| S9639 |
VX-803 (M4344) |
VX-803 (M4344, ATR inhibitor 2) is an ATP-competitive, orally active, and selective inhibitor of ataxia telangiectasia and Rad3 related (ATR) kinase with Ki of < 150 pM. VX-803 (M4344) potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (P-Chk1) phosphorylation with IC50 of 8 nM. VX-803 (M4344) exhibits potential antineoplastic activity. |
Selective |
ATR, Ki: 150 pM |
| S7693 |
Ceralasertib (AZD6738) |
Ceralasertib (AZD6738) is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.
|
Selective |
ATR, IC50: 1 nM |
| S7050 |
AZ20 |
AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM in a cell-free assay, 8-fold selectivity over mTOR. |
Selective |
ATR, IC50: 5 nM |
| S8666 |
Elimusertib (BAY-1895344) hydrochloride |
Elimusertib (BAY-1895344) hydrochloride is a potent, highly selective and orally available ATR inhibitor with an IC50 of 7 nM. |
Selective |
ATR, IC50: 7 nM |
| S9864 |
Elimusertib (BAY-1895344) |
Elimusertib (BAY-1895344) is a very potent and highly selective ATR (ataxia telangiectasia and Rad3-related) inhibitor with IC50 of 7 nM. Elimusertib potently inhibits proliferation of a broad spectrum of human tumor cell lines with median IC50 of 78 nM. |
Selective |
ATR, IC50: 7 nM |
| S8050 |
ETP-46464 |
ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM. |
Selective |
ATR, IC50: 14 nM |
| S7102 |
Berzosertib (VE-822) |
Berzosertib (VE-822, VX970, M6620) is an ATR inhibitor with IC50 of 19 nM in HT29 cells. |
Selective |
ATR, IC50: 19 nM |
| S1009 |
Dactolisib (BEZ235) |
Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2. |
Selective |
ATR, IC50: 21 nM |
| S8007 |
VE-821 |
VE-821(ATR inhibitor IV) is a potent and selective ATP competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM in cell-free assays, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ. |
Selective |
ATR, Ki: 13 nM |
| S3600 |
Schisandrin B (Sch B) |
Schisandrin B is the most abundant dibenzocyclooctadiene lignan present in the traditional Chinese medicinal herb Schisandra chinensis (Turcz.) Baill. It is a kind of ATR and P-gp inhibitor with high safety. |
Selective |
ATR, IC50: 7.25 μM |
| S0148 |
HAMNO |
HAMNO (NSC-111847) is a potent and selective replication protein A (RPA) inhibitor with anti-tumor activity. HAMNO inhibits both ATR autophosphorylation and phosphorylation of RPA32 Ser33 by ATR. |
Selective |
|
| S2817 |
Torin 2 |
Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively. Torin 2 decreases cell viability and induces autophagy and apoptosis. |
Pan |
ATR, EC50: 35 nM |
| S7136 |
CGK 733 |
CGK 733 is a potent and selective inhibitor of ATM/ATR with IC50 of ~200 nM. |
Pan |
ATR, IC50: 200 nM |
