ChEMBL ligand: CHEMBL4226570
bromodomain containing 2/Bromodomain-containing protein 2 in Human [ChEMBL: CHEMBL1293289] [GtoPdb: 1944] [UniProtKB: P25440] There should be some charts here, you may need to enable JavaScript!
bromodomain containing 3/Bromodomain-containing protein 3 in Human [ChEMBL: CHEMBL1795186] [GtoPdb: 2725] [UniProtKB: Q15059] There should be some charts here, you may need to enable JavaScript!
bromodomain containing 4/Bromodomain-containing protein 4 in Human [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885] There should be some charts here, you may need to enable JavaScript!
von Hippel-Lindau tumor suppressor/Von Hippel-Lindau disease tumor suppressor in Human [ChEMBL: CHEMBL3108660] [GtoPdb: 3204] [UniProtKB: P40337] There should be some charts here, you may need to enable JavaScript!
von Hippel-Lindau tumor suppressor/Von Hippel-Lindau disease tumor suppressor/Elongin B/Elongin C in Human [ChEMBL: CHEMBL3301400] [GtoPdb: 3204] [UniProtKB: P40337, Q15369, Q15370] There should be some charts here, you may need to enable JavaScript!

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	Binding affinity to BRD2 BD1 (unknown origin) assessed as dissociation constant by isothermal titration calorimetry assay	B	6.13	pKd	740	nM	Kd	Bioorg Med Chem (2022) 73: 117033-117033 [PMID:36202064]
ChEMBL	Binding affinity to BRD2 BD1 domain (unknown origin)	B	6.51	pKd	307	nM	Kd	Eur J Med Chem (2020) 207: 112750-112750 [PMID:32871345]
ChEMBL	Binding affinity to BRD2 BD2 domain (unknown origin)	B	6.64	pKd	228	nM	Kd	Eur J Med Chem (2020) 207: 112750-112750 [PMID:32871345]
ChEMBL	Binding affinity to BRD2 (unknown origin) assessed as dissociation constant	B	6.94	pKd	115	nM	Kd	Bioorg Med Chem (2022) 73: 117033-117033 [PMID:36202064]
bromodomain containing 3/Bromodomain-containing protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795186] [GtoPdb: 2725] [UniProtKB: Q15059]
ChEMBL	Binding affinity to BRD3 BD1 domain (unknown origin)	B	6.92	pKd	119	nM	Kd	Eur J Med Chem (2020) 207: 112750-112750 [PMID:32871345]
ChEMBL	Binding affinity to BRD3 BD2 domain (unknown origin)	B	6.94	pKd	115	nM	Kd	Eur J Med Chem (2020) 207: 112750-112750 [PMID:32871345]
ChEMBL	Binding affinity to BRD3 (unknown origin) assessed as dissociation constant	B	6.94	pKd	115	nM	Kd	Bioorg Med Chem (2022) 73: 117033-117033 [PMID:36202064]
bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
ChEMBL	Binding affinity to BRD4 BD2 (unknown origin) assessed as dissociation constant by isothermal titration calorimetry assay	B	6.13	pKd	740	nM	Kd	Bioorg Med Chem (2022) 73: 117033-117033 [PMID:36202064]
ChEMBL	Binding affinity to BRD4 BD1 domain (unknown origin)	B	6.42	pKd	382	nM	Kd	Eur J Med Chem (2020) 207: 112750-112750 [PMID:32871345]
ChEMBL	Binding affinity to BRD4 BD2 domain (unknown origin)	B	6.92	pKd	120	nM	Kd	Eur J Med Chem (2020) 207: 112750-112750 [PMID:32871345]
ChEMBL	Binding affinity to BRD4 (unknown origin) assessed as dissociation constant	B	6.94	pKd	115	nM	Kd	Bioorg Med Chem (2022) 73: 117033-117033 [PMID:36202064]
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 VHL (unknown origin) assessed as dissociation constant by isothermal titration calorimetry assay	B	7.18	pKd	66	nM	Kd	Bioorg Med Chem (2022) 73: 117033-117033 [PMID:36202064]
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	Displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex assessed as inhibition constant by 19F NMR assay	B	6.55	pKi	282	nM	Ki	RSC Med Chem (2021) 12: 1765-1770 [PMID:34778777]
ChEMBL	Displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from VBC E3 ligase (unknown origin) binary complex by 19F NMR assay	B	6.05	pIC50	882	nM	IC50	RSC Med Chem (2021) 12: 1765-1770 [PMID:34778777]

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]