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SEW2871 is a potent and selective sphingosine-1-phosphate 1 (S1P1) receptor agonist. Activates S1P1 receptor with an EC50 of 13 nM, but does not activate S1P2, S1P3, S1P4 or S1P5 receptors at concentrations up to 10 μM. Cell-permeable and active in vivo.
VX-765 is a potent and selective inhibitor of caspase-1 with Ki of 0.8 nM in a cell-free assay.
WZ811 is a small molecular and potency CXCR4 antagonist with EC50 of 0.3 nM.
AT9283 is a multi-targeted inhibitor with IC50s of 4, 1.2, 1.1 and approximate 3 nM for Bcr-Abl (T315I), JAK2 and JAK3, Aurora A and Aurora B, respectively.
AZ3451 is a protease-activated receptor-2 (PAR2) antagonist.
AZD1480 is a selective ATP-competitive JAK1/2 inhibitor with IC50 value of 1.3 and <0.4 nM, respectively, as well as shows inhibitory effect on JAK3 and Tyk2.
AZD3264 is an IkB-kinase IKK2 Inhibitor. IKK2 has been identified as one of the pathways to treat inflammatory conditions such as asthma, chronic pulmonary obstructive disorder (COPD) and rheumatoid arthritis.
BGJ-398 is a selective, pan-specific FGFR inhibitor with IC50 of 0.9, 1.4, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively and > 40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes.
BIBF0775 is an inhibitor of transforming growth factor β receptor I (TGFβRI) by soaking into the kinase domain of TGFβRI.
BLZ945 is a highly selective and brain-penetrant inhibitor of CSF1R with IC50 of 1 nM and > 3200-fold higher than its affinity for other kinases.
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