| DP1041 | Growth Hormone Deficiency | ssr5_human | primary | A (Rhodopsin) | Somatostatin receptors | in trial | 1 | completed | - | peptide | agonist | no | |
| drinabant | Schizophrenia | cnr1_human | primary | A (Rhodopsin) | Cannabinoid receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| drm04 | Hyperhidrosis | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | completed | - | small molecule | antagonist | no | |
| dsc127 | Diabetic Foot Ulcers | agtr1_human | primary | A (Rhodopsin) | Angiotensin receptors | in trial | 3 | discontinued | - | peptide | agonist | no | |
| ecopipam | Speech And Language Disorders | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| efpeglenatide | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 2 | completed | - | peptide | agonist | no | |
| Elagolix | Endometriosis, Antineoplastic | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| elagolix | Endometriosis | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| elinogrel | Antiplatelet | p2y12_human | primary | A (Rhodopsin) | P2Y receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| eltoprazine | Dyskinesias | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | ongoing | - | small molecule | agonist | no | |
| eltoprazine | Dyskinesias | 5ht1b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | ongoing | - | small molecule | agonist | no | |
| elubrixin | Ulcerative Colitis | cxcr2_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| ema401 | Peripheral Neuropathic Pain; Post Herpetic Neuralgia | agtr2_human | primary | A (Rhodopsin) | Angiotensin receptors | in trial | 2 | not open yet | - | small molecule | antagonist | no | |
| emicerfont | Irritable Bowel Syndrome | crfr1_human | primary | B1 (Secretin) | Corticotropin-releasing factor receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| fenfluramine | Epilepsy; Dravet'S Syndrome | 5ht2b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | recruiting | - | small molecule | agonist | no | Refs |
| ep-100 | Antineoplastic | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | in trial | 2 | completed | - | peptide | not available | no | |
| epelsiban | Premature Ejaculation | oxyr_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | in trial | 2 | withdrawn | - | small molecule | antagonist | no | |
| eplivanserine | Insomnia | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | discontinued | - | small molecule | inverse agonist | no | |
| eplivanserine | Insomnia | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | discontinued | - | small molecule | inverse agonist | no | |
| erenumab | Anti-Migraine | calrl_human | primary | B1 (Secretin) | Calcitonin receptors | in trial | 3 | completed | - | antibody | antagonist | no | |
| esmirtazapine | Insomnia | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | Refs |
| fenfluramine | Epilepsy; Dravet'S Syndrome | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | recruiting | - | small molecule | agonist | no | Refs |
| esmirtazapine | Insomnia; Menopausal Symptoms | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| esmirtazapine | Insomnia; Menopausal Symptoms | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| etilevodopa | Antiparkinson | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | |
| etilevodopa | Antiparkinson | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | |
| etilevodopa | Antiparkinson | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | |
| etilevodopa | Antiparkinson | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | |
| etilevodopa | Antiparkinson | drd5_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | |
| esmirtazapine | Insomnia | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| esmirtazapine | Insomnia | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| esmirtazapine | Insomnia | ada2c_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| exenatide | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 3 | not open yet | - | peptide | agonist | yes | Refs |
| exendin (9-39) | Hypoglycemia | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 2 | recruiting | - | peptide | antagonist | no | |
| fasoracetam monohydrate | Attention Deficit Hyperactivity Disorder (Adhd) | grm5_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 3 | completed | - | small molecule | not available | no | |
| fentanyl | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| fentanyl | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 1 | discontinued | - | small molecule | agonist | yes | Refs |
| fentanyl | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| fasoracetam monohydrate | Attention Deficit Hyperactivity Disorder (Adhd) | grm2_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 3 | completed | - | small molecule | not available | no | |
| fasoracetam monohydrate | Attention Deficit Hyperactivity Disorder (Adhd) | grm3_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 3 | completed | - | small molecule | not available | no | |
| fasoracetam monohydrate | Attention Deficit Hyperactivity Disorder (Adhd) | grm4_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 3 | completed | - | small molecule | not available | no | |
| fasoracetam monohydrate | Attention Deficit Hyperactivity Disorder (Adhd) | grm6_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 3 | completed | - | small molecule | not available | no | |
| fasoracetam monohydrate | Attention Deficit Hyperactivity Disorder (Adhd) | grm7_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 3 | completed | - | small molecule | not available | no | |
| fasoracetam monohydrate | Attention Deficit Hyperactivity Disorder (Adhd) | grm8_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 3 | completed | - | small molecule | not available | no | |
| felypressin | Hemostatic S; Vasoconstricting | v1ar_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | in trial | 1 | completed | - | peptide | agonist | no | Refs |
| fentanyl | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 1 | discontinued | - | small molecule | agonist | yes | Refs |
| fentanyl | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | discontinued | - | small molecule | agonist | yes | Refs |
| fentanyl | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| fentanyl | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 1 | discontinued | - | small molecule | agonist | yes | Refs |
| fentanyl | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| fentanyl | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 1 | discontinued | - | small molecule | agonist | yes | Refs |
| fentanyl | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | discontinued | - | small molecule | agonist | yes | Refs |
| fevipiprant | Anti-Asthmatic | pd2r2_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| fipamezole | Antiparkinson | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| fipamezole | Antiparkinson | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| fipamezole | Antiparkinson | ada2c_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| fk352b | Antihypertensive | aa1r_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| flupenthixol | Schizophrenia | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| flupenthixol | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| formoterol | Chronic Obstructive Pulmonary Disease (Copd) | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 3 | discontinued | - | small molecule | agonist | yes | Refs |
| formoterol | Bronchodilator | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 3 | completed | - | small molecule | agonist | yes | Refs |
| formoterol | Appetite Stimulant | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| fsh-gex | Fertility | fshr_human | primary | A (Rhodopsin) | Glycoprotein hormone receptors | in trial | 2 | completed | - | protein | agonist | no | |
| fx125l | Anti-Asthmatic | ssr2_human | primary | A (Rhodopsin) | Somatostatin receptors | in trial | 1 | completed | - | small molecule | agonist | no | |
| gc021109 | Alzheimer'S Disease | p2ry6_human | primary | A (Rhodopsin) | P2Y receptors | in trial | 1 | completed | - | small molecule | agonist | no | |
| gepirone | Anti-Depressant | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | completed | - | small molecule | partial agonist | no | |
| glasdegib | Antineoplastic | smo_human | primary | F (Frizzled) | Frizzled | in trial | 2 | completed | - | small molecule | antagonist | no | |
| glp | Appetite Suppressant | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 2 | completed | - | peptide | agonist | no | |
| glp1 agonist | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 1 | completed | - | unknown | agonist | no | |
| glpg0974 | Anti-Inflammatory ; Neutrophil Driven Inflammation; Ulcerative Colitis | ffar2_human | primary | A (Rhodopsin) | Free fatty acid receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| glpg1205 | For Ulcerative Colitis; Ibs | gpr84_human | primary | A (Rhodopsin) | Class A orphans | in trial | 2 | completed | - | small molecule | antagonist | no | |
| GMA102 | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 1 | ongoing | - | antibody | antagonist | no | |
| HTL18318 | Dementia ; Schizophrenia | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 1 | completed | - | small molecule | agonist | no | |
| gsk-1004723 | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| gsk-1004723 | Anti-Allergic | hrh3_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| hydrocodone | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | Refs |
| gsk163090 | Unipolar Depression | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| gsk163090 | Unipolar Depression | 5ht1b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| gsk163090 | Unipolar Depression | 5ht1d_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| gsk-961081 | Bronchodilator | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| gsk-961081 | Bronchodilator | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 2 | completed | - | small molecule | antagonist | no | |
| gtp-010 | Irritable Bowel Syndrome | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 2 | discontinued | - | protein | antagonist | no | |
| gtp-200 | Appetite Stimulant | ghsr_human | primary | A (Rhodopsin) | Ghrelin receptors | in trial | 2 | discontinued | - | peptide | agonist | no | |
| gtx-758 | Antineoplastic | lshr_human | primary | A (Rhodopsin) | Glycoprotein hormone receptors | in trial | 2 | recruiting | - | small molecule | agonist | no | |
| histamine | Cytorprotective During Cancer Treatment | hrh2_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 3 | recruiting | - | small molecule | agonist | no | Refs |
| homspera | Idiopathic Pulmonary Fibrosis | nk1r_human | primary | A (Rhodopsin) | Tachykinin receptors | in trial | 1 | ongoing | - | protein | agonist | no | |
| h-pth 1-34 | Anti-Osteoporotic | pth1r_human | primary | B1 (Secretin) | Parathyroid hormone receptors | in trial | 2 | discontinued | - | peptide | partial agonist | no | |
