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ML348 is a selective and reversible lysophospholipase 1 (LYPLA1) inhibitor (IC50 = 210 nM), Exhibits 14-fold selectivity for LYPLA1 over LYPLA2, Also selective over a panel of ~30 other serine hydrolases.
ML348 is a selective and reversible lysophospholipase 1 (LYPLA1) inhibitor (IC50 = 210 nM), Exhibits 14-fold selectivity for LYPLA1 over LYPLA2, Also selective over a panel of ~30 other serine hydrolases.
LYPLA1 Over-expression Lysate Product
PI4KIIIbeta-IN-9 is a potent PI4KIIIβ inhibitor (IC50 of 7 nM) and is >140-fold selective over PI3Kγ and >20-fold selective over PI3Kδ, and shows no inhibition of vps34 at concentrations up to 20 μM.
JWH 133 is a potent CB2 selective agonist with Ki of 3.4 nM, 200-fold selective over CB1 receptors.
UK-383367 (UK 383367) is a potent and selective inhibitor of BMP-1 (procollagen C-proteinase) with IC50 of 44 nM; Selective for BMP-1 over MMPs 1, 2, 3, 9 and 14 (IC50 values are >10,000 nM for listed MMPs).
SCIO-469 is a selective ATP-competitive p38 inhibitor with IC50 of 9 nM for p38αin vitro, about 10-fold selectivity for p38α over p38β, and at least 2000-fold selectivity for p38α over an in vitro panel of 20 other kinases, including other MAK kinases.
EPZ011989 trifluoroacetate is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.
EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.
AZD3839 (free base) is a potent and selective BACE1 inhibitor with IC50 of 23.6 uM, about 14-fold selectivity over BACE2, also a β-secretase enzyme inhibitor.
Tandospirone citrate is a potent and selective 5-HT1A receptor partial agonist (Ki = 27 nM) that displays selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Ki values ranging from 1300-41000 nM).
PF-2545920 is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, with >1000-fold selectivity over the PDE.
RQ-00203078 is a highly selective, potent and orally available TRPM8 antagonist (IC50 values are 5.3 and 8.3 nM for rat and human channels respectively), exhibits >350-fold selectivity for TRPM8 over TRPV4, TRPV1 and TRPA1.
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