Showing 4833–4848 of 5738 results

Bazedoxifene Acetate

Bazedoxifene Acetate is a third generation selective estrogen receptor modulator (SERM).

PF-4708671

PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) with Ki/IC50 of 20 nM/160 nM in cell-free assays, 400-fold greater selectivity for S6K1 than S6K2, and 4- and >20-fold selectivity for S6K1 than MSK1 and RSK1/2, respectively. First S6K1-specific inhibitor to be reported.

AZD1480

AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM in a cell-free assay, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1.

RAF265 (CHIR-265)

RAF265 (CHIR-265) is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM in cell-free assays. Phase 2.

Almorexant HCl

Almorexant HCl is an orally active, dual orexin receptor antagonist with IC50 of 6.6 nM and 3.4 nM for OX1 and OX2 receptor, respectively. Phase 3.

Tebipenem Pivoxil

Tebipenem pivoxil is an oral carbapenem antibiotic, use to treat otolaryngologic and respiratory infections.

KW-2449

KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 with IC50 of 6.6 nM, modestly potent to FGFR1, Bcr-Abl and Aurora A little effect on PDGFRβ, IGF-1R, EGFR. Phase 1.

Taladegib (LY2940680)

Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.

LY2886721

LY2886721 is a BACE inhibitor used for the treatment of Alzheimer’s Disease. Phase 1/2.

LY2608204

LY2608204 activates glucokinase (GK) with EC50 of 42 nM. Phase 2.

Dabigatran Etexilate

Dabigatran Etexilate is the prodrug of dabigatran, a potent, nonpeptidic small molecule that specifically and reversibly inhibits both free and clot-bound thrombin by binding to the active site of the thrombin molecule.

CGS 21680 HCl

CGS 21680 HCl is an adenosine A2 receptor agonist with IC50 of 22 nM, exhibits 140-fold over A1 receptor.

Sitafloxacin Hydrate

Sitafloxacin Hydrate is a new-generation, broad-spectrum oral fluoroquinolone antibiotic.

Sonidegib (Erismodegib, NVP-LDE225)

Sonidegib (Erismodegib, NVP-LDE225) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human) in cell-free assays, respectively. Phase 3.

Neratinib (HKI-272)

Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3.

GSK1292263

GSK1292263 is a novel GPR119 agonist, showing potential for the treatment of type 2 diabetes. Phase 2.