| h-pth 1-34 | Anti-Osteoporotic | pth2r_human | primary | B1 (Secretin) | Parathyroid hormone receptors | in trial | 2 | discontinued | - | peptide | partial agonist | no | |
| hydrocodone | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | Refs |
| hydromorphone | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 1 | completed | - | small molecule | agonist | yes | Refs |
| hydromorphone | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 1 | completed | - | small molecule | agonist | yes | Refs |
| hydromorphone | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 1 | completed | - | small molecule | agonist | yes | Refs |
| ibipinabant | Antidiabetic | cnr1_human | primary | A (Rhodopsin) | Cannabinoid receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| idalopirdine | Alzheimer'S Disease | 5ht6r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| iferanserin | Antihemorrhoidal | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| incb3284 | Anti-Inflammatory ; Dmard | ccr2_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| ino-8875 | Antiglaucomic | aa1r_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 3 | completed | - | small molecule | agonist | no | |
| ins-50589 | Antithrombotic | p2y12_human | primary | A (Rhodopsin) | P2Y receptors | in trial | 2 | discontinued | - | unknown | antagonist | no | |
| int-767 | Treatment Of Liver Fibrosis | gpbar_human | primary | A (Rhodopsin) | Bile acid receptors | in trial | 1 | ongoing | - | small molecule | agonist | no | |
| intepirdine | Alzheimer'S Disease | 5ht6r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| inv102 | For Inflammatory Lung Disease | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | ongoing | - | small molecule | inverse agonist | no | Refs |
| ipafricept | Antineoplastic | fzd8_human | primary | F (Frizzled) | Frizzled | in trial | 1 | ongoing | - | antibody | antagonist | no | |
| iph5401 | Antineoplastic | c5ar1_human | primary | A (Rhodopsin) | Complement peptide receptors | in trial | 1 | recruiting | - | antibody | antagonist | no | |
| ipi-926 | Antineoplastic | smo_human | primary | F (Frizzled) | Frizzled | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| irdabisant | Cognitive Impairment | hrh3_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 1 | completed | - | small molecule | antagonist | no | |
| isis 325568 | Antidiabetic | glr_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 1 | discontinued | - | antisense oligo | antagonist | no | |
| istradefylline | Antiparkinson | aa2ar_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 3 | completed | - | small molecule | antagonist | no | |
| itopride | Motilitant | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | completed | - | small molecule | antagonist | no | Refs |
| iti-007 | Schizophrenia | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| iti-007 | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| jnj-37822681 | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| jvs-100 | Cardioprotectant | cxcr4_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 2 | recruiting | - | dna plasmid | agonist | no | |
| kn38-7271 | Neuroprotectant | cnr1_human | primary | A (Rhodopsin) | Cannabinoid receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| kn38-7271 | Neuroprotectant | cnr2_human | primary | A (Rhodopsin) | Cannabinoid receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| kos-2187 | Gastrointestinal Motility Disorders | mtlr_human | primary | A (Rhodopsin) | Motilin receptors | in trial | 1 | discontinued | - | small molecule | agonist | no | |
| kuc-7483 | Overactive Bladder | adrb3_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 3 | completed | - | small molecule | agonist | no | |
| ladarixin | Bullous Pemphigoid | cxcr1_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| ladarixin | Bullous Pemphigoid | cxcr2_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| ljpc-501 | Hepatorenal Syndrome-Catecholamine-Resistant Hypotension (Crh) | agtr2_human | primary | A (Rhodopsin) | Angiotensin receptors | in trial | 3 | completed | - | peptide | agonist | no | |
| laropiprant | For Counteracting Niacin-Induced Flushing | pd2r_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| las-100977 | Bronchodilator | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| lasmiditan | Anti-Migraine | 5ht1f_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | ongoing | - | small molecule | agonist | no | |
| latanoprost | Antiglaucomic | pf2r_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| latanoprost | Antiglaucomic | pf2r_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 3 | completed | - | small molecule | agonist | yes | Refs |
| latanoprost | Antiglaucomic | pf2r_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 1 | completed | - | small molecule | agonist | yes | Refs |
| lecozotan | Alzheimer'S Disease | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| lemborexant | Insomnia | ox1r_human | primary | A (Rhodopsin) | Orexin receptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| lemborexant | Insomnia | ox2r_human | primary | A (Rhodopsin) | Orexin receptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| lesogaberan | Gastrointestinal Reflux Disease | gabr1_human | primary | C (Glutamate) | GABAB receptors | in trial | 2 | ongoing | - | small molecule | agonist | no | |
| lesogaberan | Gastrointestinal Reflux Disease | gabr2_human | primary | C (Glutamate) | GABAB receptors | in trial | 2 | ongoing | - | small molecule | agonist | no | |
| levodopa | Antiparkinson | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | suspended | - | small molecule | agonist | yes | Refs |
| nktr-181 | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | ongoing | - | small molecule polymer conjugate | agonist | no | |
| levodopa | Antiparkinson | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | recruiting | - | small molecule | agonist | yes | Refs |
| mar701 | Antidiabetic | gipr_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 1 | discontinued | - | peptide | agonist | no | |
| mar701 | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 1 | discontinued | - | peptide | agonist | no | |
| levodopa | Antiparkinson | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | suspended | - | small molecule | agonist | yes | Refs |
| levodopa | Antiparkinson | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | suspended | - | small molecule | agonist | yes | Refs |
| levodopa | Antiparkinson | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | suspended | - | small molecule | agonist | yes | Refs |
| levodopa | Antiparkinson | drd5_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | suspended | - | small molecule | agonist | yes | Refs |
| lu 02-750 | Antiparkinson | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 1 | discontinued | - | unknown | unknown | no | |
| lu 02-750 | Antiparkinson | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 1 | discontinued | - | unknown | unknown | no | |
| lu 02-750 | Antiparkinson | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 1 | discontinued | - | unknown | unknown | no | |
| lu 02-750 | Antiparkinson | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 1 | discontinued | - | unknown | unknown | no | |
| lu 02-750 | Antiparkinson | drd5_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 1 | discontinued | - | unknown | unknown | no | |
| levodopa | Antiparkinson | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | recruiting | - | small molecule | agonist | yes | Refs |
| levodopa | Antiparkinson | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | recruiting | - | small molecule | agonist | yes | Refs |
| levodopa | Antiparkinson | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | recruiting | - | small molecule | agonist | yes | Refs |
| levodopa | Antiparkinson | drd5_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | recruiting | - | small molecule | agonist | yes | Refs |
| lgd-6972 | Antidiabetic | glr_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| lixivaptan | Hyponatremia | v2r_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | in trial | 3 | completed | - | small molecule | antagonist | no | |
| ljpc-501 | Hepatorenal Syndrome-Catecholamine-Resistant Hypotension (Crh) | agtr1_human | primary | A (Rhodopsin) | Angiotensin receptors | in trial | 3 | completed | - | peptide | agonist | no | |
| mavoglurant | Obsessive-Compulsive Disorder | grm5_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| mbx-2982 | Antidiabetic | gp119_human | primary | A (Rhodopsin) | GPR18, GPR55 and GPR119 | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| lu ae04621 | Antiparkinson | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 1 | completed | - | unknown | agonist | no | |
| lu ae04621 | Antiparkinson | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 1 | completed | - | unknown | agonist | no | |
| lu ae04621 | Antiparkinson | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 1 | completed | - | unknown | agonist | no | |
| lu ae04621 | Antiparkinson | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 1 | completed | - | unknown | agonist | no | |
| lu ae04621 | Antiparkinson | drd5_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 1 | completed | - | unknown | agonist | no | |
| lu-ae58054 | Schizophrenia | 5ht6r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | ongoing | - | small molecule | antagonist | no | |
| luteinizing hormone-releasing hormone | Antineoplastic | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | in trial | 2 | completed | - | peptide | antagonist | no | |
| metoclopramide | Diabetic Gastroparesis | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | completed | - | small molecule | antagonist | yes | Refs |
| ly2140023 | Schizophrenia | grm2_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | |
| ly2140023 | Schizophrenia | grm3_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | |
| ly2590443 | Anti-Migraine | 5ht7r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| ly2881835 | Antidiabetic | ffar1_human | primary | A (Rhodopsin) | Free fatty acid receptors | in trial | 1 | completed | - | small molecule | agonist | no | |
| m0002 | Ascites | v2r_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| macimorelin | Growth Hormone Deficiency, Cancer Cachexia | ghsr_human | primary | A (Rhodopsin) | Ghrelin receptors | in trial | 3 | completed | - | peptide | agonist | no | |
| mc-4232 + mc-1 | Cardioprotectant | p2y12_human | primary | A (Rhodopsin) | P2Y receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| metoclopramide | Anti-Migraine | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | completed | - | small molecule | antagonist | yes | Refs |
