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ChEMBL ligand: CHEMBL2140523 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | 4.44 | pIC50 | 36000 | nM | IC50 | J Med Chem (2013) 56: 10045-10065 [PMID:24256217] |
TTK protein kinase/Dual specificity protein kinase TTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3983] [GtoPdb: 2264] [UniProtKB: P33981] | ||||||||
ChEMBL | Inhibition of Myc-tagged wild type MPS1 autophosphorylation in human HCT116 cells after 2 hrs in presence of proteosome inhibitor MG132 | B | 6.14 | pIC50 | 720 | nM | IC50 | J Med Chem (2013) 56: 10045-10065 [PMID:24256217] |
ChEMBL | Displacement of tracer K9 from NanoLuc-fused MPS1 (unknown origin) expressed in HEK293T cells measured after 2 hrs by NanoBRET assay | B | 6.37 | pIC50 | 429 | nM | IC50 | J Med Chem (2022) 65: 3173-3192 [PMID:35167750] |
ChEMBL | Inhibition of N-terminal GST-tagged full-length human Mps1 expressed in insect cells using FITC-DHTGFLTEYVATR-CONH2 as substrate after 25 mins by fluorescence assay | B | 7.46 | pIC50 | 35 | nM | IC50 | Eur J Med Chem (2019) 175: 247-268 [PMID:31121430] |
ChEMBL | Inhibition of human His-tagged TTK (510 to 857)-mediated MBP phosphorylation after 20 mins by scintillation counting analysis in presence of gamma-[32P]ATP | B | 7.46 | pIC50 | 35 | nM | IC50 | J Med Chem (2015) 58: 3366-3392 [PMID:25763473] |
ChEMBL | Inhibition of GST-fused full length human TTK compound pre-incubated for 15 mins prior ATP addition by MBP-based assay | B | 7.46 | pIC50 | 35 | nM | IC50 | Bioorg Med Chem (2014) 22: 4968-4997 [PMID:25043312] |
GtoPdb | In vitro assay using a His-tagged catalytic domain fragment of MPS1 (amino acids 510–857). | - | 7.46 | pIC50 | ~35 | nM | IC50 | J Cell Biol (2010) 190: 25-34 [PMID:20624899] |
ChEMBL | Inhibition of recombinant human full length N-terminal GST-fused MPS1 (1 to 857 residues) using histone H3 as substrate by TR-FRET assay | B | 8.01 | pIC50 | 9.79 | nM | IC50 | J Med Chem (2022) 65: 3173-3192 [PMID:35167750] |
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 | 4.68 | pIC50 | 21000 | nM | IC50 | J Med Chem (2013) 56: 10045-10065 [PMID:24256217] |
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]