Showing 5457–5472 of 5741 results

IC-87114

IC-87114 is a selective PI3Kδ inhibitor with IC50 of 0.5 μM in a cell-free assay, 58-fold more selective for PI3Kδ than PI3Kγ, and over 100-fold more selective than PI3Kα/β.

WYE-354

WYE-354 is a potent, specific and ATP-competitive inhibitor of mTOR with IC50 of 5 nM, blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) not P-AKT(T308), selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).

PD173074

PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM in cell-free assays, ~1000-fold selective for FGFR1 than PDGFR and c-Src.

CHIR-99021 (CT99021)

CHIR-99021 (CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs.

Avagacestat (BMS-708163)

Avagacestat (BMS-708163) is a potent, selective, orally bioavailable γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, demonstrating a 193-fold selectivity against Notch. Phase 2.

Celecoxib

Celecoxib is a selective COX-2 inhibitor with IC50 of 40 nM in Sf9 cells.

Cinacalcet HCl

Cinacalcet HCl represents a new class of compounds for the treatment of hyperparathyroidism.

Ramelteon

Ramelteon is a novel melatonin receptor agonist for human MT1 and MT2 receptors and chick forebrain melatonin receptors with Ki of 14 pM, 112 pM and 23.1 pM, respectively.

Prasugrel

Prasugrel is a thienopyridine ADP receptor (P2Y12) antagonist, used for the reduction of thrombotic cardiovascular events.

Posaconazole

Posaconazole is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes Also an inhibitor of sterol C14ɑ demethylase inhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 15-35 hours.

Rufinamide

Rufinamide is a voltage-gated sodium channel blocker, used an anticonvulsant medication.

Nepafenac

Nepafenac is a prodrug of amfenac that acts as an inhibitor of COX-1 and COX-2 activity, used in the treatment of pain and inflammation associated with cataract surgery.

Entecavir Hydrate

Entecavir, a new deoxyguanine nucleoside analogue, is a selective inhibitor of the replication of the hepatitis B virus (HBV).

Dienogest

Dienogest is an orally active synthetic progesterone, used for contraception and the treatment of endometriosis.

Enzalutamide (MDV3100)

Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.

JNJ-7706621

JNJ-7706621 is pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.