| mc-1 | Cardioprotectant | p2ry1_human | primary | A (Rhodopsin) | P2Y receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| mc-1 | Cardioprotectant | p2ry4_human | primary | A (Rhodopsin) | P2Y receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| mc-1 | Cardioprotectant | p2y11_human | primary | A (Rhodopsin) | P2Y receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| mc-1 | Cardioprotectant | p2y13_human | primary | A (Rhodopsin) | P2Y receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| mc-1 | Cardioprotectant | p2y14_human | primary | A (Rhodopsin) | P2Y receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| mc-1 | Cardioprotectant | p2ry8_human | primary | A (Rhodopsin) | Class A orphans | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| mc-1 | Cardioprotectant | p2y10_human | primary | A (Rhodopsin) | Class A orphans | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| metoclopramide | Diabetic Gastroparesis | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | completed | - | small molecule | agonist | yes | Refs |
| metoclopramide | Anti-Migraine | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | completed | - | small molecule | agonist | yes | Refs |
| mc-4232 + mc-1 | Cardioprotectant | p2ry1_human | primary | A (Rhodopsin) | P2Y receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| mc-4232 + mc-1 | Cardioprotectant | p2ry2_human | primary | A (Rhodopsin) | P2Y receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| mc-4232 + mc-1 | Cardioprotectant | p2ry4_human | primary | A (Rhodopsin) | P2Y receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| mc-4232 + mc-1 | Cardioprotectant | p2ry6_human | primary | A (Rhodopsin) | P2Y receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| mc-4232 + mc-1 | Cardioprotectant | p2y11_human | primary | A (Rhodopsin) | P2Y receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| mc-4232 + mc-1 | Cardioprotectant | p2y13_human | primary | A (Rhodopsin) | P2Y receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| mc-4232 + mc-1 | Cardioprotectant | p2y14_human | primary | A (Rhodopsin) | P2Y receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| mc-4232 + mc-1 | Cardioprotectant | p2ry8_human | primary | A (Rhodopsin) | Class A orphans | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| mc-4232 + mc-1 | Cardioprotectant | p2y10_human | primary | A (Rhodopsin) | Class A orphans | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| mcd-386 | Alzheimer'S Disease | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 1 | discontinued | - | small molecule | agonist | no | |
| mg01ci | Neurologic Disorders; Adhd | 5ht2b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | terminated | - | small molecule | antagonist | no | |
| milveterol | Bronchodilator | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| min-001 | Schizophrenia | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| min-117 | Anti-Depressant | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | completed | - | small molecule | not available | no | |
| min-117 | Anti-Depressant | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | completed | - | small molecule | not available | no | |
| min-117 | Anti-Depressant | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| min-117 | Anti-Depressant | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| min-202 | Anti-Depressant And Sleep Disorder Therapy | ox2r_human | primary | A (Rhodopsin) | Orexin receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| mitemcinal | Gastroparesis | mtlr_human | primary | A (Rhodopsin) | Motilin receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| mk-0893 | Antidiabetic | glr_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| mle4901 | For Polycystic Ovarian Syndrome | nk3r_human | primary | A (Rhodopsin) | Tachykinin receptors | in trial | 2 | ongoing | - | small molecule | antagonist | no | |
| mn-221 | Anti-Asthmatic | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | completed | - | unknown | agonist | no | |
| mn-246 | Overactive Bladder | adrb3_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 1 | discontinued | - | small molecule | agonist | no | |
| mn-305 | Anti-Depressant; Hypnotic | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| nabilone | Analgesics; Neuropathic Pain; Restlegs Legs Syndrome | cnr1_human | primary | A (Rhodopsin) | Cannabinoid receptors | in trial | 3 | recruiting | - | small molecule | agonist | yes | Refs |
| mod-6031 | Antidiabetic ; Anti-Obesity | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 1 | recruiting | - | peptide | agonist | no | |
| mod-6031 | Antidiabetic ; Anti-Obesity | glr_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 1 | recruiting | - | peptide | agonist | no | |
| morphine | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| modimelanotide | Acute Kidney Injury | mshr_human | primary | A (Rhodopsin) | Melanocortin receptors | in trial | 2 | discontinued | - | protein | agonist | no | |
| modimelanotide | Acute Kidney Injury | mc3r_human | primary | A (Rhodopsin) | Melanocortin receptors | in trial | 2 | discontinued | - | protein | agonist | no | |
| mogamulizumab | Antineoplastic | ccr4_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 3 | ongoing | - | antibody | antagonist | no | |
| molindone | Adhd | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | Refs |
| montelukast | Anti-Asthmatic | cltr1_human | primary | A (Rhodopsin) | Leukotriene receptors | in trial | 3 | completed | - | small molecule | antagonist | yes | Refs |
| MOR107 | Diabetic Kidney Disease | agtr2_human | primary | A (Rhodopsin) | Angiotensin receptors | in trial | 1 | ongoing | - | peptide | agonist | no | |
| morphine | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| morphine | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | completed | - | small molecule | agonist | yes | Refs |
| morphine | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | completed | - | small molecule | agonist | yes | Refs |
| morphine | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | discontinued | - | small molecule | agonist | yes | Refs |
| morphine | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| morphine | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| morphine | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | completed | - | small molecule | agonist | yes | Refs |
| morphine | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | completed | - | small molecule | agonist | yes | Refs |
| morphine | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | completed | - | small molecule | agonist | yes | Refs |
| morphine | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | discontinued | - | small molecule | agonist | yes | Refs |
| morphine | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | completed | - | small molecule | agonist | yes | Refs |
| morphine | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | completed | - | small molecule | agonist | yes | Refs |
| morphine | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | discontinued | - | small molecule | agonist | yes | Refs |
| morphine | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| mosapride | Gastrointestinal Reflux Disease (Gerd) | 5ht4r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | recruiting | - | small molecule | agonist | no | |
| msx-122 | Antineoplastic | cxcr4_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 1 | discontinued | - | small molecule | antagonist | no | |
| mt-1303 | Autoimmune Diseases; Multiple Sclerosis; Crohn'S Disease | s1pr1_human | primary | A (Rhodopsin) | Lysophospholipid (S1P) receptors | in trial | 2 | ongoing | - | small molecule | antagonist | no | |
| nabilone | Analgesics; Neuropathic Pain; Restlegs Legs Syndrome | cnr2_human | primary | A (Rhodopsin) | Cannabinoid receptors | in trial | 3 | recruiting | - | small molecule | agonist | yes | Refs |
| nalbuphine | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| nalbuphine | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| nalbuphine | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| naltrexone | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | antagonist | yes | Refs |
| naltrexone | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | antagonist | yes | Refs |
| naltrexone | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | discontinued | - | small molecule | antagonist | yes | Refs |
| naltrexone | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | antagonist | yes | Refs |
| naltrexone | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | antagonist | yes | Refs |
| naltrexone | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | discontinued | - | small molecule | antagonist | yes | Refs |
| naltrexone | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | antagonist | yes | Refs |
| naltrexone | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | antagonist | yes | Refs |
| naltrexone | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | discontinued | - | small molecule | antagonist | yes | Refs |
| namacizumab¬â | Fibrosisâ¬Â | cnr1_human | primary | A (Rhodopsin) | Cannabinoid receptors | in trial | 1 | ongoing | - | antibody | NAM | no | |
| nu206 | Gastrointestinal Disease | lgr4_human | primary | A (Rhodopsin) | Class A orphans | in trial | 1 | discontinued | - | protein | not available | no | |
| nu206 | Gastrointestinal Disease | lgr5_human | primary | A (Rhodopsin) | Class A orphans | in trial | 1 | discontinued | - | protein | not available | no | |
| nbi-42902 | Postmenopausal Symptoms; Antineoplastic | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| ncx 1510 | Anti-Allergic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| ncx116 | Antiglaucomic | pf2r_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 3 | ongoing | - | small molecule | agonist | no | |
| nelotanserin | Dementia; Parkinson'S Disease | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | recruiting | - | small molecule | inverse agonist | no | |
| nemifitide | Anti-Depressant | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | discontinued | - | peptide | antagonist | no | |
| ngd-4715 | Appetite Suppressant | mchr1_human | primary | A (Rhodopsin) | Melanin-concentrating hormone | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| ngx267 | Dry Mouth | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| niacin | Antidyslipidaemic | hcar2_human | primary | A (Rhodopsin) | Hydroxycarboxylic acid receptors | in trial | 1 | discontinued | - | small molecule | agonist | no | Refs |
| niacin | Antidyslipidaemic | hcar2_human | primary | A (Rhodopsin) | Hydroxycarboxylic acid receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | Refs |
| niacin | Substance Abuse Deterrant | hcar2_human | primary | A (Rhodopsin) | Hydroxycarboxylic acid receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | Refs |
| niacin | Antidyslipidaemic | hcar3_human | primary | A (Rhodopsin) | Hydroxycarboxylic acid receptors | in trial | 1 | discontinued | - | small molecule | agonist | no | Refs |
