compound 31 [PMID: 22902653] [Ligand Id: 8117] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2070615
  • testis associated actin remodelling kinase 1/Dual specificity testis-specific protein kinase 1 in Human [ChEMBL: CHEMBL5604] [GtoPdb: 2239] [UniProtKB: Q15569]
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  • testis associated actin remodelling kinase 2/Dual specificity testis-specific protein kinase 2 in Human [ChEMBL: CHEMBL2069163] [GtoPdb: 2240] [UniProtKB: Q96S53]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
testis associated actin remodelling kinase 1/Dual specificity testis-specific protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5604] [GtoPdb: 2239] [UniProtKB: Q15569]
GtoPdb - - 6.34 pIC50 455 nM IC50 Bioorg Med Chem Lett (2012) 22: 5995-8 [PMID:22902653]
ChEMBL Inhibition of TESK1 B 6.34 pIC50 455 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 5995-5998 [PMID:22902653]
testis associated actin remodelling kinase 2/Dual specificity testis-specific protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069163] [GtoPdb: 2240] [UniProtKB: Q96S53]
ChEMBL Inhibition of TESK2 B 6.6 pIC50 252 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 5995-5998 [PMID:22902653]
GtoPdb - - 6.6 pIC50 252 nM IC50 Bioorg Med Chem Lett (2012) 22: 5995-8 [PMID:22902653]
LIM domain kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3836] [GtoPdb: 2054] [UniProtKB: P53667]
ChEMBL Inhibition of LIMK1 B 7.24 pIC50 58 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 5995-5998 [PMID:22902653]
GtoPdb - - 7.24 pIC50 58 nM IC50 Bioorg Med Chem Lett (2012) 22: 5995-8 [PMID:22902653]
ChEMBL Inhibition of LIMK1 (unknown origin) assessed as ADP formation using cofilin-2 protein as substrate measured after 60 mins incubation with enzyme by Transcreener assay B 7.27 pIC50 54 nM IC50 MedChemComm (2011) 2: 982-986
ChEMBL Inhibition of LIMK1-catalyzed cofilin phosphorylation in human ZR-75-1 cells B 9 pIC50 1 nM IC50 MedChemComm (2011) 2: 982-986
LIM domain kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5932] [GtoPdb: 2055] [UniProtKB: P53671]
ChEMBL Inhibition of LIMK2 (unknown origin) B 6.16 pIC50 696 nM IC50 MedChemComm (2011) 2: 982-986
GtoPdb - - 7.42 pIC50 38 nM IC50 Bioorg Med Chem Lett (2012) 22: 5995-8 [PMID:22902653]
ChEMBL Inhibition of LIMK2 B 7.42 pIC50 38 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 5995-5998 [PMID:22902653]

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]