Receptor | Class | PMIDd | PDB ID | Drug | Efficacy | Drug IDa | Action |
---|---|---|---|---|---|---|---|
Approved drugs | |||||||
β1 adrenergic receptor (turkey) | A | 21228877 | 2Y04 | Salbutamol | Agonist (partial) | DB01001 | Asthma and obstructive pulmonary disease |
21228877 | 2Y03 | Isoprenaline | Agonist | DB01064 | Bronchodilator and heart stimulant | ||
21228877 | 2Y01 | Dobutamine | Agonist (partial) | DB00841 | Cardiac stimulant used after heart attack | ||
22579251 | 4AMJ | Carvedilol | Inverse agonist | DB01136 | Congestive heart failure | ||
β2 adrenergic receptor (human) | A | 18547522 | 3D4S | Timolol | Inverse agonist | DB00373 | Antihypertensive, antiangina, and antiarrhythmic. |
20669948 | 3NYA | Alprenolol | Antagonist | DB00866 | Antihypertensive, antiangina, and antiarrhythmic | ||
24056936 | 4LDO | Adrenaline | Agonist | DB00668 | Asthma and cardiac failure | ||
M3 muscarinic acetylcholine receptor (rat) | A | 22358844 | 4DAJ | Tiotropium | Inverse agonist | DB01409 | Bronchodilator used in the management of chronic obstructive pulmonary disease |
Serotonin 1b receptor (human) | A | 23519210 | 4IAR | Ergotamine | Agonist | DB00696 | Treatment of migraine |
23519210 | 4IAQ | Dihydroergotamine | Agonist | DB00320 | Treatment of migraine | ||
Serotonin 2b receptor (human) | A | 23519210 | 4IB4 | Ergotamine | Agonist | DB00696 | Treatment of migraine |
H1 histamine receptor (human) | A | 21697825 | 3RZE | Doxepin (E,Z) | Antagonist | DB01142 | Sedativeb |
Adenosine A2A receptor (human) | A | 21593763 | 2YDO | Adenosine | Agonist | DB00640 | Treatment of some types of tachycardia |
21885291 | 3RFM | Caffeine | Antagonist | DB00201 | Central nervous system stimulant, appears to be useful in the treatment of some types of headache | ||
CCR5 C-C chemokine receptor type 5 (human) | A | 24030490 | 4MBS | Maraviroc | Antagonist | DB04835 | Treatment of human immunodeficiency virus infection |
OX2 orexin 2 receptor (human) | A | 25533960 | 4S0V | Suvorexant | Antagonist | 24965990c | Treatment of insomnia |
Protease-activated receptor type 1 (human) | A | 23222541 | 3VW7 | Vorapaxar | Antagonist | 10077130c | Treatment of acute coronary syndrome chest pain caused by coronary artery disease |
In clinical trials | |||||||
P2Y12 purinergic receptor (human) | A | 24670650 | 4NTJ | AZD1283 | Antagonist | 23649325c | Treatment of acute arterial thrombosis |
Smoothened receptor (human) | F | 23636324 | 4JKV | LY2940680 | Antagonist | 49848070c | Treatment of small-cell lung cancer |
Development discontinued | |||||||
κ Opioid receptor (human) | A | 22437504 | 4DJH | JDTic | Antagonist | 9956146c | Treatment of cocaine abuse |
Free fatty acid receptor type 1 (human) | A | 25043059 | 4PHU | TAK-875 (fasiglifam) | Agonist | 24857286c | Treatment of type 2 diabetes |
Metabotropic glutamate receptor type 5 (human) | C | 25042998 | 4OO9 | Mavoglurant | Negative allosteric modulator | 9926832c | Treatment of fragile X syndrome |
AZD1283, ethyl 6-[4-(benzylsulfonylcarbamoyl)piperidin-1-yl]-5-cyano-2-methylpyridine-3-carboxylate; JDTic, (3R)-7-hydroxy-N-[(2S)-1-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]-3-methylbutan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide; LY2940680, 4-fluoro-N-methyl-N-[1-[4-(2-methylpyrazol-3-yl)phthalazin-1-yl]piperidin-4-yl]-2-(trifluoromethyl)benzamide.
↵a DrugBank ID (when available).
↵b Doxepin has antidepressant effects, due to an overall increase in serotonergic neurotransmission; blocking of histamine H1 receptors accounts for its sedative effects.
↵c PubChem CID.
↵d PubMed manuscript ID.