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

Almorexant(ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.

ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated prodrug of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound. ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease.

AMG 333 is a potent and highly selective TRPM8 antagonist with an IC50 of 13 nM.

AMG-579 is a potent, selective, CNS penetrant, orally bioavailable PDE10A inhibitor with IC50 of 0.1 nM.

AMG9810 is a potent and selective, competitive vanilloid TRPV1 receptor antagonist (IC50 = 17 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.

Atipamezole Hcl(MPV1248 Hcl) is an alpha-adrenoceptor antagonist with high affinity and selectivity for the alpha 2-receptor.

Atipamezole(MPV1248) is an alpha-adrenoceptor antagonist with high affinity and selectivity for the alpha 2-receptor.

AZD3293 is a potent and selective orally active, brain-permeable BACE1 inhibitor,currently in development as a potential treatment for early Alzheimer’s disease.

AZD3839 is a potent and selective BACE1 inhibitor with Ki of 26.1 nM, about 14-fold selectivity over BACE2. Phase 1.

Azeliragon is an oral, small-molecule inhibitor of RAGE.

Basmisanil is a highly selective inverse agonist/negative allosteric modulator of α5 subunit-containing GABAA receptors which is under development by Roche for the treatment of cognitive impairment associated with Down syndrome.

BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.

beta-secretase inhibitor.

BI 409306 is an inhibitor of phosphodisterase 9A（PDE9A）.

BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH) with IC50 values of 50 to 70mg/kg in various rat brain regions.

Bitopertin, also known as RG1678, is a potent and selective inhibitor of GlyT1 with an EC50 of 30nM.

BMS-708163 is a potent, selective γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, respectively.

BP897 is a partially selective D3 dopamine receptor agonist.

branopadol(GRT-6005) is a novel first in class compounds with potent agonist activity on ORL-1 (opioid receptor like -1) and the well established mu opioid receptor.

Bryostatin 1 (NSC 339555) is a macrocyclic lactone derived from a marine invertebrate, fuctions as an activator of PKC with high binding affinity (Ki=1.35 nM).