AX15836 [Ligand Id: 11980] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4541479 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885] | ||||||||
| ChEMBL | Inhibition of BRD4 (unknown origin) | B | 5.44 | pKd | 3600 | nM | Kd | Eur J Med Chem (2019) 178: 530-543 [PMID:31212132] |
| ChEMBL | Binding affinity to human BRD4 BD1 (44 to 168 residues) expressed in bacterial expression system by bromoscan assay | B | 5.44 | pKd | 3600 | nM | Kd | J Med Chem (2022) 65: 6513-6540 [PMID:35468293] |
| mitogen-activated protein kinase 7/Mitogen-activated protein kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5332] [GtoPdb: 2093] [UniProtKB: Q13164] | ||||||||
| ChEMBL | Inhibition of ERK5 in human SN12C cells transduced with MEF2-responsive transcription element assessed as reduction in MEF2 transcription by measuring luciferase signal after 16 hrs by luciferase reporter gene assay | B | 7.07 | pIC50 | 86 | nM | IC50 | J Med Chem (2019) 62: 928-940 [PMID:30563338] |
| ChEMBL | Inhibition of His-tagged MAP2K5 activated N-terminal GST-tagged recombinant human ERK5 (1 to 398 residues) expressed in Escherichia coli using biotin-Ahx-PPGDYSTTPGGTLFSTTPGGTRI peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins in presence of ATP by TR-FRET assay | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2019) 62: 928-940 [PMID:30563338] |
| ChEMBL | Inhibition of ERK5 in human HeLa cells by KiNativ profiling method | B | 8.1 | pIC50 | 8 | nM | IC50 | Eur J Med Chem (2019) 178: 530-543 [PMID:31212132] |
| ChEMBL | Inhibition of ERK5 (unknown origin) incubated for 1 hr by KiNativ profiling analysis | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2022) 65: 6513-6540 [PMID:35468293] |
| GtoPdb | - | - | 8.1 | pIC50 | 8 | nM | IC50 | Proc Natl Acad Sci U S A (2016) 113: 11865-11870 [PMID:27679845] |
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]
