DC7359 |
Asp-3026
Featured
|
ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM. |
|
DC10588 |
ASP-9521
Featured
|
ASP-9521 is a potent, selective and orally available AKR1C3 inhibitor with an IC50 of 11 nM for human AKR1C3. |
|
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. |
|
DC11163 |
AST-3424
Featured
|
AST-3424 (OBI-3424, TH-3424) is a first-in-class, novel prodrug that selectively targets cancers overexpressing the enzyme AKR1C3, OBI-3424 is a highly selective prodrug that is converted by AKR1C3 to a DNA alkylating agent. |
|
DC2015 |
AT-101 (AT101) |
AT-101 is a BH3 mimetic known to be a potent inhibitor of antiapoptotic Bcl-2 family members. |
|
DC7363 |
AT-406
Featured
|
AT-406 (formerly known as SM-406) is an orally bioavailable potent IAP (inhibitor of apoptosis protein) of XIAP, cIAP1, and cIAP2 with Ki of 66.4 nM, 1.9 nM, and 5.1 nM, respectively. |
|
DC9676 |
AT7519
Featured
|
AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM; less potent to CDK3 and little active to CDK7. |
|
DC1025 |
AT7519 HCL
Featured
|
AT7519 is a novel multi-CDK inhibitor for CDK1/cyclin B, CDK2/Cyclin A, CDK3/Cyclin E, CDK4/Cyclin D1, CDK5/p35 and CDK6/Cyclin D3 with IC50 of 210 nM, 47 nM, 360 nM, 100 nM, 13 nM and 170 nM, respectively. |
|
DC9395 |
AT7519 (trifluoroacetate) |
AT7519 trifluoroacetate is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM; less potent to CDK3 and little active to CDK7. |
|
DC7070 |
AT9283
Featured
|
AT9283 is a small molecule a multi-targeted inhibitor with of 4, 1.2, 1.1 and approximate 3 nM for Bcr-Abl(T3151), Jak2 and Jak3, aurora A and B, respectively. |
|
DC5202 |
Luminespib (NVP-AUY922)
Featured
|
AUY922 (NVP-AUY922) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Phase 1/2. |
|
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. |
|
DC10009 |
Avitinib free base
Featured
|
Avitinib is an orally available, irreversible, epidermal growth factor receptor (EGFR) mutant-selective inhibitor, with potential antineoplastic activity. |
|
DC10008 |
Avitinib maleate
Featured
|
Avitinib is an orally available, irreversible, epidermal growth factor receptor (EGFR) mutant-selective inhibitor, with potential antineoplastic activity. |
|
DC7367 |
AZ-960
Featured
|
AZ 960 is a novel ATP competitive JAK2 inhibitor with IC50 and Ki of <3 nM and 0.45 nM, 3-fold selectivity of AZ960 for JAK2 over JAK3. |
|
DC9309 |
AZD-0156
Featured
|
AZD-0156 is an orally bioavailable ataxia telangiectasia mutated (ATM) kinase inhibitor, with potential chemo-/radio-sensitizing and antineoplastic activities. |
|
DC7060 |
AZD1152
Featured
|
AZD1152 (barasertib), pro-drug of barasertib-hQPA, is a selective Aurora B kinase inhibitor, AZD1152 inhibited the proliferation various types of human leukemia cells with an IC50 ranging from 3 nM to 40 nM. |
|
DC5032 |
AZD1480
Featured
|
AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1/2. |
|
DC8472 |
AZD-3759
Featured
|
AZD3759 is an orally available inhibitor of the epidermal growth factor receptor (EGFR), with potential antineoplastic activity. |
|
DC9263 |
AZD-3965
Featured
|
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. |
|
DC1075 |
AZD4547
Featured
|
AZD4547 is a novel selective FGFR inhibitor targeting FGFR1, FGFR2, and FGFR3 with IC50 of of 0.2 nM, 2.5 nM, and 1.8 nM, respectively. |
|
DC11295 |
AZD-4573 |
AZD4573 is a CDK9 inhibitor with an IC50 of <3 nM extracted from patent US 20160376287 A1, example 14. |
|
DC10739 |
AZD4635
Featured
|
AZD4635 is a novel adenosine 2A receptor (A2AR) inhibitor with a Ki of 1.7 nM. |
|
DC10773 |
AZD5069
Featured
|
AZD-5069 is a potent and selective CXCR2 antagonist with the potential to inhibit neutrophil migration into the airways in patients with COPD. |
|
DC10774 |
AZD5153
Featured
|
AZD5153 is a potent bivalent triazolopyridazine based Bromodomain and Extraterminal (BET) Inhibitor. |
|
DC7369 |
AZD5438
Featured
|
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. |
|
DC1069 |
AZD6244 (Selumetinib,ARRY-142886)
Featured
|
AZD6244 (Selumetinib, ARRY-142886) is highly potent to inhibit MEK1 with IC50 of 14 nM. |
|
DC8468 |
AZD-6738
Featured
|
AZD6738 is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2. |
|
DC7076 |
AZD-7762
Featured
|
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. |
|
DC5084 |
AZD-8055
Featured
|
AZD-8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM. |
|