BAY1217389 [Ligand Id: 12705] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4456085 (Bay-1217389, BAY-1217389) |
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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] | ||||||||
| GtoPdb | - | - | 8 | pIC50 | <10 | nM | IC50 | Mol Cancer Ther (2016) 15: 583-92 [PMID:26832791] |
| ChEMBL | Inhibition of GST-tagged recombinant human MPS1 expressed in baculovirus expression system using biotin-Ahx-PWDPDDADITEILG as substrate preincubated for 15 mins followed by substrate and 2 mM ATP addition and measured after 60 mins by TR-FRET assay | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2020) 63: 8025-8042 [PMID:32338514] |
| ChEMBL | Displacement of tracer K9 from NanoLuc-fused MPS1 (unknown origin) expressed in HEK293T cells measured after 2 hrs by NanoBRET assay | B | 9 | pIC50 | <1 | nM | IC50 | J Med Chem (2022) 65: 3173-3192 [PMID:35167750] |
| 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 | 9 | pIC50 | <1 | nM | IC50 | J Med Chem (2022) 65: 3173-3192 [PMID:35167750] |
| ChEMBL | Inhibition of GST-tagged recombinant human MPS1 expressed in baculovirus expression system using biotin-Ahx-PWDPDDADITEILG as substrate preincubated for 15 mins followed by substrate and 10 uM ATP addition and measured after 60 mins by TR-FRET assay | B | 9.15 | pIC50 | 0.7 | nM | IC50 | J Med Chem (2020) 63: 8025-8042 [PMID:32338514] |
| ChEMBL | Inhibition of MPS1 (unknown origin) using biotin-AhxPWDPDDADITEILG-NH2 as substrate preincubated for 15 mins followed by substrate addition by TR-FRET assay | B | 9.2 | pIC50 | 0.63 | nM | IC50 | Eur J Med Chem (2019) 175: 247-268 [PMID:31121430] |
| ChEMBL | Inhibition of MPS1 in human HeLa cells assessed as reduction in spindle assembly checkpoint incubated for 4 hrs by p-histone H3/Hoechst 33342 staining based microscopic analysis | B | 9.6 | pIC50 | 0.25 | nM | IC50 | J Med Chem (2020) 63: 8025-8042 [PMID:32338514] |
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]