| opc-51803 | Incontinence | v2r_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| niacin | Antidyslipidaemic | hcar3_human | primary | A (Rhodopsin) | Hydroxycarboxylic acid receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | Refs |
| niacin | Substance Abuse Deterrant | hcar3_human | primary | A (Rhodopsin) | Hydroxycarboxylic acid receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | Refs |
| nxn-188 | Anti-Migraine | 5ht1b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| nxn-188 | Anti-Migraine | 5ht1d_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| niacin receptor agonist | Anti-Atherosclerotic | hcar2_human | primary | A (Rhodopsin) | Hydroxycarboxylic acid receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| niacin receptor agonist | Anti-Atherosclerotic | hcar3_human | primary | A (Rhodopsin) | Hydroxycarboxylic acid receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| np2 enkephalin | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | viral gene delivery | agonist | no | |
| npsp795 | Hypocalcaemia | casr_human | primary | C (Glutamate) | Calcium-sensing receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| obe001 | Labor And Delivery | oxyr_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| nrp290 | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 1 | discontinued | - | small molecule | agonist | no | |
| nrp290 | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 1 | discontinued | - | small molecule | agonist | no | |
| nrp290 | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 1 | discontinued | - | small molecule | agonist | no | |
| OBE2109 | Endometriosis; Uterine Fibroids | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | in trial | 2 | ongoing | - | small molecule | antagonist | no | |
| ordopidine | Antiparkinson | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 1 | completed | - | small molecule | not available | no | |
| obinepitide | Anti-Obesity | npy2r_human | primary | A (Rhodopsin) | Neuropeptide Y receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| obinepitide | Anti-Obesity | npy4r_human | primary | A (Rhodopsin) | Neuropeptide Y receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| oc000459 | Anti-Allergic | pd2r2_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| oc459 | For Allergic Rhinitis | pd2r2_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| ormd-0901 | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 1 | completed | - | peptide | agonist | no | |
| odelepran | Alcohol Dependence | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| odelepran | Alcohol Dependence | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| odelepran | Alcohol Dependence | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| opa-6566 | Antiglaucomic | aa2ar_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| opc-14523 | Anti-Depressant | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| opc-28326 | Vasodilator | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| opc-28326 | Vasodilator | ada2c_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| orvepitant | Unipolar Depression | nk1r_human | primary | A (Rhodopsin) | Tachykinin receptors | in trial | 2 | not open yet | - | small molecule | antagonist | no | |
| oxybutynin | Incontinence | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | discontinued | - | small molecule | antagonist | yes | Refs |
| ostabolin-c | Anti-Osteoporotic | pth1r_human | primary | B1 (Secretin) | Parathyroid hormone receptors | in trial | 2 | discontinued | - | peptide | agonist | no | |
| ostabolin-c | Anti-Osteoporotic | pth2r_human | primary | B1 (Secretin) | Parathyroid hormone receptors | in trial | 2 | discontinued | - | peptide | agonist | no | |
| ot-730 | Antiglaucomic | adrb1_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| ot-730 | Antiglaucomic | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| OTSA-101-DTPA-90Y‰ | Antineoplastic | fzd10_human | primary | F (Frizzled) | Frizzled | in trial | 1 | ongoing | - | antibody | antagonist | no | |
| oxybutynin | Incontinence | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | discontinued | - | small molecule | antagonist | yes | Refs |
| oxybutynin | Incontinence | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | discontinued | - | small molecule | antagonist | yes | Refs |
| oxycodone | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| oxycodone | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| oxycodone | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | completed | - | small molecule | agonist | yes | Refs |
| oxycodone | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | discontinued | - | small molecule | agonist | yes | Refs |
| oxycodone | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| oxycodone | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| oxycodone | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | completed | - | small molecule | agonist | yes | Refs |
| oxycodone | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | discontinued | - | small molecule | agonist | yes | Refs |
| oxycodone | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| oxycodone | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| piclozotan | Stroke | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| oxycodone | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | discontinued | - | small molecule | agonist | yes | Refs |
| oxycodone | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | completed | - | small molecule | agonist | yes | Refs |
| ozanimod | Multiple Sclerosis | s1pr1_human | primary | A (Rhodopsin) | Lysophospholipid (S1P) receptors | in trial | 3 | completed | - | small molecule | agonist | no | |
| pitolisant | Antiparkinson | hrh3_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 3 | not open yet | - | small molecule | inverse agonist | no | |
| ozarelix | Antineoplastic | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | in trial | 2 | discontinued | - | peptide | antagonist | no | |
| p2045 | Antineoplastic | ssr2_human | primary | A (Rhodopsin) | Somatostatin receptors | in trial | 1 | withdrawn | - | peptide | agonist | no | |
| pa-401 | Anti-Inflammatory ; Immunosuppressant | cxcr1_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 1 | discontinued | - | protein | antagonist | no | |
| pa-401 | Anti-Inflammatory ; Immunosuppressant | cxcr2_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 1 | discontinued | - | protein | antagonist | no | |
| plozalizumab | Anti-Inflammatory ; Dmard; Diabetic Neophropathy | ccr2_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 2 | discontinued | - | antibody | antagonist | no | |
| pardoprunox | Antiparkinson | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | |
| pardoprunox | Antiparkinson | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | |
| pardoprunox | Antiparkinson | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | |
| pb1023 | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 2 | completed | - | protein | agonist | no | |
| pbf-509 | Antineoplastic | aa2ar_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| pbf-680 | Anti-Asthmatic | aa1r_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| pbf-999 | Huntington'S Disease | aa1r_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 1 | terminated | - | small molecule | antagonist | no | |
| plozalizumab | Antineoplastic | ccr2_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 2 | completed | - | antibody | antagonist | no | |
| pd-6735 | Hypnotics And Sedatives | mtr1a_human | primary | A (Rhodopsin) | Melatonin | in trial | 2 | completed | - | small molecule | agonist | no | |
| pd-6735 | Hypnotics And Sedatives | mtr1b_human | primary | A (Rhodopsin) | Melatonin | in trial | 2 | completed | - | small molecule | agonist | no | |
| pdc31 | Pre-Term Labor; Dysmenorrhea | pf2r_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 1 | completed | - | peptide | antagonist | no | |
| peptide yy | Appetite Suppressant | npy2r_human | primary | A (Rhodopsin) | Neuropeptide Y receptors | in trial | 1 | completed | - | peptide | agonist | no | |
| pexacerfont | Anxiety | crfr1_human | primary | B1 (Secretin) | Corticotropin-releasing factor receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| pf-00610355 | Bronchodilator | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| pf-03654746 | Allergic Rhinitis | hrh3_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| pf-03654764 | Allergic Rhinitis | hrh3_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| pf-05212377 | Alzheimer'S Disease | 5ht6r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | terminated | - | small molecule | antagonist | no | |
| ponesimod | Anti-Inflammatory ; Multiple Sclerosis | s1pr1_human | primary | A (Rhodopsin) | Lysophospholipid (S1P) receptors | in trial | 3 | recruiting | - | small molecule | agonist | no | |
| pramipexole | Antiparkinson | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | ongoing | - | small molecule | agonist | yes | Refs |
| pramipexole | Antiparkinson | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | ongoing | - | small molecule | agonist | yes | Refs |
| pramipexole | Antiparkinson | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | ongoing | - | small molecule | agonist | yes | Refs |
| preladenant | Antiparkinson | aa2ar_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| pridopidine | Huntington'S Disease | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | completed | - | small molecule | antagonist | no | |
| pro 140 | Antiviral ; Hiv | ccr5_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 3 | recruiting | - | antibody | antagonist | no | |
| procaterol | Bronchodilator | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 3 | recruiting | - | small molecule | agonist | no | Refs |
| prochlorperazine | Anti-Migraine | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | recruiting | - | small molecule | antagonist | yes | Refs |
| promethazine | Hypnotics And Sedatives; Anti-Anxiety S; Anti-Allergic ; Treat Migraines And Cluster Headaches | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 3 | completed | - | small molecule | antagonist | yes | Refs |
| prs-211375 | Analgesics | cnr2_human | primary | A (Rhodopsin) | Cannabinoid receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| prx-00023 | Anti-Depressant | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | |
| prx-07034 | Anti-Obesity ; Nootropic | 5ht6r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 1 | completed | - | small molecule | antagonist | no | |
