Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity.

M3541 (M 3541) is a novel potent, selective and ATP-competitive ATM kinase inhibitor with IC50 of 0.25 nM (ATP, 10 uM).M3541 displays a good margin of selectivity (>60-fold) against the closely related PIKK family members with DNA-PK, PI3K isoforms, mTOR, and ATR.M3541 inhibits the phosphorylation of ATM as well as its cellular substrates CHK2, KAP1, and p53 in a concentration-dependent manner in A549 cells.M3541 inhibits double strand break repair and sensitizes cancer cells to radiation.M3541 suppresses ATM pathway activity and potentiates radiation efficacy in xenograft models of human cancer, synergizes with topoisomerase and PARP inhibitors.

ART0380 (ART-0380) is a potent, selective and ATP-competitive ATR kinase inhibitor, inhibits ATR-ATRIP complex enzyme activity with IC50 of 51.7 nM, and phospho-Chk1 IC50 of 22 nM in cell western assay.

KU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM.

GJ103 sodium salt is an active analog of the read-through compound GJ072.

ATR inhibitor 4 (compound 121) is a potent ATR inhibitor. ATR inhibitor 4 has antitumor activity.

VE-821 is a potent and selective ATP competitive inhibitor of ATR with Ki and IC50 of 13 nM and 26 nM, respectively.

KU-55933 is a potent and specific ATM inhibitor with IC50 and Ki of 13 nM and 2.2 nM, respectively.

CP-466722 is an potent and reversible ATM inhibitor.

BAY-1895344 is a potent and selective ATM inhibitor. BAY 1895344 shows potent anti-tumor efficacy in monotherapy and strong combination potential with the targeted alpha therapy Radium-223 dichloride.

AZD6738 is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.

RP-3500 (Camonsertib, ATR inhibitor) is a highly potent and selective inhibitor of ATR kinase with an IC50 of 1 nM.

M4076 is a higly potent, selective, ATP-competitive inhibitor of ATM kinase with IC50 of 0.2 nM.M4076 sensitizes tumor cell lines to radiation therapy in vitro and strongly enhances the anti-tumor activity of ionizing radiation in vivo.

ATR-IN-12 (Compound 5g) is a potent inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase with an IC50 value of 0.007 μM. ATR-IN-12 displays good anti-tumor activity and significantly reduces the phosphorylation level of ATR and its downstream signaling protein. ATR-IN-12 is a promising lead compound for subsequent drug discovery targeting ATR kinase.

ATR-IN-11 (Compound Hit01) is a potent inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase. ATR kinase is a key regulating protein within the DNA damage response (DDR), responsible for sensing replication stress (RS). ATR-IN-11 is a promising lead compound for subsequent drug discovery targeting ATR kinase. ATR-IN-11 has the potential for the research of cancer disease.

ATR-IN-6 is a potent inhibitor of ATR. ATR is a class of protein kinases involved in genome stability and DNA damage repair, and is a member of the PIKK family. ATR-IN-6 has the potential for the research of ATR kinase-mediated diseases such as proliferative diseases and cancer (extracted from patent WO2021233376A1, compound A22).

ATR-IN-5 is a potent inhibitor of ATR. ATR is a class of protein kinases involved in genome stability and DNA damage repair, and is a member of the PIKK family. ATR-IN-5 has the potential for the research of ATR kinase-mediated diseases such as proliferative diseases and cancer (extracted from patent CN112047938A, compound D24).

ATR-IN-10 is a potent and highly selective inhibitor of ataxia telangiectasia mutated and Rad3-Related (ATR) kinase with an IC50 value of 2.978 μM.

SKLB-197 showed an IC50 value of 0.013 μM against ATR but very weak or no activity against other 402 protein kinases. It displayed potent antitumor activity against ATM-deficent tumors both in vitro and in vivo.

ATR-IN-7 is a potent inhibitor of ATR. ATR is a class of protein kinases involved in genome stability and DNA damage repair, and is a member of the PIKK family. ATR-IN-7 has the potential for the research of ATR kinase-mediated diseases such as proliferative diseases and cancer (extracted from patent WO2021238999A1, compound 1).

AZD-0156 is an orally bioavailable ataxia telangiectasia mutated (ATM) kinase inhibitor, with potential chemo-/radio-sensitizing and antineoplastic activities.

AZ31 is a novel ATM inhibitor.

ATR-IN-4 is a potent ATR (Ataxia telangiectasia mutated gene Rad 3-associated kinase) inhibitor. ATR-IN-4 inhibits growth of human prostate cancer cells DU145 and human lung cancer cells NCI-H460 with IC50s of 130.9 nM and 41 .33 nM, respectively. (Patent CN112142744A, compound 13).

AZ32 is an orally bioavailable and blood-brain-barrier penetrating ATM inhibitor (AZ32) that radiosensitizes intracranial gliomas in mice.