GNE-049 [Ligand Id: 13247] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4076748 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| bromodomain adjacent to zinc finger domain 2B/Bromodomain adjacent to zinc finger domain protein 2B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741220] [GtoPdb: 2722] [UniProtKB: Q9UIF8] | ||||||||
| ChEMBL | Displacement of biotinylated histone H3K14 peptide ligand from human recombinant His-tagged BAZ2B measured after 10 mins by TR-FRET assay | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2017) 60: 9162-9183 [PMID:28892380] |
| bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885] | ||||||||
| ChEMBL | Displacement of biotinylated histone H3K14 peptide ligand from human recombinant His-tagged BRD4 bromodomain-2 measured after 10 mins by TR-FRET assay | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2017) 60: 9162-9183 [PMID:28892380] |
| ChEMBL | Displacement of biotinylated histone H3K14 peptide ligand from human recombinant His-tagged BRD4 bromodomain-1 measured after 10 mins by TR-FRET assay | B | 5.38 | pIC50 | 4200 | nM | IC50 | J Med Chem (2017) 60: 9162-9183 [PMID:28892380] |
| bromodomain containing 8/Bromodomain-containing protein 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3588731] [GtoPdb: 2727] [UniProtKB: Q9H0E9] | ||||||||
| ChEMBL | Displacement of biotinylated histone H3K14 peptide ligand from recombinant His-tagged BRD8 bromodomain-1 (unknown origin) measured after 10 mins by TR-FRET assay | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2017) 60: 9162-9183 [PMID:28892380] |
| bromodomain containing 9/Bromodomain-containing protein 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108640] [GtoPdb: 2728] [UniProtKB: Q9H8M2] | ||||||||
| ChEMBL | Displacement of biotinylated histone H3K14 peptide ligand from human recombinant His-tagged BRD9 measured after 10 mins by TR-FRET assay | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2017) 60: 9162-9183 [PMID:28892380] |
| CECR2 histone acetyl-lysine reader/Cat eye syndrome critical region protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108639] [GtoPdb: 2733] [UniProtKB: Q9BXF3] | ||||||||
| ChEMBL | Displacement of biotinylated histone H3K14 peptide ligand from human recombinant His-tagged CECR2 measured after 10 mins by TR-FRET assay | B | 4.85 | pIC50 | 14000 | nM | IC50 | J Med Chem (2017) 60: 9162-9183 [PMID:28892380] |
| CREB binding protein/CREB-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793] | ||||||||
| ChEMBL | Inhibition of Halo-tagged histone H3.3 binding to NanoLuc luciferase conjugated human CBP expressed in HEK293 cells after overnight incubation by BRET assay | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2017) 60: 9162-9183 [PMID:28892380] |
| ChEMBL | Displacement of biotinylated histone H3K14 peptide ligand from human recombinant His-tagged CBP measured after 10 mins by TR-FRET assay | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2017) 60: 9162-9183 [PMID:28892380] |
| GtoPdb | - | - | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2017) 60: 9162-9183 [PMID:28892380] |
| ChEMBL | Inhibition of CBP in human MV-4-11 cells assessed as decrease in MYC expression incubated for 4 hrs measured by luminescence method | B | 7.85 | pEC50 | 14 | nM | EC50 | J Med Chem (2017) 60: 9162-9183 [PMID:28892380] |
| lysine acetyltransferase 2A/Histone acetyltransferase GCN5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5501] [GtoPdb: 2736] [UniProtKB: Q92830] | ||||||||
| ChEMBL | Displacement of biotinylated histone H3K14 peptide ligand from recombinant His-tagged human GCN5L2 measured after 10 mins by TR-FRET assay | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2017) 60: 9162-9183 [PMID:28892380] |
| E1A binding protein p300/Histone acetyltransferase p300 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3784] [GtoPdb: 2735] [UniProtKB: Q09472] | ||||||||
| ChEMBL | Displacement of biotinylated histone H3K14 peptide ligand from human recombinant His-tagged P300 measured after 10 mins by TR-FRET assay | B | 8.89 | pIC50 | 1.3 | nM | IC50 | J Med Chem (2017) 60: 9162-9183 [PMID:28892380] |
| lysine acetyltransferase 2B/Histone acetyltransferase PCAF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5500] [GtoPdb: 2737] [UniProtKB: Q92831] | ||||||||
| ChEMBL | Displacement of biotinylated histone H3K14 peptide ligand from human recombinant His-tagged PCAF measured after 10 mins by TR-FRET assay | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2017) 60: 9162-9183 [PMID:28892380] |
| bromodomain PHD finger transcription factor/Nucleosome-remodeling factor subunit BPTF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3085621] [GtoPdb: 2723] [UniProtKB: Q12830] | ||||||||
| ChEMBL | Displacement of biotinylated histone H3K14 peptide ligand from recombinant His-tagged BPTF (unknown origin) measured after 10 mins by TR-FRET assay | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2017) 60: 9162-9183 [PMID:28892380] |
| bromodomain and PHD finger containing 1/Peregrin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3132741] [GtoPdb: 2730] [UniProtKB: P55201] | ||||||||
| ChEMBL | Displacement of biotinylated histone H3K14 peptide ligand from human recombinant His-tagged BRPF1 measured after 10 mins by TR-FRET assay | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2017) 60: 9162-9183 [PMID:28892380] |
| TATA-box binding protein associated factor 1/Transcription initiation factor TFIID subunit 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3217390] [GtoPdb: 2231] [UniProtKB: P21675] | ||||||||
| ChEMBL | Displacement of biotinylated histone H3K14 peptide ligand from recombinant His-tagged TAF1 bromodomain-2 (unknown origin) measured after 10 mins by TR-FRET assay | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2017) 60: 9162-9183 [PMID:28892380] |
| ChEMBL | Displacement of biotinylated histone H3K14 peptide ligand from human recombinant His-tagged TAF1 bromodomain-1 measured after 10 mins by TR-FRET assay | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2017) 60: 9162-9183 [PMID:28892380] |
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]