| prx-08066 | Antihypertensive | 5ht2b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| prx-3140 | Alzheimer'S Disease | 5ht4r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| ps433540 | Focal Segmental Glomerulosclerosis, Antihypertensive | agtr2_human | primary | A (Rhodopsin) | Angiotensin receptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| ps433540 | Focal Segmental Glomerulosclerosis, Antihypertensive | agtr1_human | primary | A (Rhodopsin) | Angiotensin receptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| ps433540 | Focal Segmental Glomerulosclerosis, Antihypertensive | ednra_human | primary | A (Rhodopsin) | Endothelin receptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| psd-506 | Overactive Bladder | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| psd-506 | Overactive Bladder | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| psn602 | Anti-Obesity | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 1 | discontinued | - | small molecule | agonist | no | |
| psn821 | Antidiabetic | gp119_human | primary | A (Rhodopsin) | GPR18, GPR55 and GPR119 | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| PTH analog | Anti-Osteoporotic | pth1r_human | primary | B1 (Secretin) | Parathyroid hormone receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| pti-202 | Analgesics | oprd_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 1 | completed | - | unknown | not available | no | |
| pti-202 | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 1 | completed | - | unknown | not available | no | |
| pti-202 | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 1 | completed | - | unknown | not available | no | |
| PTR-36 | Anti-Asthmatic | pd2r2_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 2 | ongoing | - | small molecule | antagonist | no | |
| pw2101 | Antihypertensive | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 1 | discontinued | - | small molecule | antagonist | no | |
| pxt002331 | Antiparkinson | grm4_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 1 | completed | - | small molecule | PAM | no | |
| q-122 | Anti-Inflammatory ; Hot Flashes | cxcr4_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 1 | completed | - | small molecule | antagonist | no | |
| ralinepag | Antihypertensive | pi2r_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 2 | recruiting | - | small molecule | agonist | no | |
| re-021 | Kidney Disease; Nephropathy | agtr1_human | primary | A (Rhodopsin) | Angiotensin receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| re-021 | Kidney Disease; Nephropathy | ednra_human | primary | A (Rhodopsin) | Endothelin receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| relugolix | Endometriosis | gnrhr_human | primary | A (Rhodopsin) | Gonadotrophin-releasing hormone receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| remd-477 | Antidiabetic | glr_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 2 | recruiting | - | antibody | antagonist | no | |
| renzapride | Irritable Bowel Syndrome | 5ht4r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | Refs |
| renzapride | Irritable Bowel Syndrome | 5ht2b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| ryi-018 | Liver Disease; Nonalcoholic Steatohepatitis | cnr1_human | primary | A (Rhodopsin) | Cannabinoid receptors | in trial | 1 | not open yet | - | antibody | antagonist | no | |
| reparixin | Antidiabetic; Type I Diabetes | cxcr1_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 3 | ongoing | - | small molecule | antagonist | no | |
| reparixin | Antidiabetic; Type I Diabetes | cxcr2_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 3 | ongoing | - | small molecule | antagonist | no | |
| retosiban | Premature Birth | oxyr_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| rev131 | Anti-Allergic | hrh4_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| rg1068 | Autism, Schizophrenia | sctr_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 3 | discontinued | - | peptide | agonist | no | |
| rimegepant | Anti-Migraine | calrl_human | primary | B1 (Secretin) | Calcitonin receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| rm-493 | Anti-Obesity | mc4r_human | primary | A (Rhodopsin) | Melanocortin receptors | in trial | 3 | recruiting | - | peptide | agonist | no | |
| ro4917523 | Major Depressive Disorder, Fragile X Syndrome | grm5_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| rolofylline | Congestive Heart Failure | aa1r_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| ronacaleret | Anti-Osteoporotic | casr_human | primary | C (Glutamate) | Calcium-sensing receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | Refs |
| ropinirole | Restless Legs Syndrome | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 1 | discontinued | - | small molecule | agonist | yes | Refs |
| ropinirole | Restless Legs Syndrome | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 1 | discontinued | - | small molecule | agonist | yes | Refs |
| samidoprhan | Addiction | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| rusalatide | Diabetic Foot Ulcers | par1_human | primary | A (Rhodopsin) | Proteinase-activated receptors | in trial | 3 | discontinued | - | peptide | agonist | no | |
| rusalatide | Diabetic Foot Ulcers | par3_human | primary | A (Rhodopsin) | Proteinase-activated receptors | in trial | 3 | discontinued | - | peptide | agonist | no | |
| rusalatide | Diabetic Foot Ulcers | par4_human | primary | A (Rhodopsin) | Proteinase-activated receptors | in trial | 3 | discontinued | - | peptide | agonist | no | |
| rvt-101 | Alzheimer'S Disease | 5ht6r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | ongoing | - | small molecule | antagonist | no | |
| rx-10045 | Dry Eye | cml1_human | primary | A (Rhodopsin) | Chemerin receptor | in trial | 2 | completed | - | small molecule | agonist | no | |
| rx-10045 | Dry Eye | lt4r1_human | primary | A (Rhodopsin) | Leukotriene receptors | in trial | 2 | completed | - | small molecule | partial agonist | no | |
| saprisartan | Antihypertensive | agtr1_human | primary | A (Rhodopsin) | Angiotensin receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | Refs |
| saredutant | Anti-Depressant | nk2r_human | primary | A (Rhodopsin) | Tachykinin receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| sb-649868 | Insomnia | ox1r_human | primary | A (Rhodopsin) | Orexin receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| sb-649868 | Insomnia | ox2r_human | primary | A (Rhodopsin) | Orexin receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| sch-527123 | Chronic Obstructive Pulmonary Disease (Copd) | cxcr1_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| sch-527123 | Chronic Obstructive Pulmonary Disease (Copd) | cxcr2_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| selepressin | Septic Shock | v1ar_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | in trial | 3 | recruiting | - | protein | agonist | no | |
| semaglutide | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 3 | recruiting | - | peptide | agonist | no | |
| sens-111 | For Vertigo And Tinnitus | hrh4_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| serelaxin | Heart Failure Therapies | rxfp1_human | primary | A (Rhodopsin) | Relaxin family peptide receptors | in trial | 3 | completed | - | peptide | agonist | no | |
| serelaxin | Heart Failure Therapies | rxfp2_human | primary | A (Rhodopsin) | Relaxin family peptide receptors | in trial | 3 | completed | - | peptide | agonist | no | |
| SEP-363856 | Antiparkinson; Schizophrenia; Psychosis | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| SEP-363856 | Antiparkinson; Schizophrenia; Psychosis | taar1_human | primary | A (Rhodopsin) | Trace amine receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| ser100 | Antihypertensive | oprx_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| setipiprant | Seasonal Allergic Rhinitis | pd2r2_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| siponimod | Chronic Progressive Multiple Sclerosis | s1pr1_human | primary | A (Rhodopsin) | Lysophospholipid (S1P) receptors | in trial | 3 | ongoing | - | small molecule | agonist | no | |
| solabegron | Antidiabetic; Irritable Bowel Syndrome; Incontinence | adrb3_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 1 | recruiting | - | small molecule | agonist | no | Refs |
| SL 650472 | Intermittent Claudication | 5ht1b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| SL 650472 | Intermittent Claudication | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| sofpironium bromide | Anticholinergics; For Theâ¢¬à ¬öÂÇÂ좬ì Topical Treatment Of Primary Axillary Hyperhidrosis | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| spi-1620 | Adjuvant To Chemotherapy | ednrb_human | primary | A (Rhodopsin) | Endothelin receptors | in trial | 2 | discontinued | - | peptide | agonist | no | |
| sou-001 | Incontinence | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | discontinued | - | small molecule | not available | no | |
| sou-001 | Incontinence | ada1b_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | discontinued | - | small molecule | not available | no | |
| sou-001 | Incontinence | ada1d_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | discontinued | - | small molecule | not available | no | |
| strontium ranelate | Anti-Osteoporotic | casr_human | primary | C (Glutamate) | Calcium-sensing receptors | in trial | 3 | completed | - | small molecule | agonist | no | |
| stx107 | Fragile X Syndrome | grm5_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 2 | completed | - | small molecule | NAM | no | |
| sufentanil | Analgesics; Adjuvant To Anesthesia | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | suspended | - | small molecule | agonist | no | Refs |
| sufentanil | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | Refs |
| sulpiride | Antidepressive ; Second-Generation; Antipsychotic | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | Refs |
| sumatriptan | Anti-Migraine | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | completed | - | small molecule | agonist | yes | Refs |
| sumatriptan | Anti-Migraine | 5ht1f_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | completed | - | small molecule | agonist | yes | Refs |
| sumatriptan | Anti-Migraine | 5ht1b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | completed | - | small molecule | agonist | yes | Refs |
| sumatriptan | Anti-Migraine | 5ht1d_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | completed | - | small molecule | agonist | yes | Refs |
| surinabant | Smoking-Cessation, Obesity | cnr1_human | primary | A (Rhodopsin) | Cannabinoid receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| suvn-502 | Alzheimer'S Disease | 5ht6r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| suvn-d4010 | Alzheimer'S Disease | 5ht4r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 1 | recruiting | - | small molecule | agonist | no | |
| suvn-g3031 | Alzheimer'S Disease | hrh3_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 1 | recruiting | - | small molecule | antagonist | no | |
| svt-40776 | Incontinence | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 2 | completed | - | small molecule | antagonist | no | |
| syl040012 | Antiglaucomic | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | completed | - | sirna | antagonist | no | |
