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] |
| ChEMBL | Inhibition of PIM1 (unknown origin) | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2022) 65: 893-921 [PMID:33539089] |
| 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
