| 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 | |