Lomitapide
Lomitapide is a potent microsomal triglyceride transfer protein (MTP) inhibitor, used in the treatment of familial hypercholesterolemia.
Showing 1265–1280 of 5738 results
Cerdulatinib (PRT062070, PRT2070)
Cerdulatinib (PRT-062070) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.
Lomitapide Mesylate
Lomitapide Mesylate is a potent microsomal triglyceride transfer protein (MTP) inhibitor, used in the treatment of familial hypercholesterolemia.
TH588
TH588 is a potent and selective MTH1 (NUDT1) inhibitor with IC50 of 5 nM. It has no relevant inhibition of any of the other tested proteins at 100 μM, although TH588 showed reasonable selectivity when tested on a much larger panel of 87 enzymes, GPCRs, kinases, ion channels and transporters at 10 μM.
TH287
TH287 is a potent and selective MTH1 (NUDT1) inhibitor with IC50 of 0.8 nM.
LDN-214117
LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM.
Niraparib (MK-4827) Tosylate
Niraparib (MK-4827) tosylate is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM.
SD-208
SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII.
PI-3065
PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, >70-fold selectivity over other PI3K family members.
GSK1324726A (I-BET726)
GSK1324726A (I-BET726) is a highly selective inhibitor of BET family proteins with IC50 of 41 nM, 31 nM, and 22 nM for BRD2, BRD3, and BRD4, respectively.
MI-3 (Menin-MLL Inhibitor)
MI-3 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 648 nM.
MI-2 (Menin-MLL Inhibitor)
MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.
Tasquinimod
Tasquinimod is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. Phase 3.
CPI-169
CPI-169 is a potent, and selective EZH2 inhibitor with IC50 of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively.
PX-478 2HCl
PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. Phase 1.
EI1
EI1 is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.