nuvisertib [Ligand Id: 13215] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3975308 (SGI-9481, Tp-3654, TP-3654) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Fast Patch Assay: Representative compounds were tested for hERG activity using the Fast Patch assay available from WuXiApptec (Shanghai China). | B | 4.52 | pIC50 | >30000 | nM | IC50 | US-9416132-B2. Substituted imidazo[1,2-b]pyridazines as protein kinase inhibitors (2016) |
| Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309] | ||||||||
| GtoPdb | - | - | 8.3 | pKi | 5 | nM | Ki | Neoplasia (2014) 16: 403-12 [PMID:24953177] |
| ChEMBL | Inhibition of PIM1 (unknown origin) up to 120 mins by Michaelis-Menten plot analysis | B | 8.3 | pKi | 5 | nM | Ki | Eur J Med Chem (2019) 172: 95-108 [PMID:30954777] |
| ChEMBL | Kinase-Glo Assay: These assays are set up in duplicate 50 ul volumes in white, flat bottom 96 well plates. Inhibitors are added to the solution of 1× kinase buffer, 10 uM ATP, 100 uM Pim-1-specific substrate, 50 ng of active Pim-1 enzyme, and water in serial dilutions ranging from micromolar to nanomolar concentrations. This solution is incubated at 30 degrees Celsius at 360 rpm for two hours. Following the incubation, 50 ul of Kinase-Glo reagent is added to each well, including all positive and negative control wells, and incubated at room temperature for 15 minutes. The plate is then read by the Luminoskan Ascent instrument and the results displayed with the Ascent Software version 2.6. | B | 9 | pIC50 | 1 | nM | IC50 | US-9416132-B2. Substituted imidazo[1,2-b]pyridazines as protein kinase inhibitors (2016) |
| fms related receptor tyrosine kinase 3 in Human [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| GtoPdb | - | - | 6.55 | pIC50 | 279 | nM | IC50 | Neoplasia (2014) 16: 403-12 [PMID:24953177] |
| Pim-2 proto-oncogene, serine/threonine kinase in Human [GtoPdb: 2159] [UniProtKB: Q9P1W9] | ||||||||
| GtoPdb | - | - | 6.62 | pKi | 239 | nM | Ki | Neoplasia (2014) 16: 403-12 [PMID:24953177] |
| Pim-3 proto-oncogene, serine/threonine kinase in Human [GtoPdb: 2160] [UniProtKB: Q86V86] | ||||||||
| GtoPdb | - | - | 7.38 | pKi | 42 | nM | Ki | Neoplasia (2014) 16: 403-12 [PMID:24953177] |
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]
