A marine sponge alkaloid that inhibits Chk1 and Chk2 with IC50 of 3 and 3.5 uM, respectively.

A novel potent, selective CHK1 inhibitor 2 nM, >80-fold selectivity over CHK2.

A potent and highly selective Chk2 inhibitor with IC50 of 0.14 nM.

A potent and selective Chk2 inhibitor with Ki/IC50 of 11 nM/120 nM.

A potent, ATP-competitive and highly selective Chk2 inhibitor with IC50 of 138 nM.

A potent, reasonably selective Chk1 inhibitor with cell IC50 of 5 nM.

A potent, selective and orally active Chk1 inhibitor.

A potent, selective, ATP-competitive Chk1 and Chk2 inhibitor with IC50 of 4.4 nM and 4.5 nM, respectively.

A potent, selective, ATP-competitive Chk1 inhibitor with IC50 of 13.3 nM.

A potent, selective, reversible, ATP-competitive Chk2 inhibitor with IC50 of 0.2 uM.

A potent, specific, orally available, ATP‑competitive inhibitor of Chk1 and Chk2 with Ki of 2.2 nM and 0.07 nM, respectively.

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.

CCT241533 Hcl is a potent serine/threonine checkpoint kinase (Chk2) inhibitor with IC50 of 3 nM; shows minimal cross-reactivity against a panel of kinases at 1 uM.

CCT244747 represents the first structural disclosure of a highly selective, orally active CHK1 inhibitor and warrants further evaluation alone or combined with genotoxic anticancer therapies.

GDC0575（ARRY-575，RG7441）is a small molecule inhibitor of cell cycle checkpoint kinase 1 (Chk1), with potential chemosensitization activity.

GNE-900 (GNE900) is a potent, selective, ATP-competitive, and orally bioavailable Chk1 inhibitor with IC50 of <1 nM.

LY2603618(IC-83) is a potent and selective small molecule inhibitor of Chk1 protein kinase activity in vitro (IC50=7 nM) and the first selective Chk1 inhibitor to enter clinical cancer trials.

LY2606368 2Hcl is a potent and selective ATP competitive inhibitor(IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.

LY2606368 is a potent and selective ATP competitive inhibitor(IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.

PF 477736 is a CHK inhitor with Ki values of 0.49 and 47 nM for Chk1 and Chk2 respectively. A proprietary compound targeting cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiation activity

SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC(50) of 13.3 nmol/L on the isolated human enzyme.

SB218078 is an inhibitor of checkpoint kinase 1 (Chk1) that displays selectivity over other protein kinases (IC50 values are 15, 250 and 1000 nM for Chk1, cdc2 and PKC respectively).

SCH 900776 is a selective Chk1 inhibitor with IC50 of 3 nM. It shows 50-fold selectivity against Chk2. Phase 2.

Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model.

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib Mesylate Hydrate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib Mesylate Hydrate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib Mesylate Hydrate shows potent anti-tumor activity.

Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity.

Chk1-IN-6 is a potent, selective, and orally bioavailable CHK1 inhibitor candidate.

LY2880070 is an orally active inhibitor of CHK1. LY2880070 can be used as an anticancer agent and shows promise in preclinical models of pancreatic ductal adenocarcinoma (PDAC) when used in combination with DNA-damaging agents.