| syn120 | Cognitive Disorders | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| syn120 | Cognitive Disorders | 5ht6r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| t111 | Pruritus | aa2ar_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 3 | ongoing | - | small molecule | agonist | no | |
| t-62 | Analgesics | aa1r_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| tak-441 | Basal Cell Carcinoma | smo_human | primary | F (Frizzled) | Frizzled | in trial | 1 | discontinued | - | small molecule | antagonist | no | |
| tak-875 | Antidiabetic | ffar1_human | primary | A (Rhodopsin) | Free fatty acid receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | |
| taladegib | Antineoplastic | smo_human | primary | F (Frizzled) | Frizzled | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| talnetant | Schizophrenia | nk3r_human | primary | A (Rhodopsin) | Tachykinin receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| taranabant | Anti-Obesity ; Smoking-Cessation | cnr1_human | primary | A (Rhodopsin) | Cannabinoid receptors | in trial | 3 | discontinued | - | small molecule | inverse agonist | no | |
| tasosartan | Antihypertensive | agtr1_human | primary | A (Rhodopsin) | Angiotensin receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | Refs |
| taspoglutide | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 3 | discontinued | - | protein | agonist | no | |
| tbr-652 | Antiviral ; Hiv; Nonalcoholic Steatohepatitis | ccr5_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| td-1211 | Opioid-Induced Gastrointestinal Side-Effects | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| td-2749 | Motilitant | 5ht4r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 1 | discontinued | - | unknown | agonist | no | |
| td-4208 | Chronic Obstructive Pulmonary Disease (Copd) | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| tecadenoson | Anti-Arrhythmia | aa1r_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | Refs |
| THC:CBD | Multiple Sclerosis | cnr1_human | primary | A (Rhodopsin) | Cannabinoid receptors | in trial | 2 | ongoing | - | small molecule | antagonist | no | |
| THC:CBD | Multiple Sclerosis | cnr2_human | primary | A (Rhodopsin) | Cannabinoid receptors | in trial | 2 | ongoing | - | small molecule | antagonist | no | |
| tedatioxetine | Anti-Depressant | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| tedatioxetine | Anti-Depressant | ada1a_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| telcagepant | Anti-Migraine | calrl_human | primary | B1 (Secretin) | Calcitonin receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| temanogrel | Acute Coronary Syndrome | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 1 | unknown | - | small molecule | inverse agonist | no | |
| terguride | Diffuse Cutaneous Systemic Sclerosis, Antihypertensive | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | ongoing | - | small molecule | antagonist | no | |
| terguride | Diffuse Cutaneous Systemic Sclerosis, Antihypertensive | 5ht2b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | ongoing | - | small molecule | antagonist | no | |
| tetrahydrocannabivarin (thcv) | Antidiabetic | cnr1_human | primary | A (Rhodopsin) | Cannabinoid receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| tm30339 | Anti-Obesity | npy4r_human | primary | A (Rhodopsin) | Neuropeptide Y receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| tezosentan | Heart Failure | ednra_human | primary | A (Rhodopsin) | Endothelin receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| tezosentan | Heart Failure | ednrb_human | primary | A (Rhodopsin) | Endothelin receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| tg-0054 | Adjuvant To Stem Cell Transplantation | cxcr4_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| th0318 | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 1 | discontinued | - | peptide | agonist | no | |
| tonabersat | Anti-Migraine | 5ht1d_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| tm38837 | Anti-Obesity | cnr1_human | primary | A (Rhodopsin) | Cannabinoid receptors | in trial | 1 | completed | - | small molecule | antagonist | no | |
| tolterodine | Incontinence | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | completed | - | small molecule | antagonist | yes | Refs |
| tolterodine | Incontinence | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | completed | - | small molecule | antagonist | yes | Refs |
| tolterodine | Incontinence | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | completed | - | small molecule | antagonist | yes | Refs |
| toreforant | Anti-Asthmatic | hrh4_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| tozadenant | Antiparkinson | aa2ar_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 3 | not open yet | - | small molecule | antagonist | no | |
| tpi-asm8 | Anti-Asthmatic | ccr3_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 2 | discontinued | - | antisense oligo | antagonist | no | |
| trabodenoson | Antiglaucomic | aa1r_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| tradipitant | Alcohol Dependence | nk1r_human | primary | A (Rhodopsin) | Tachykinin receptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| tramadol | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| tramadol | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | recruiting | - | small molecule | agonist | yes | Refs |
| tramadol | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| tramadol | Analgesics | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | recruiting | - | small molecule | agonist | yes | Refs |
| tramadol | Analgesics | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | discontinued | - | small molecule | agonist | yes | Refs |
| tramadol | Analgesics | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | recruiting | - | small molecule | agonist | yes | Refs |
| trospium | Chronic Obstructive Pulmonary Disease (Copd) | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 2 | discontinued | - | small molecule | antagonist | yes | Refs |
| trv120027 | Antihypertensive | agtr1_human | primary | A (Rhodopsin) | Angiotensin receptors | in trial | 2 | recruiting | - | protein | antagonist | no | |
| trv130 | Analgesics; Post-Operative Pain | oprm_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 3 | recruiting | - | small molecule | agonist | no | |
| trv734 | Analgesics | oprk_human | primary | A (Rhodopsin) | Opioid receptors | in trial | 1 | completed | - | small molecule | agonist | no | |
| ts-032 | Schizophrenia | grm2_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 1 | discontinued | - | unknown | agonist | no | |
| ts-032 | Schizophrenia | grm3_human | primary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 1 | discontinued | - | unknown | agonist | no | |
| va111913 | Dysmenorrhea | v1ar_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| tt-223 | Antidiabetic; Injectable Islet Neogenesis Therapy For Diabetes | gasr_human | primary | A (Rhodopsin) | Cholecystokinin receptors | in trial | 2 | discontinued | - | injectible islet neogenesis therapy | agonist | no | |
| tt-223 | Antidiabetic; Injectable Islet Neogenesis Therapy For Diabetes | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 2 | discontinued | - | injectible islet neogenesis therapy | agonist | no | |
| tt-401 | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 2 | completed | - | peptide | agonist | no | |
| tt-401 | Antidiabetic | glr_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 2 | completed | - | peptide | agonist | no | |
| ttp054 | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| ttp273 | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 2 | completed | - | small molecule | agonist | no | |
| txa127 | For Stem Cell Engraftment And Thrombocytopenia | mas_human | primary | A (Rhodopsin) | Class A orphans | in trial | 2 | discontinued | - | peptide | agonist | no | |
| txa127 | Non-Hodgkinhodgkin Disease, Multiple Myeloma | mas_human | primary | A (Rhodopsin) | Class A orphans | in trial | 2 | ongoing | - | peptide | agonist | no | |
| tzp-102 | Gastroparesis | ghsr_human | primary | A (Rhodopsin) | Ghrelin receptors | in trial | 2 | terminated | - | small molecule | agonist | no | |
| ubrogepant | Anti-Migraine | calrl_human | primary | B1 (Secretin) | Calcitonin receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| ulimorelin | Gastroparesis | ghsr_human | primary | A (Rhodopsin) | Ghrelin receptors | in trial | 2 | recruiting | - | small molecule | agonist | no | Refs |
| ulocuplumab | Antineoplastic | cxcr4_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 3 | ongoing | - | antibody | antagonist | no | |
| vabicaserin | Schizophrenia | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| umeclidinium | Chronic Obstructive Pulmonary Disease (Copd) | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | ongoing | - | small molecule | antagonist | yes | Refs |
| umeclidinium | Chronic Obstructive Pulmonary Disease (Copd) | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | ongoing | - | small molecule | antagonist | yes | Refs |
| urocortin 2 | Congestive Heart Failure | crfr2_human | primary | B1 (Secretin) | Corticotropin-releasing factor receptors | in trial | 2 | discontinued | - | peptide | agonist | no | |
| v24343 | Anti-Obesity | cnr1_human | primary | A (Rhodopsin) | Cannabinoid receptors | in trial | 1 | discontinued | - | small molecule | antagonist | no | |
| v81444 | Antiparkinson | aa2ar_human | primary | A (Rhodopsin) | Adenosine receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| va106483 | Bph-Related Urinary Symptoms | v2r_human | primary | A (Rhodopsin) | Vasopressin and oxytocin receptors | in trial | 3 | recruiting | - | small molecule | agonist | no | |
| vantictumab | Antineoplastic | fzd7_human | primary | F (Frizzled) | Frizzled | in trial | 1 | ongoing | - | antibody | antagonist | no | |
| vapitadine | Anti-Allergic, Pruritus | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| vicriviroc | Antiviral ; Hiv | ccr5_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| vasoactive intestinal peptide | Sexual Dysfunction | vipr1_human | primary | B1 (Secretin) | VIP and PACAP receptors | in trial | 3 | completed | - | peptide | antagonist | no | |
| vasoactive intestinal peptide | Sexual Dysfunction | vipr2_human | primary | B1 (Secretin) | VIP and PACAP receptors | in trial | 3 | completed | - | peptide | antagonist | no | |
| vasomera | Antihypertensive | vipr2_human | primary | B1 (Secretin) | VIP and PACAP receptors | in trial | 2 | recruiting | - | peptide | antagonist | no | |
| velneperit | Anti-Obesity | npy5r_human | primary | A (Rhodopsin) | Neuropeptide Y receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| velusetrag | Motilitant | 5ht4r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | ongoing | - | small molecule | agonist | no | |
