Showing 4945–4960 of 7522 results

CH5132799

CH5132799 inhibits class I PI3Ks, particularly PI3Kα with IC50 of 14 nM less potent to PI3Kβδγ, while sensitive in PIK3CA mutations cell lines. Phase 1.

RS-127445

RS-127445 is a selective 5-HT2B receptor antagonist with pKi of 9.5 and pIC50 of 10.4, exhibits >1000-fold selectivity against other 5-HT receptors.

A-769662

A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM in cell-free assays, little effect on GPPase/FBPase activity.

Apitolisib (GDC-0980, RG7422)

Apitolisib (GDC-0980, RG7422) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively. Also a mTOR inhibitor with Ki of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases. Phase 2.

Nepicastat (SYN-117) HCl

Nepicastat (SYN-117) HCl is a potent and selective inhibitor of both bovine and human dopamine-β-hydroxylase with IC50 of 8.5 nM and 9 nM, with negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors. Phase 2.

Turofexorate Isopropyl (XL335)

Turofexorate Isopropyl (XL335) is a potent, selective FXR agonist with EC50 of 4 nM, highly selective versus other nuclear receptors, such as LXR, PPAR, ER and etc. Phase 1.

Resminostat

Resminostat dose-dependently and selectively inhibits HDAC1/3/6 with IC50 of 42.5 nM/50.1 nM/71.8 nM, less potent to HDAC8 with IC50 of 877 nM.

TG101209

TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM in cell-free assays, ~30-fold selective for JAK2 than JAK3, sensitive to JAK2V617F and MPLW515L/K mutations.

BMY 7378 Dihydrochloride

BMY 7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pKi of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pKi of 8.3.

ADX-47273

ADX47273 is a potent and specific mGlu5 positive allosteric modulator(PAM) with EC50 of 0.17 μM, showing no activity at other mGlu subtypes.

WAY-600

WAY-600 is a potent, ATP-competitive and selective inhibitor of mTOR with IC50 of 9 nM blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) but not P-AKT(T308) selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).

R547

R547 is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. Phase 1.

Mardepodect (PF-2545920)

PF-2545920 is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, with >1000-fold selectivity over the PDE.

NVP-BSK805 2HCl

NVP-BSK805 2HCl is a potent and selective ATP-competitive JAK2 inhibitor with IC50 of 0.5 nM,>20-fold selectivity towards JAK1, JAK3 and TYK2.

KW-2478

KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1.

CX-5461

CX-5461 is an inhibitor of rRNA synthesis, selectively inhibits Pol I-driven transcription of rRNA with IC50 of 142 nM in HCT-116, A375, and MIA PaCa-2 cells, has no effect on Pol II, and possesses 250- to 300-fold selectivity for inhibition of rRNA transcription versus DNA replication and protein translation.