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 |
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| 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 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]