| vercirnon | Crohn'S Disease | ccr9_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| verucerfont | Congenital Adrenal Hyperplasia | crfr1_human | primary | B1 (Secretin) | Corticotropin-releasing factor receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| vestipitant | Tinnitus; Hypnotic | nk1r_human | primary | A (Rhodopsin) | Tachykinin receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| vibegron | Urinary Incontinence | adrb3_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | completed | nan | small molecule | agonist | no | |
| vidupiprant | Anti-Asthmatic | pd2r_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| vidupiprant | Anti-Asthmatic | pd2r2_human | primary | A (Rhodopsin) | Prostanoid receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| vilanterol | Chronic Obstructive Pulmonary Disease (Copd) | adrb2_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 3 | ongoing | - | small molecule | agonist | yes | Refs |
| vofopitant | Post-Traumatic Stress Disorder; Hypnotic | nk1r_human | primary | A (Rhodopsin) | Tachykinin receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| volinanserin | Hypnotics And Sedatives | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| vpd-737 | Pruritus | nk1r_human | primary | A (Rhodopsin) | Tachykinin receptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| vr-147 | Anti-Migraine | 5ht1b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 1 | discontinued | - | small molecule | not available | no | |
| vr-147 | Anti-Migraine | 5ht1d_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 1 | discontinued | - | small molecule | not available | no | |
| vrs-859 | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 1 | ongoing | - | peptide | agonist | no | |
| vsn16r | Antispasmodics; For Spatisity Related To Multiple Sclerosis | gpr55_human | primary | A (Rhodopsin) | GPR18, GPR55 and GPR119 | in trial | 2 | recruiting | - | small molecule | agonist | no | |
| x4p-001 | Antineoplastic ; Renal Cell Carcinoma | cxcr4_human | primary | A (Rhodopsin) | Chemokine receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| xaliproden | Neuroprotectant | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | |
| xanomeline + trospium chloride | Schizophrenia; Alzheimer'S Disease | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 2 | ongoing | - | small molecule | agonist | no | |
| xp21279 | Antiparkinson | drd1_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| xp21279 | Antiparkinson | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| xp21279 | Antiparkinson | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| xp21279 | Antiparkinson | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| xp21279 | Antiparkinson | drd5_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| ykp10811 | For Chronic Or Functional Constipation | 5ht4r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | completed | - | small molecule | agonist | no | |
| ykp-1358 | Schizophrenia | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | completed | - | unknown | antagonist | no | |
| ykp-1358 | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 2 | completed | - | unknown | antagonist | no | |
| ym-178 | Overactive Bladder | adrb3_human | primary | A (Rhodopsin) | Adrenoceptors | in trial | 3 | recruiting | - | small molecule | agonist | no | |
| ym-598 | Antineoplastic | ednra_human | primary | A (Rhodopsin) | Endothelin receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| cannabidiol | Schizophrenia | cnr1_human | secondary | A (Rhodopsin) | Cannabinoid receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| cannabidiol | Schizophrenia | cnr2_human | secondary | A (Rhodopsin) | Cannabinoid receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| yttrium-90 edotreotide | Antineoplastic | ssr1_human | primary | A (Rhodopsin) | Somatostatin receptors | in trial | 2 | not open yet | - | peptide | antagonist | no | |
| yttrium-90 edotreotide | Antineoplastic | ssr2_human | primary | A (Rhodopsin) | Somatostatin receptors | in trial | 2 | not open yet | - | peptide | antagonist | no | |
| yttrium-90 edotreotide | Antineoplastic | ssr5_human | primary | A (Rhodopsin) | Somatostatin receptors | in trial | 2 | not open yet | - | peptide | antagonist | no | |
| zibotentan | Antineoplastic | ednra_human | primary | A (Rhodopsin) | Endothelin receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| zicronapine | Schizophrenia | drd4_human | primary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | completed | - | small molecule | antagonist | no | |
| zolmitriptan | Anti-Migraine | 5ht1a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | completed | - | small molecule | agonist | yes | Refs |
| zolmitriptan | Anti-Migraine | 5ht1d_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | completed | - | small molecule | agonist | yes | Refs |
| zolmitriptan | Anti-Migraine | 5ht1b_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | completed | - | small molecule | agonist | yes | Refs |
| zolmitriptan | Anti-Migraine | 5ht1f_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | completed | - | small molecule | agonist | yes | Refs |
| zp1848 | Crohn'S Disease | glp2r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 2 | recruiting | - | peptide | agonist | no | |
| zpl-389 | Anti-Inflammatory ; Atopic Dermatitis | hrh4_human | primary | A (Rhodopsin) | Histamine receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| zyd1 | Antidiabetic | glp1r_human | primary | B1 (Secretin) | Glucagon receptor family | in trial | 1 | completed | - | peptide | agonist | no | |
| cannabidiol | Graft Versus Host Disease | cnr1_human | secondary | A (Rhodopsin) | Cannabinoid receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| cannabidiol | Graft Versus Host Disease | cnr2_human | secondary | A (Rhodopsin) | Cannabinoid receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| dexpramipexole | Amyotrophic Lateral Sclerosis (Als) | drd2_human | secondary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | terminated | - | small molecule | agonist | no | |
| dexpramipexole | Amyotrophic Lateral Sclerosis (Als) | drd3_human | secondary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | terminated | - | small molecule | agonist | no | |
| dexpramipexole | Amyotrophic Lateral Sclerosis (Als) | drd4_human | secondary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | terminated | - | small molecule | agonist | no | |
| agn-214868 | Analgesics; Neuralgia | ada1a_human | secondary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | terminated | - | small molecule | antagonist | no | |
| agn-214868 | Analgesics; Neuralgia | ada1b_human | secondary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | terminated | - | small molecule | antagonist | no | |
| agn-214868 | Analgesics; Neuralgia | ada1d_human | secondary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | terminated | - | small molecule | antagonist | no | |
| agn-214868 | Analgesics; Neuralgia | ada2a_human | secondary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | terminated | - | small molecule | antagonist | no | |
| agn-214868 | Analgesics; Neuralgia | ada2b_human | secondary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | terminated | - | small molecule | antagonist | no | |
| agn-214868 | Analgesics; Neuralgia | ada2c_human | secondary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | terminated | - | small molecule | antagonist | no | |
| alks 33 | Alcohol Dependance; Anti-Depressant | oprd_human | secondary | A (Rhodopsin) | Opioid receptors | in trial | 1 | discontinued | - | small molecule | antagonist | no | |
| alks 33 | Alcohol Dependance; Anti-Depressant | oprd_human | secondary | A (Rhodopsin) | Opioid receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| alks 33 | Alcohol Dependance; Anti-Depressant | oprd_human | secondary | A (Rhodopsin) | Opioid receptors | in trial | 3 | completed | - | small molecule | antagonist | no | |
| alks 33 | Anti-Obesity | oprd_human | secondary | A (Rhodopsin) | Opioid receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| alks 37 | Motilitant | oprd_human | secondary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| cannabidiol | Epilepsy | cnr1_human | secondary | A (Rhodopsin) | Cannabinoid receptors | in trial | 3 | not open yet | - | small molecule | antagonist | no | |
| cannabidiol | Epilepsy | cnr2_human | secondary | A (Rhodopsin) | Cannabinoid receptors | in trial | 3 | not open yet | - | small molecule | antagonist | no | |
| avr118 | Antineoplastic Agent, Wound Healing Accelerant | aa2ar_human | secondary | A (Rhodopsin) | Adenosine receptors | in trial | 2 | discontinued | - | peptide nucleic acid | not available | no | |
| avr118 | Antineoplastic Agent, Wound Healing Accelerant | aa2br_human | secondary | A (Rhodopsin) | Adenosine receptors | in trial | 2 | discontinued | - | peptide nucleic acid | not available | no | |
| avr118 | Antineoplastic Agent, Wound Healing Accelerant | aa3r_human | secondary | A (Rhodopsin) | Adenosine receptors | in trial | 2 | discontinued | - | peptide nucleic acid | not available | no | |
| cannabidiol | Epilepsy | cnr1_human | secondary | A (Rhodopsin) | Cannabinoid receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| cannabidiol | Epilepsy | cnr2_human | secondary | A (Rhodopsin) | Cannabinoid receptors | in trial | 3 | recruiting | - | small molecule | antagonist | no | |
| dg3173 | Hormone Replacement | ssr1_human | secondary | A (Rhodopsin) | Somatostatin receptors | in trial | 2 | ongoing | - | small molecule | agonist | no | |
| cannabidivarin | Epilepsy | cnr1_human | secondary | A (Rhodopsin) | Cannabinoid receptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| cannabidivarin | Epilepsy | cnr2_human | secondary | A (Rhodopsin) | Cannabinoid receptors | in trial | 2 | recruiting | - | small molecule | antagonist | no | |
| fasoracetam monohydrate | Attention Deficit Hyperactivity Disorder (Adhd) | grm1_human | secondary | C (Glutamate) | Metabotropic glutamate receptors | in trial | 3 | completed | - | small molecule | not available | no | |
| guanabenz | Multiple Sclerosis | ada2b_human | secondary | A (Rhodopsin) | Adrenoceptors | in trial | 1 | recruiting | - | small molecule | agonist | no | Refs |
| cicletanine | Antihypertensive | ada1a_human | secondary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | not open yet | - | small molecule | not available | no | |
| cicletanine | Antihypertensive | ada1d_human | secondary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | not open yet | - | small molecule | not available | no | |
| cicletanine | Antihypertensive | ada2a_human | secondary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | not open yet | - | small molecule | not available | no | |
| cicletanine | Antihypertensive | ada2b_human | secondary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | not open yet | - | small molecule | not available | no | |
