NMS-P715 [Ligand Id: 9401] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1236095
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  • 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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  • 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
cyclin dependent kinase 2/CDK2/Cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038469] [GtoPdb: 1973] [UniProtKB: P20248, P24941]
ChEMBL Inhibition of full length CDK2/Cyclin A (unknown origin) using 5FAMQSPKKG-CONH2 as substrate after 60 mins by fluorescence assay B 4 pIC50 >100000 nM IC50 J Med Chem (2013) 56: 10045-10065 [PMID:24256217]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094128] [GtoPdb: 1973] [UniProtKB: P20248, P24941, P78396]
ChEMBL Inhibition of CDK2/Cyclin A assessed as [33P]-gamma-ATP incorporation into substrate by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 4507-4511 [PMID:21723120]
TTK protein kinase/Dual specificity protein kinase TTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3983] [GtoPdb: 2264] [UniProtKB: P33981]
ChEMBL Inhibition of MPS1 assessed as [33P]-gamma-ATP incorporation into substrate P38-betatide by gamma counting B 6.74 pIC50 182 nM IC50 Bioorg Med Chem Lett (2011) 21: 4507-4511 [PMID:21723120]
ChEMBL Inhibition of MPS1 (unknown origin) B 6.74 pIC50 182 nM IC50 Eur J Med Chem (2019) 175: 247-268 [PMID:31121430]
GtoPdb - - 6.74 pIC50 182 nM IC50 Bioorg Med Chem Lett (2011) 21: 4507-11 [PMID:21723120]
ChEMBL Inhibition of Myc-tagged wild type MPS1 autophosphorylation in human HCT116 cells after 2 hrs in presence of proteosome inhibitor MG132 B 6.8 pIC50 160 nM IC50 J Med Chem (2013) 56: 10045-10065 [PMID:24256217]
ChEMBL Inhibition of MPS1 (unknown origin) B 8.1 pIC50 8 nM IC50 J Med Chem (2013) 56: 4343-4356 [PMID:23634759]
ChEMBL Inhibition of N-terminal 6XHis-tagged/GST-tagged full length human MPS1 expressed in recombinant baculovirus infected sf9 insect cells using 5FAM-DHTGFLTEYVATRCONH2 as substrate after 60 to 90 mins by fluorescence assay B 8.15 pIC50 7 nM IC50 J Med Chem (2013) 56: 10045-10065 [PMID:24256217]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL Inhibition of N-terminal His-tagged Aurora A (unknown origin) using 5FAM-LRRASLG-CONH2 as substrate after 60 mins by fluorescence assay B 4.52 pIC50 >30000 nM IC50 J Med Chem (2013) 56: 10045-10065 [PMID:24256217]
ChEMBL Inhibition of Aur-A assessed as [33P]-gamma-ATP incorporation into substrate by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 4507-4511 [PMID:21723120]
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 assessed as [33P]-gamma-ATP incorporation into substrate by gamma counting B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 4507-4511 [PMID:21723120]

ChEMBL data shown on this page come from version 32:

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]