CX-6258 [Ligand Id: 9368] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2037200 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309] | ||||||||
| ChEMBL | Reversible inhibition of human recombinant Pim1 using RSRHSSYPAGT as substrate | B | 8.3 | pKi | 5 | nM | Ki | ACS Med Chem Lett (2012) 3: 135-139 [PMID:24900437] |
| GtoPdb | - | - | 8.3 | pIC50 | 5 | nM | IC50 | ACS Med Chem Lett (2012) 3: 135-9 [PMID:24900437] |
| ChEMBL | Inhibition of human recombinant Pim1 using RSRHSSYPAGT as substrate by radiometric assay | B | 8.3 | pIC50 | 5 | nM | IC50 | ACS Med Chem Lett (2012) 3: 135-139 [PMID:24900437] |
| Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9] | ||||||||
| GtoPdb | - | - | 7.6 | pIC50 | 25 | nM | IC50 | ACS Med Chem Lett (2012) 3: 135-9 [PMID:24900437] |
| ChEMBL | Inhibition of human recombinant Pim2 using RSRHSSYPAGT as substrate by radiometric assay | B | 7.6 | pIC50 | 25 | nM | IC50 | ACS Med Chem Lett (2012) 3: 135-139 [PMID:24900437] |
| Pim-3 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5407] [GtoPdb: 2160] [UniProtKB: Q86V86] | ||||||||
| ChEMBL | Inhibition of Pim3 using RSRHSSYPAGT as substrate by radiometric assay | B | 7.8 | pIC50 | 16 | nM | IC50 | ACS Med Chem Lett (2012) 3: 135-139 [PMID:24900437] |
| GtoPdb | - | - | 7.8 | pIC50 | 16 | nM | IC50 | ACS Med Chem Lett (2012) 3: 135-9 [PMID:24900437] |
| fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| ChEMBL | Inhibition of Flt3 phosphorylation at Y591 in human MV411 cells after 2 hrs by Western blot analysis | B | 5 | pIC50 | >10000 | nM | IC50 | ACS Med Chem Lett (2012) 3: 135-139 [PMID:24900437] |
| ChEMBL | Inhibition of Flt3 using EAIYAAPFAKKK as substrate by radiometric assay | B | 6.87 | pIC50 | 134 | nM | IC50 | ACS Med Chem Lett (2012) 3: 135-139 [PMID:24900437] |
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]
