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DOPA decarboxylase inhibitor
Methyldopa Sesquihydrate is a DOPA decarboxylase inhibitor and indirect α2-adrenergic receptor agonist used to treat hypertension. -
alpha-1 adrenergic receptors / mAChRs inhibitor
Anisodamine is an inhibitor of alpha-1 adrenergic receptors and mAChRs isolated from Chinese solanacea plant. -
EGFR inhibitor
Olafertinib (CK-101, RX518) is an epidermal growth factor receptor (EGFR) inhibitor.
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5-HT1A receptor agonist/serotonin reuptake inhibitor
YL0919, a novel antidepressant candidate with dual activity as a 5-HT1A receptor agonist and a selective serotonin reuptake inhibitor,the IC50 values of YL-0919 inhibiting the uptake of 5-HT into rat cerebral cortical synaptosomes and human recombinant cells were 1.78??0.34 nM and 1.93??0.18 nM respectively. -
Histamine H1 receptor inhibitor
Antazoline HCl is a first generation antihistamine, binding to the histamine H1 receptor and blocking the action of endogenous histamine. -
Histamine/cholinergic inhibitor
Azatadine is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively. -
5-HT1A receptor antagonist/COMT inhibitor
Flopropione is a 5-HT1A receptor antagonist and also a catechol-o-methyltransferase (COMT) inhibitor. -
thromboxane synthesis inhibitor
Ro-24-0238 is an antagonist of platelet activating factor (PAF) and inhibitor of thromboxane synthesis, used for lessening the inflammation and damage resulting from a local release of PAF. -
GRK2 inhibitor
GSK180736A is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM. -
leukotriene A4 hydrolase inhibitor
Acebilustat (CTX-4430) is a leukotriene A4 hydrolase inhibitor, used for an oral antiinflammatory drug. -
monoamine reuptake inhibitor
Diclofensine hydrochloride (Ro-8-4650 hydrochloride) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively. -
dual NE/DA transporter inhibitor
Centanafadine is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively. -
5-HT1A/5-HT1B/5-HT3A/5-HT7 receptor/SERT inhibitor
Vortioxetine is a inhibitor of 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT, with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively. -
DP1 inhibitor
Laropiprant is used in combination with niacin to reduce blood cholesterol. Laropiprant acts as a DP1 antagonist, reducing the vasodilation. -
serotonin transporter (SER) inhibitor
Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist. -
Thromboxane A2 synthesis inhibitor
Ozagrel is an antiplatelet agent working as a thromboxane A2 synthesis inhibitor. -
PGF2α/LTB4 production inhibitor
Darbufelone mesylate (CI-1004 mesylate) is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50 = 0.19 μM) but is much less potent with PGHS-1 (IC50= 20 μM). -
COX inhibitor/histamine H1 receptor agonist
Fexofenadine HCl is an antihistamine that inhibits Cox-1, Cox-2, and is a histamine H1 receptor agonist -
GPR40 Inhibitor
GW 9508 is a cell-permeable aminophenylpropanoate that acts as a potent and selective agonist for the G-protein coupled receptor (GPCR) GRP40/FFA1 receptor (EC50 ?50 nM) with reduced activity towards family members GRP120 (EC50 ?3.5 μM), GRP41/GRP43 (EC50 >50 μM), as well as a panel of eight other free fatty acid (FFA) and prostaglandin receptors. -
lysophaphatidic acid 1 (LPA1/Edg-2) receptor inhibitor
SAR-100842 is a lysophaphatidic acid 1 (LPA1/Edg-2) receptor inhibitor. -
5-Lipoxygenase (5-LO) inhibitor
Atreleuton (ABT-761) is a selective, reversible, and orally bioavailable 5-Lipoxygenase (5-LO) inhibitor. Atreleuton (ABT-761) exhibits potent and selective inhibition of leukotriene formation. -
triple reuptake inhibitor/5-HT2A/5-HT2C/5-HT3/α1A-adrenergic receptor antagonis
Tedatioxetine hydrobromide acts as a triple reuptake inhibitor and 5-HT2A, 5-HT2C, 5-HT3 and α1A-adrenergic receptor antagonist. -
adrenergic receptor/5-HT receptor inhibitor
Asenapine hydrochloride inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM. -
Dopamine reuptake inhibitor
Phenylpiracetam is a phenylated derivative of the nootropic drug piracetam. It is used as a stimulant nootropic drug that can be up to 30-60 times more potent than piracetam. -
CXCL8 receptor inhibitor
Reparixin L-lysine salt is an inhibitor of CXCL8 receptor, also inhibit CXCR1 and CXCR2 activation,which has been shown to attenuate inflammatory responses in various injury models. -
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 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.

