-
glutamate receptors agonist
(S)-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). -
EGFR inhibitor
AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively. -
serotonin (5-HT)/norepinephrine (NE) reuptake inhibitor
Desvenlafaxine succinate hydrate is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI). -
5-HT3 receptor antagonist
Ricasetron is a drug which acts as a selective antagonist at the serotonin 5-HT3 receptor. -
5HT3 receptor antagonist
Lerisetron is a serotonin type 3 (5-HT3) receptor antagonist with antiemetic activity. -
5-HT3 receptor inhibitor
Eucalyptol is a bicyclic monoterpene that has been found in Eucalyptus and other plants. It is an inhibitor of 5-HT3 receptor ,potassium channel, TNF-α and IL-1β. - Buclizine HCl is an antihistamine and anticholinergic of the piperazine derivative family.
-
5HT(1A) receptor agonist
Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders. -
CRTH2 antagonist
ACT-129968 is a potent and selective CRTH2 antagonist. -
mGlu2 receptor modulator
CBiPES hydrochloride is a selective positive allosteric modulator of the mGluR-2 with IC50 value of 98.2 nM -
S1PR1 modulators
RPC1063 is a selective sphingosine 1 phosphate receptor modulators and methods which may be useful in the treatment of S1P1-?associated diseases.- Alessia Favaron, .et al. , Eur J Pharm Sci, 2024, Sep 1:200:106845 PMID: 38971433
-
EGFR inhibitor
Olafertinib (CK-101, RX518) is an epidermal growth factor receptor (EGFR) inhibitor.
-
EP2 Agonist
C-544326 is a potent and selective prostaglandin E2 receptor agonist with EC50 value of 2.8 nM. -
β2 adrenergic receptor antagonist
ICI-118551 is a selective beta2 adrenergic receptor (adrenoreceptor) antagonist.- Moon Jain, .et al. , Tropical Journal of Pharmaceutical Research, 2020, Vol. 19 No. 4
-
Serotonin2A Receptor Inverse Agonist
Pimavanserin is a potent and selective serotonin 5-HT2A inverse agonist with pIC50 of 8.73, used to treat psychosis associated with Parkinson?€?s disease. -
sGC activator?€?
BAY 41-2272 is a direct and NO-independent soluble guanylate cyclase (sGC) stimulator. -
5HT(1A) receptor agonist
Eptapirone is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential. -
prostaglandin EP4 receptor antagonist
Grapiprant is a novel, potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties. -
Opioid antagonist
Naloxegol is a peripherally-selective opioid antagonist for the treatment of opioid-induced constipation. -
Orexin 2 receptor agonist
A potent and selective Orexin2 receptor agonist. -
CysLT1 receptor antagonist
MK-571 is a selective, orally active CysLT1 receptor antagonist. It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively. -
CCK-2 receptor antagonist
Nastorazepide is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity. -
β2-adrenergic receptor agonist
Vilanterol is a long-acting beta-2 agonist drug, which in May 2013 was approved in combination with fluticasone furoate for sale as Breo Ellipta by GlaxoSmithKline for the treatment of chronic obstructive pulmonary disease (COPD). - cAMPS-Sp, triethylammonium salt is a cell-permeable cAMP analog that activates cAMP receptor proteins such as PKA and cAMP-regulated guanine nucleotide exchange factor.
-
dopaminergic stabilizer
ACR 16 hydrochloride is a dopaminergic stabilizer (Ki values 17550 nM and 7521 for D2(low) and D2(high), respectively) that state-dependently stabilizes psychomotor activity by the dual actions of functional dopamine D2 receptor antagonism and strengthening of cortical glutamate functions in various settings of perturbed neurotransmission. -
dopamine D2 receptor agonist
UNC 9994 hydrochloride, unique, beta-arrestin-biased functionally selective dopamine D2 receptor (D2R) agonist (Ki value 30 nM; EC50 value 50 nM in ??-arrestin-2 recruitment assay) that exhibits antipsychotic activity in vivo. UNC9994 markedly inhibited PCP-induced hyperlocomotion in wild-type mice, which effect was completely abolished in ??-arrestin-2 knockout mice.- Anika Mann, .et al. , Sci Rep, 2021, Apr 15;11(1):8288 PMID: 33859231
-
Adenosine A Receptor agonist
2-Chloroadenosine is a metabolically stable analog of adenosine that behaves as an Adenosine A Receptor agonist (Ki values are 300, 80 and 1900 nM for Adenosine A1-R, Adenosine A2A-R and Adenosine A3-R, respectively). -
mGluR agonist
(S)-3,5-DHPG is an agonist of the group I metabotropic glutamate receptors (mGluRs), binding both mGluR1a and mGluR5a (Ki = 0.9 and 3.9 uM, respectively) but not ionotropic glutamate receptors. -
GLP-1 receptor agonist
Liraglutide is a long-acting glucagon-like peptide-1(GLP-1) receptor agonist. -
adenylyl cyclase inhibitor
SQ22536 is an inhibitor of adenylyl cyclase with an IC50 of 1.4 uM. It can inhibit PGE1-stimulated increases in cAMP levels in intact human platelets.- Ke Qian, .et al. , EBioMedicine, 2023, Dec:98:104863 PMID: 37950995
-
histamine-H1 receptor blocking agent
Carbinoxamine maleate is a histamine-H1 receptor blocking agent with antihistamine and anticholinergic properties.

