compound 14k [PMID: 21982499] [Ligand Id: 8214] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1915438 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Bcl2-antagonist of cell death (BAD) in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3817] [UniProtKB: Q92934] | ||||||||
| ChEMBL | Inhibition of BAD phosphorylation at Ser112 in human MV-4-11 cells assessed as phospho-BAD level after 4 hrs by ELISA | B | 7.52 | pEC50 | 30 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 6687-6692 [PMID:21982499] |
| 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 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6687-92 [PMID:21982499] |
| ChEMBL | Inhibition of human recombinant Pim1 using RSRHSSYPAGT as substrate by radiometric assay in the presence of 30 uM [ATP] | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6687-6692 [PMID:21982499] |
| ChEMBL | Inhibition of human recombinant PIM1 in presence of ATP by ELISA based spectrophotometric analysis | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem (2017) 25: 4855-4875 [PMID:28760531] |
| ChEMBL | Inhibition of PIM1 using KKRNRTLTV as substrate by millipore assay in the presence of 90 uM [ATP] | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6687-6692 [PMID:21982499] |
| 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 | - | - | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6687-92 [PMID:21982499] |
| ChEMBL | Inhibition of human recombinant Pim2 using RSRHSSYPAGT as substrate by radiometric assay in the presence of 5 uM [ATP] | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6687-6692 [PMID:21982499] |
| ChEMBL | Inhibition of PIM2 by millipore assay in the presence of 15 uM [ATP] | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6687-6692 [PMID:21982499] |
| 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 in the presence of 155 uM [ATP] | B | 7.07 | pIC50 | 86 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6687-6692 [PMID:21982499] |
| GtoPdb | - | - | 7.07 | pIC50 | 86 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6687-92 [PMID:21982499] |
| fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| GtoPdb | - | - | 6.98 | pIC50 | 104 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6687-92 [PMID:21982499] |
| ChEMBL | Inhibition of FLT3 using EAIYAAPFAKKK as substrate by radiometric assay in the presence of 200 uM [ATP] | B | 6.98 | pIC50 | 104 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6687-6692 [PMID:21982499] |
| ChEMBL | Inhibition of FLT3 phosphorylation at Tyr591 in human MV-4-11 cells assessed as phospho-FLT3 level after 4 hrs by ELISA | B | 5.32 | pEC50 | 4800 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 6687-6692 [PMID:21982499] |
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]
