Showing 1905–1920 of 7558 results

ML323

ML323 displays reversible, nanomolar inhibitory activity and excellent selectivity toward USP1/UAF1 with IC50 of 76 nM.

GNE-7915

GNE-7915 is a highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) inhibitor, with IC50 and Ki of 9 nM and 1 nM, respectively.

GNF-5

GNF-5 is a selective and allosteric Bcr-Abl inhibitor with IC50 of 220 nM.

XMD8-92

XMD8-92 is a potent and selective BMK1/ERK5 inhibitor with Kd of 80 nM.

FR 180204

FR 180204 is an ATP-competitive, selective ERK inhibitor with Ki of 0.31 μM and 0.14 μM for ERK1 And ERK2, respectively. It is 30-fold less potent against the related kinase p38α and failed to inhibit any kinases(MEK1, MKK4, IKKα, PKCα, Src, Syc, and PDGFα) at less than 30 μM.

Entospletinib (GS-9973)

Entospletinib (GS-9973) is an orally bioavailable, selective Syk inhibitor with IC50 of 7.7 nM in a cell-free assay and showed 13- to >1000-fold cellular selectivity for Syk over other kinases(including Jak2, ckit, Flt3, Ret, KDR) as assessed by target protein phosphorylation or functional response.

Afuresertib (GSK2110183)

Afuresertib (GSK2110183) is a potent, orally bioavailable Akt inhibitor with Ki of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2.

Darapladib (SB-480848)

Darapladib (SB-480848) is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.25 nM. Phase 3.

GNF-5837

GNF-5837 is a selective, and orally bioavailable pan-TRK inhibitor for TrkA, and TrkB with IC50 of 8 nM, and 12 nM, respectively.

AZD7545

AZD7545 is a potent PDHK inhibitor with IC50 of 36.8 nM and 6.4 nM for PDHK1 and PDHK2, respectively. It failed to inhibit PDHK4 at higher concentrations(>10 nM), AZD7545 stimulates PDHK4 activity.

Y-320

Y-320 is an orally active immunomodulator, and inhibits IL-17 production by CD4 T cells stimulated with IL-15 with IC50 of 20 to 60 nM.

VGX-1027

VGX-1027 is an orally active immunomodulator. Phase 1.

Trelagliptin

Trelagliptin is a highly selective, long-acting DPP-4 inhibitor. Phase 3.

LY2857785

LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9(IC50=0.011 μM) and also inhibits other transcription kinases CDK8(IC50=0.016 μM) and CDK7 (IC50=0.246 μM).

ML167

ML167 is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor with IC50 of 136 nM, >10-fold selectivity for closely related kinases Clk1-3 and Dyrk1A/1B.