Aripiprazole(Abilify) is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.

APD-371 (APD371, Olorinab) is a potent, selective and orally available CB2 agonist with EC50 of 6.2 nM; displays no activity against CB1 receptors (EC50>10 uM); exhibits activity in rat model of osteoarthritis pain.

AMG 853 is novel a CRTH2 and DP Dual Antagonist.

AM9405 (AM-9405) is novel potent, peripherally active cannabinoid type 1 (CB1) and 5-HT3 receptor agonist, inhibits the EFS-induced twitch contraction of the ileum and the colon with IC50 of 0.076 and 45.71 nM, respectively.

AM-6538 (AM6538) is a potent, selective cannabinoid receptor CB1 antagonist with Ki of 5.1 nM..

Alvimopan(LY 246736; ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.

Alvimopan(LY 246736; ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.

Alosetron Hydrochloride is the hydrochloride salt form of alosetron, a potent and selective 5-HT3 receptor antagonist.

Alfuzosin is an α1 adrenergic receptor antagonist used to treat benign prostatic hyperplasia (BPH).

Alcaftadine

Agomelatine is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor.

AGN192836 (AGN 192836) is a potent, selective α2 adrenergic (alpha 2-adrenoceptor) agonist with EC50 of 8.7, 41 and 6.6 nM for α2A, α2B and α2C receptor, respectively.

AGN 210676 is a selective prostaglandin EP2 agonist extracted from patent US20070203222A1, Compound example 23, has an EC50 of 5 nM.

ACT-246475 (ACT246475) is a potent, selective, reversible P2Y12 receptor antagonist with binding IC50 of 1.0 nM.

Acrivastine (BW825C) is a short acting histamine 1 receptor antagonist for the treatment of allergic rhinitis.

AC264613 is a potent and selective protease-activated receptor 2 (PAR2) agonist (pEC50 = 7.5). Displays no activity at other PAR subtypes and exhibits no significant activity at over 30 other receptors implicated in nociception and inflammation.

AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6.

A synthetic immunosuppressant that functions as a S1P1 receptor agonist.

A small-molecule partial agonist of CXCR7 (ACKR3)..

A small-molecule partial agonist of CXCR7 (ACKR3)..

A small-molecule partial agonist of CXCR7 (ACKR3)..

A small molecule CMKLR1 antagonist that inhibits chemerin-stimulated β-arrestin2 association with CMKLR1 (EC50=9.7 nM).

A potential antipsychotic agent that binds selectively to D4 and 5-HT2A receptors with Ki of 3.0 and 5.8 nM, respectively.

A potent, specific, noncompetitive dual CXCR1 and CXCR2 antagonist with IC50 of 38 nM (vs. CXCL1) and 36 nM (vs. CXCL8), respectively.

A potent, specfic CXCR2 antagonist that inhibits IL8 down-regulation of forskolin-induced cAMP with IC50 of 7.79 uM.

A potent, selective, orally bioavailable GPR120 agonist with EC50 of 42 nM in calcium flux assays.

A potent, selective, orally available GPR40 agonist with Ki of 15 nM, β-arrestin EC50 of 108 nM.

A potent, selective, orally available GPR40 agonist with EC50 of 9 nM.

A potent, selective, orally available GPR40 agonist with EC50 of 8 nM.

A potent, selective, orally active agonist of dopamine D3 receptor with EC50 of 21 nM.