ABBV-744 [Ligand Id: 10730] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4297454 (Abbv-744, ABBV-744) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| bromodomain containing 2/Bromodomain-containing protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293289] [GtoPdb: 1944] [UniProtKB: P25440] | ||||||||
| ChEMBL | Inhibition of N-terminal His6-tagged human BRD2 BD1 (73 to 194 residues) after 1 hr by TR-FRET assay | B | 5.93 | pKi | 1162 | nM | Ki | J Med Chem (2020) 63: 5585-5623 [PMID:32324999] |
| ChEMBL | Inhibition of N-terminal His6-tagged human BRD2 BD2 (348 to 455 residues) after 1 hr by TR-FRET assay | B | 8.34 | pKi | 4.6 | nM | Ki | J Med Chem (2020) 63: 5585-5623 [PMID:32324999] |
| bromodomain containing 3/Bromodomain-containing protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795186] [GtoPdb: 2725] [UniProtKB: Q15059] | ||||||||
| ChEMBL | Inhibition of BRD3 BD1 (unknown origin) after 1 hr by TR-FRET assay | B | 5.5 | pKi | 3140 | nM | Ki | J Med Chem (2020) 63: 5585-5623 [PMID:32324999] |
| ChEMBL | Inhibition of BRD3 BD2 (unknown origin) after 1 hr by TR-FRET assay | B | 8.31 | pKi | 4.9 | nM | Ki | J Med Chem (2020) 63: 5585-5623 [PMID:32324999] |
| bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885] | ||||||||
| ChEMBL | Binding affinity to BRD4 BD1 (unknown origin) assessed as dissociation constant by Discover X assay | B | 5.48 | pKd | 3300 | nM | Kd | J Med Chem (2021) 64: 10497-10511 [PMID:34236185] |
| ChEMBL | Inhibition of BRD4-BD1 (unknown origin) assessed as dissociation constant by TR-FRET method | B | 6.28 | pKd | 520 | nM | Kd | J Med Chem (2022) 65: 5660-5674 [PMID:35348328] |
| ChEMBL | Binding affinity to human partial length BRD4 BD2 expressed in bacterial expression system assessed as dissociation constant by BROMOscan assay | B | 8.68 | pKd | 2.1 | nM | Kd | J Med Chem (2021) 64: 10497-10511 [PMID:34236185] |
| ChEMBL | Inhibition of BRD4-BD2 (unknown origin) assessed as dissociation constant by TR-FRET method | B | 8.8 | pKd | 1.6 | nM | Kd | J Med Chem (2022) 65: 5660-5674 [PMID:35348328] |
| ChEMBL | Inhibition of human N-terminal His6 tagged BRD4 BD1 (57 to 168) residues expressed in Escherichia coli BL21(DE3) cells after 1 hr by TR-FRET assay | B | 6.28 | pKi | 520 | nM | Ki | J Med Chem (2020) 63: 5585-5623 [PMID:32324999] |
| ChEMBL | Inhibition of human N-terminal His6 tagged BRD4 BD2 (352 to 457) residues expressed in Escherichia coli BL21(DE3) cells after 1 hr by TR-FRET assay | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (2020) 63: 5585-5623 [PMID:32324999] |
| ChEMBL | Inhibition of NanoLuc-tagged BRD4 BD1 (unknown origin) expressed in human HeLa cells after 2 hrs by NanoBRET assay | B | 4.68 | pIC50 | 20700 | nM | IC50 | J Med Chem (2020) 63: 5585-5623 [PMID:32324999] |
| ChEMBL | Inhibition of His-tagged BRD4 bromodomain 1 (unknown origin) using [Lys (5,8,12,16) Ac] H4(1-21) as substrate by fluorescence based assay | B | 6.48 | pIC50 | 327.5 | nM | IC50 | Eur J Med Chem (2021) 209: 112868-112868 [PMID:33077265] |
| ChEMBL | Inhibition of NanoLuc-tagged BRD4 BD2 (unknown origin) expressed in human HeLa cells after 2 hrs by NanoBRET assay | B | 7.56 | pIC50 | 27.5 | nM | IC50 | J Med Chem (2020) 63: 5585-5623 [PMID:32324999] |
| ChEMBL | Inhibition of His-tagged BRD4 bromodomain 2 (unknown origin) using [Lys (5,8,12,16) Ac] H4(1-21) as substrate by fluorescence based assay | B | 8.48 | pIC50 | 3.3 | nM | IC50 | Eur J Med Chem (2021) 209: 112868-112868 [PMID:33077265] |
| bromodomain testis associated/Bromodomain testis-specific protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21] | ||||||||
| ChEMBL | Inhibition of BRDT BD1 (unknown origin) after 1 hr by TR-FRET assay | B | 6.04 | pKi | 917 | nM | Ki | J Med Chem (2020) 63: 5585-5623 [PMID:32324999] |
| ChEMBL | Inhibition of BRDT BD2 (unknown origin) after 1 hr by TR-FRET assay | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2020) 63: 5585-5623 [PMID:32324999] |
| histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547] | ||||||||
| ChEMBL | Inhibition of HDAC1 (unknown origin) by fluorescence based assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2021) 209: 112868-112868 [PMID:33077265] |
| histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
| ChEMBL | Inhibition of HDAC6 (unknown origin) by fluorescence based assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2021) 209: 112868-112868 [PMID:33077265] |
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]
