NMS-P715 [Ligand Id: 9401] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1236095 |
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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 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]
