Chk2 inhibitor II [Ligand Id: 5954] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL179583
  • checkpoint kinase 2/Serine/threonine-protein kinase Chk2 in Human [ChEMBL: CHEMBL2527] [GtoPdb: 1988] [UniProtKB: O96017]
1 CHEMBL179583_lig_chart_1 Serine/threonine-protein kinase Chk2 Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
checkpoint kinase 2/Serine/threonine-protein kinase Chk2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2527] [GtoPdb: 1988] [UniProtKB: O96017]
GtoPdb - - 7.43 pKi 37 nM Ki Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-8 [PMID:18077363]
ChEMBL Inhibition of Chk2 B 7.43 pKi 37 nM Ki Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of recombinant human Chk2 kinase B 7.8 pIC50 16 nM IC50 J. Med. Chem. (2005) 48: 1873-1885 [PMID:15771432]
ChEMBL Inhibition of chk2 kinase B 7.8 pIC50 16 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 1924-1928 [PMID:16442290]
ChEMBL Inhibition of recombinant human CDS1 using N-terminal biotin-labeled SGLYRSPSMPENLNRPR as substrate in presence of [gamma-33P]-ADP after 3 hrs by scintillation counting method B 7.8 pIC50 16 nM IC50 EP-1435947-B1. 2-phenyl benzimidazoles and imidazo-4,5|-pyridines as CDS1/CHK2-inhibitors and adjuvants to chemotherapy or radiation therapy in the treatment of cancer (2007)
ChEMBL Inhibition of recombinant human Chk2 kinase B 7.82 pIC50 15 nM IC50 J. Med. Chem. (2005) 48: 1873-1885 [PMID:15771432]
ChEMBL Inhibition of human recombinant Chk2 B 7.82 pIC50 15 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 6467-6471 [PMID:17937984]
ChEMBL Inhibition of Chk2 B 7.82 pIC50 15 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]