MPI-0479605 [Ligand Id: 9399] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2047943
  • TTK protein kinase/Dual specificity protein kinase TTK in Human [ChEMBL: CHEMBL3983] [GtoPdb: 2264] [UniProtKB: P33981]
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  • aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
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  • aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
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  • polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
TTK protein kinase/Dual specificity protein kinase TTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3983] [GtoPdb: 2264] [UniProtKB: P33981]
ChEMBL Inhibition of full-length Mps1 kinase (unknown origin) B 8.3 pIC50 5 nM IC50 Bioorg Med Chem Lett (2013) 23: 6829-6833 [PMID:24183538]
ChEMBL Inhibition of Mps1 B 8.4 pIC50 4 nM IC50 Bioorg Med Chem Lett (2012) 22: 4377-4385 [PMID:22632936]
GtoPdb - - 8.74 pIC50 1.8 nM IC50 Mol Cancer Ther (2011) 10: 2267-75 [PMID:21980130]
ChEMBL Inhibition of human MPS1 expressed in Escherichia coli B 8.74 pIC50 1.8 nM IC50 J Med Chem (2013) 56: 4343-4356 [PMID:23634759]
ChEMBL Inhibition of GST-fused full length human TTK compound pre-incubated for 15 mins prior ATP addition by MBP-based assay B 8.74 pIC50 1.8 nM IC50 Bioorg Med Chem (2014) 22: 4968-4997 [PMID:25043312]
ChEMBL Inhibition of MPS1 (519 to 808 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) after 18 hrs B 8.74 pIC50 1.8 nM IC50 Eur J Med Chem (2019) 175: 247-268 [PMID:31121430]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL Inhibition of Aur A B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2012) 22: 4377-4385 [PMID:22632936]
aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
ChEMBL Inhibition of Aur B B 5.3 pIC50 >5000 nM IC50 Bioorg Med Chem Lett (2012) 22: 4377-4385 [PMID:22632936]
polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
ChEMBL Inhibition of PLK1 B 5.3 pIC50 >5000 nM IC50 Bioorg Med Chem Lett (2012) 22: 4377-4385 [PMID:22632936]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]