DC11861 |
TAK-441 |
A highly potent, orally active hedgehog signaling (Hh) inhibitor with IC50 of 4.4 nM in Gli-luc reporter assays. |
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DC11710 |
GDC-0425 |
A potent, selective and orally active Chk1 inhibitor. |
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DC11495 |
Allitinib
Featured
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Allitinib (AST-1306, ALS1306)) is a novel potent, selective irreversible EGFR and HER2 inhibitor with IC50 of 0.5 and 3 nM in cell-free assays. |
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DC8618 |
AMG-319
Featured
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AMG 319 is an investigational, highly selective, small molecule inhibitor of PI3Kδ that blocks B cell proliferation following BCR stimulation both in vitro and in vivo, inhibits basal AKT phosphorylation, and inhibits proliferation in lymphoid tumor cells |
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DC7360 |
AST-1306 |
AST-1306 is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases. |
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DC8253 |
AV-412(MP-412) |
AV-412(MP-412) is a potent dual inhibitor of EGFR and ErbB2(IC50=19 nM) tyrosine kinases, including the mutant EGFR(L858R IC50=0.51 nM, T790M IC50=0.79 nM); inhibits autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively. |
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DC9309 |
AZD-0156
Featured
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AZD-0156 is an orally bioavailable ataxia telangiectasia mutated (ATM) kinase inhibitor, with potential chemo-/radio-sensitizing and antineoplastic activities. |
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DC9263 |
AZD-3965
Featured
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AZD3965 is a selective inhibitor of monocarboxylate transporter 1 (MCT1) with a binding affinity of 1.6 nM, is 6 fold selective over MCT2 and does not inhibit MCT4 at 10 μM. |
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DC7369 |
AZD5438
Featured
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AZD5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 nM/6 nM/20 nM. It is less potent to CDK5/6. |
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DC7076 |
AZD-7762
Featured
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AZD7762 is a potent and selective inhibitor of Chk1 with IC50 of 5 nM; equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck. |
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DC5084 |
AZD-8055
Featured
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AZD-8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM. |
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DC7077 |
AZD8330(ARRY-424704; ARRY-704)
Featured
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AZD8330(ARRY-424704; ARRY-704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. |
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DC9939 |
BAY 1082439 |
BAY 1082439 is a highly selective and balanced PI3Kα/β inhibitor demonstrated potent activity in tumors with activated PI3Kα and loss-of-function of PTEN. |
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DC10408 |
BAY1125976
Featured
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BAY1125976 is a selective allosteric Akt1/2 inhibitor; inhibits Akt1 and Akt2 activity with IC50 values of 5.2 nM and 18 nM at 10 μM ATP, respectively. |
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DC9679 |
BAY1217389
Featured
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BAY1217389 is an orally bioavailable, selective inhibitor of the serine/threonine kinase monopolar spindle 1 (Mps1, TTK), with potential antineoplastic activity. |
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DC8401 |
BI-847325
Featured
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BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1. |
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DC8103 |
BLZ-945
Featured
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BLZ945 is a highly selective and brain-penetrant inhibitor of CSF1R with IC50 of 1 nM; >3200-fold higher than its affinity for other kinases. |
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DC9638 |
BMS-794833 |
BMS-794833 is a potent ATP competitive inhibitor of Met/VEGFR2 with IC50 of 1.7/15 nM; also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378.
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DC10609 |
BMS-986158
Featured
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BMS-986158 is an inhibitor of the bromodomain and extra-terminal (BET) proteins. |
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DC10864 |
C188-9
Featured
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C188-9 is a potent inhibitor of STAT3 that binds to STAT3 with high affinity (KD=4.7±0.4 nM). C188-9 is well tolerated in mice, shows good oral bioavailability, and is concentrated in tumors. |
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DC11709 |
CB-1158 |
CB-1158 (INCB-01158) is a potent, selective, oral available Arginase inhibitor with IC50 of 98 nM. |
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DC8418 |
CH5183284 (Debio-1347)
Featured
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CH5183284 is a selective and orally available FGFR inhibitor with IC50 of 9.3 nM, 7.6 nM, 22 nM, and 290 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. Phase 1. |
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DC7544 |
CUDC-101
Featured
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CUDC-101 is a potent multi-targeted inhibitor against HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, and inhibits class I/II HDACs, but not class III, Sir-type HDACs. Phase 1. |
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DC7810 |
CX-5461
Featured
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CX-5461 is an inhibitor of rRNA synthesis, selectively inhibits Pol I-driven transcription of rRNA, has no effect on Pol II, and possesses 250-to 300-fold selectivity for inhibition of rRNA transcription versus DNA replication and protein translation. |
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DC8404 |
E3330
Featured
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E3330 is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity. |
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DC7128 |
Lucitanib(E3810)
Featured
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E-3810 is a novel dual inhibitor targeting human vascular endothelial growth factor receptors (VEGFRs) and fibroblast growth factor receptors (FGFRs) with antiangiogenic activity. |
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DC10563 |
E-7046
Featured
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E7046 is an orally bioavailable and specific EP4 antagonist, with IC50 of 13.5 nM and Ki of 23.14 nM, exhibiting anti-tumor activities. |
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DC11062 |
E7107 |
E7107 (E-7107) is a derivative of pladienolide that targets the SF3b subunit of the spliceosome, shows significant antitumor activity in vitro and in vivo. |
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DC8489 |
ETC-159
Featured
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ETC-159 is a potent and specific inhibitor of Wnt secretion. ETC-159 inhibits _beta_-catenin reporter activity in a dose-dependent manner with an IC50 of 2.9 nM. |
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DC9515 |
PI3K inhibitor GS1059615 |
GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.
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