rabusertib [Ligand Id: 7960] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3039517 (LY-2603618, Ly-2603618, IC-83, LY2603618, Rabusertib)
  • Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
  • This target only has 0 pki data point
  • 0
1 CHEMBL3039517_lig_chart_1 HERG Human
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  • checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
  • This target only has 0 pki data point
  • 0
2 CHEMBL3039517_lig_chart_2 Serine/threonine-protein kinase Chk1 Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG expressed in CHO cells at -80 mV holding potential by automated patch clamp assay B 4.55 pIC50 28100 nM IC50 Eur J Med Chem (2019) 173: 44-62 [PMID:30986571]
checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged CHK1 (M1 to T476 residues) expressed in baculovirus infected insect cells using biotin-labelled STK substrate-1 as substrate incubated for 60 mins by HTRF assay B 7.98 pIC50 10.4 nM IC50 Eur J Med Chem (2019) 173: 44-62 [PMID:30986571]
GtoPdb - - 8.15 pIC50 7 nM IC50 Invest New Drugs (2014) 32: 213-26 [PMID:24114124]

ChEMBL data shown on this page come from version 28:

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]