| cicletanine | Antihypertensive | ada2c_human | secondary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | not open yet | - | small molecule | not available | no | |
| cicletanine | Antihypertensive | adrb2_human | secondary | A (Rhodopsin) | Adrenoceptors | in trial | 2 | not open yet | - | small molecule | not available | no | |
| corticotropin-releasing factor | Peritumoral Brain Edema | crfr2_human | secondary | B1 (Secretin) | Corticotropin-releasing factor receptors | in trial | 3 | discontinued | - | peptide | agonist | no | |
| darusentan | Antihypertensive | ednrb_human | secondary | A (Rhodopsin) | Endothelin receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| davalintide | Anti-Obesity | calrl_human | secondary | B1 (Secretin) | Calcitonin receptors | in trial | 2 | discontinued | - | protein | agonist | no | |
| pardoprunox | Antiparkinson | 5ht7r_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | |
| pardoprunox | Antiparkinson | ada1a_human | secondary | A (Rhodopsin) | Adrenoceptors | in trial | 3 | discontinued | - | small molecule | agonist | no | |
| pardoprunox | Antiparkinson | ada2a_human | secondary | A (Rhodopsin) | Adrenoceptors | in trial | 3 | discontinued | - | small molecule | agonist | no | |
| pardoprunox | Antiparkinson | drd4_human | secondary | A (Rhodopsin) | Dopamine receptors | in trial | 3 | discontinued | - | small molecule | agonist | no | |
| mc-1 | Cardioprotectant | lpar4_human | secondary | A (Rhodopsin) | Lysophospholipid (LPA) receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| mc-1 | Cardioprotectant | lpar6_human | secondary | A (Rhodopsin) | Lysophospholipid (LPA) receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| mc-4232 + mc-1 | Cardioprotectant | lpar4_human | secondary | A (Rhodopsin) | Lysophospholipid (LPA) receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| mc-4232 + mc-1 | Cardioprotectant | lpar6_human | secondary | A (Rhodopsin) | Lysophospholipid (LPA) receptors | in trial | 2 | discontinued | - | small molecule | antagonist | no | |
| renzapride | Irritable Bowel Syndrome | 5ht2a_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| renzapride | Irritable Bowel Syndrome | 5ht2c_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 3 | discontinued | - | small molecule | antagonist | no | |
| spi-1620 | Adjuvant To Chemotherapy | ednra_human | secondary | A (Rhodopsin) | Endothelin receptors | in trial | 2 | discontinued | - | peptide | agonist | no | |
| sufentanil | Analgesics; Adjuvant To Anesthesia | oprd_human | secondary | A (Rhodopsin) | Opioid receptors | in trial | 2 | suspended | - | small molecule | agonist | no | Refs |
| promethazine | Hypnotics And Sedatives; Anti-Anxiety S; Anti-Allergic ; Treat Migraines And Cluster Headaches | acm1_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | completed | - | small molecule | antagonist | yes | Refs |
| promethazine | Hypnotics And Sedatives; Anti-Anxiety S; Anti-Allergic ; Treat Migraines And Cluster Headaches | acm2_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | completed | - | small molecule | antagonist | yes | Refs |
| promethazine | Hypnotics And Sedatives; Anti-Anxiety S; Anti-Allergic ; Treat Migraines And Cluster Headaches | acm3_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | completed | - | small molecule | antagonist | yes | Refs |
| promethazine | Hypnotics And Sedatives; Anti-Anxiety S; Anti-Allergic ; Treat Migraines And Cluster Headaches | acm4_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | completed | - | small molecule | antagonist | yes | Refs |
| promethazine | Hypnotics And Sedatives; Anti-Anxiety S; Anti-Allergic ; Treat Migraines And Cluster Headaches | acm5_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | completed | - | small molecule | antagonist | yes | Refs |
| sufentanil | Analgesics; Adjuvant To Anesthesia | oprk_human | secondary | A (Rhodopsin) | Opioid receptors | in trial | 2 | suspended | - | small molecule | agonist | no | Refs |
| sufentanil | Analgesics | oprd_human | secondary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | Refs |
| sufentanil | Analgesics | oprk_human | secondary | A (Rhodopsin) | Opioid receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | Refs |
| tolterodine | Incontinence | acm4_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | completed | - | small molecule | antagonist | yes | Refs |
| tolterodine | Incontinence | acm5_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 3 | completed | - | small molecule | antagonist | yes | Refs |
| va111913 | Dysmenorrhea | v1br_human | secondary | A (Rhodopsin) | Vasopressin and oxytocin receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| va111913 | Dysmenorrhea | v2r_human | secondary | A (Rhodopsin) | Vasopressin and oxytocin receptors | in trial | 2 | completed | - | small molecule | antagonist | no | |
| vabicaserin | Schizophrenia | 5ht2a_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| vabicaserin | Schizophrenia | 5ht2b_human | secondary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | in trial | 2 | discontinued | - | small molecule | agonist | no | |
| xanomeline + trospium chloride | Schizophrenia; Alzheimer'S Disease | acm2_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 2 | ongoing | - | small molecule | agonist | no | |
| xanomeline + trospium chloride | Schizophrenia; Alzheimer'S Disease | acm3_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 2 | ongoing | - | small molecule | agonist | no | |
| xanomeline + trospium chloride | Schizophrenia; Alzheimer'S Disease | acm4_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 2 | ongoing | - | small molecule | agonist | no | |
| xanomeline + trospium chloride | Schizophrenia; Alzheimer'S Disease | acm5_human | secondary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | in trial | 2 | ongoing | - | small molecule | agonist | no | |
| adx71441 | Neurologic Disorders | gabr1_human | primary | C (Glutamate) | GABAB receptors | preclinical | 0 | not open yet | - | small molecule | PAM | no | |
| adx71441 | Neurologic Disorders | gabr2_human | primary | C (Glutamate) | GABAB receptors | preclinical | 0 | not open yet | - | small molecule | PAM | no | |
| cannabidiol | Anticonvulsants; Antiepileptics | gpr55_human | primary | A (Rhodopsin) | GPR18, GPR55 and GPR119 | preclinical | 0 | not open yet | - | small molecule | agonist | no | |
| CNTX-6016 | Analgesics | cnr2_human | primary | A (Rhodopsin) | Cannabinoid receptors | preclinical | 0 | not open yet | - | small molecule | agonist | no | |
| cosyntropin | Epilepsy | acthr_human | primary | A (Rhodopsin) | Melanocortin receptors | preclinical | 0 | ongoing | - | peptide | agonist | no | Refs |
| nps-2143 | Anti-Osteoporotic | casr_human | primary | C (Glutamate) | Calcium-sensing receptors | preclinical | 0 | completed | - | small molecule | antagonist | no | |
| sb-269652 | Antipsychotic | drd3_human | primary | A (Rhodopsin) | Dopamine receptors | preclinical | 0 | unknown | - | small molecule | antagonist | no | |
| srx-1177 | Antineoplastic | mshr_human | primary | A (Rhodopsin) | Melanocortin receptors | preclinical | 0 | not open yet | - | peptide | not available | no | |
| tetrahydrocannabinol prodrug | Neuropathic Pain; Fibromyalgia | cnr1_human | primary | A (Rhodopsin) | Cannabinoid receptors | preclinical | 0 | not open yet | - | small molecule | agonist | no | Refs |
| tetrahydrocannabinol prodrug | Neuropathic Pain; Fibromyalgia | cnr2_human | primary | A (Rhodopsin) | Cannabinoid receptors | preclinical | 0 | not open yet | - | small molecule | agonist | no | Refs |
| tetrahydrocannabinol prodrug | Neuropathic Pain; Fibromyalgia | gpr55_human | primary | A (Rhodopsin) | GPR18, GPR55 and GPR119 | preclinical | 0 | not open yet | - | small molecule | agonist | no | |
| yohimbine | Mydriatics; Anti-Impotence | ada2c_human | primary | A (Rhodopsin) | Adrenoceptors | preclinical | 0 | discontinued | - | small molecule | antagonist | no | Refs |
| yohimbine | Mydriatics; Anti-Impotence | ada2a_human | primary | A (Rhodopsin) | Adrenoceptors | preclinical | 0 | discontinued | - | small molecule | antagonist | no | Refs |
| yohimbine | Mydriatics; Anti-Impotence | ada2b_human | primary | A (Rhodopsin) | Adrenoceptors | preclinical | 0 | discontinued | - | small molecule | antagonist | no | Refs |
| sertindole | Schizophrenia | ada1a_human | secondary | A (Rhodopsin) | Adrenoceptors | withdrawn | 3 | recruiting | 1998 | small molecule | antagonist | no | Refs |
| cannabidiol | Anticonvulsants; Antiepileptics | cnr1_human | secondary | A (Rhodopsin) | Cannabinoid receptors | preclinical | 0 | not open yet | - | small molecule | agonist | no | |
| cannabidiol | Anticonvulsants; Antiepileptics | cnr2_human | secondary | A (Rhodopsin) | Cannabinoid receptors | preclinical | 0 | not open yet | - | small molecule | agonist | no | |
| benzquinamide | Antiemetics; Antipsychotic | acm1_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | withdrawn | 4 | - | 1974 | small molecule | antagonist | no | Refs |
| benzquinamide | Antiemetics; Antipsychotic | acm2_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | withdrawn | 4 | - | 1974 | small molecule | antagonist | no | Refs |
| benzquinamide | Antiemetics; Antipsychotic | acm3_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | withdrawn | 4 | - | 1974 | small molecule | antagonist | no | Refs |
| benzquinamide | Antiemetics; Antipsychotic | acm4_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | withdrawn | 4 | - | 1974 | small molecule | antagonist | no | Refs |
| benzquinamide | Antiemetics; Antipsychotic | acm5_human | primary | A (Rhodopsin) | Acetylcholine receptors (muscarinic) | withdrawn | 4 | - | 1974 | small molecule | antagonist | no | Refs |
| benzquinamide | Antiemetics; Antipsychotic | hrh1_human | primary | A (Rhodopsin) | Histamine receptors | withdrawn | 4 | - | 1974 | small molecule | antagonist | no | Refs |
| sertindole | Schizophrenia | 5ht6r_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | withdrawn | 3 | recruiting | 1998 | small molecule | antagonist | no | Refs |
| sertindole | Schizophrenia | 5ht2c_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | withdrawn | 3 | recruiting | 1998 | small molecule | inverse agonist | no | Refs |
| sertindole | Schizophrenia | drd2_human | primary | A (Rhodopsin) | Dopamine receptors | withdrawn | 3 | recruiting | 1998 | small molecule | antagonist | no | Refs |
| sertindole | Schizophrenia | 5ht2a_human | primary | A (Rhodopsin) | 5-Hydroxytryptamine receptors | withdrawn | 3 | recruiting | 1998 | small molecule | antagonist | no | Refs |
| sertindole | Schizophrenia | ada1b_human | secondary | A (Rhodopsin) | Adrenoceptors | withdrawn | 3 | recruiting | 1998 | small molecule | antagonist | no | Refs |
| sertindole | Schizophrenia | ada1d_human | secondary | A (Rhodopsin) | Adrenoceptors | withdrawn | 3 | recruiting | 1998 | small molecule | antagonist | no | Refs |