MZ1 [Ligand Id: 10728] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4226570 |
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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 | Binding affinity to N-terminal His6-tagged recombinant human Brd4 BD2 expressed in Escherichia coli BL21 (DE3) assessed as compound binary complex formation by isothermal titration calorimetry-based assay | B | 7.59 | pKd | 26 | nM | Kd | J Med Chem (2018) 61: 504-513 [PMID:28595007] |
| GtoPdb | Binding affiniy for recombinant human Brd4 BD2 in vitro. | - | 7.59 | pKd | 26 | nM | Kd | J Med Chem (2018) 61: 504-513 [PMID:28595007] |
| von Hippel-Lindau tumor suppressor/Von Hippel-Lindau disease tumor suppressor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108660] [GtoPdb: 3204] [UniProtKB: P40337] | ||||||||
| ChEMBL | Binding affinity to N-terminal His6-tagged VHL (54 to 213 residues) (unknown origin) expressed in Escherichia coli assessed as displacement of HIF-1alpha by binary binding competitive fluorescence polarization assay | B | 7.47 | pKd | 34 | nM | Kd | J Med Chem (2021) 64: 18082-18101 [PMID:34881891] |
| von Hippel-Lindau tumor suppressor/Von Hippel-Lindau disease tumor suppressor/Elongin B/Elongin C in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301400] [GtoPdb: 3204] [UniProtKB: P40337, Q15369, Q15370] | ||||||||
| ChEMBL | Binding affinity to N-terminal His6-tagged recombinant human VHL (54 to 213 residues)/elongin C (17 to 112 residues)/elongin B (1 to 104 residues) expressed in Escherichia coli BL21 (DE3) assessed as compound binary complex formation by isothermal titration calorimetry-based assay | B | 7.16 | pKd | 69 | nM | Kd | J Med Chem (2018) 61: 504-513 [PMID:28595007] |
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]
