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ChEMBL ligand: CHEMBL2179387 |
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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 containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885] | ||||||||
ChEMBL | Binding affinity to first bromodomain of BRD4 (unknown origin) | B | 6.87 | pKd | 136 | nM | Kd | J Med Chem (2013) 56: 8073-8088 [PMID:24090311] |
ChEMBL | Inhibition of human BRD4 BD2 (342 to 460 residues) at 30 uM preincubated for 30 mins followed by substrate addition measured after 30 mins by TR-FRET assay | B | 5.45 | pIC50 | 3540 | nM | IC50 | Eur J Med Chem (2016) 121: 294-299 [PMID:27266999] |
ChEMBL | Inhibition of BRD4 in human MOLM-14 cells harboring FLT3-ITD mutant assessed as decrease in metabolic activity measured after 72 hrs by MTT assay | B | 5.57 | pIC50 | 2700 | nM | IC50 | ACS Med Chem Lett (2020) 11: 1928-1934 [PMID:33062175] |
ChEMBL | Inhibition of BRD4 in human HEL cells harboring JAK2 V617F mutant assessed as decrease in metabolic activity measured after 72 hrs by MTT assay | B | 5.7 | pIC50 | 2000 | nM | IC50 | ACS Med Chem Lett (2020) 11: 1928-1934 [PMID:33062175] |
ChEMBL | Inhibition of human His-tagged BRD4 BD1 (49 to 170 residues) using H-SGRGK(Ac)GGK(Ac)GLGK-(Ac)GGAK(Ac)RHRK(Biotin)-OH as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by TR-FRET assay | B | 6.01 | pIC50 | 980 | nM | IC50 | Eur J Med Chem (2016) 121: 294-299 [PMID:27266999] |
ChEMBL | Inhibition of BRD4 (unknown origin) by Alphascreen assay | B | 6.66 | pIC50 | 220 | nM | IC50 | Eur J Med Chem (2018) 152: 264-273 [PMID:29730189] |
ChEMBL | Inhibition of BRD4 bromodomain (unknown origin) | B | 6.66 | pIC50 | 220 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126577-126577 [PMID:31421967] |
ChEMBL | Inhibition of recombinant His-tagged human BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells preincubated for 30 mins followed by H4K5acK8acK12acK16ac substrate addition measured after 30 mins by AlphaScreen assay | B | 6.66 | pIC50 | 220 | nM | IC50 | Bioorg Med Chem (2018) 26: 2937-2957 [PMID:29776834] |
ChEMBL | Binding affinity to human BRD4 bromodomain 1 using H4Ac4 peptide by amplified luminescent proximity homogeneous assay | B | 6.66 | pIC50 | 220 | nM | IC50 | J Med Chem (2013) 56: 3217-3227 [PMID:23517011] |
ChEMBL | Inhibition of BRD4 (unknown origin) | B | 6.66 | pIC50 | 220 | nM | IC50 | Bioorg Med Chem (2018) 26: 3399-3405 [PMID:29764756] |
ChEMBL | Inhibition of BRD4 isoform 1 by AlphaScreen assay | B | 6.66 | pIC50 | 220 | nM | IC50 | J Med Chem (2012) 55: 9831-9837 [PMID:23095041] |
GtoPdb | Assayed using recombinant BRD4-BD1. | - | 6.66 | pIC50 | 220 | nM | IC50 | J Med Chem (2012) 55: 9831-7 [PMID:23095041] |
ChEMBL | Inhibition of BRD4 BD1 (unknown origin) preincubated for 15 mins followed by peptide addition and measured after 60 mins by TR-FRET assay | B | 7.06 | pIC50 | 88 | nM | IC50 | Eur J Med Chem (2020) 208: 112780-112780 [PMID:32883643] |
CREB binding protein/CREB-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793] | ||||||||
ChEMBL | Binding affinity to CREBBP by SPR method | B | 4.31 | pKd | 49000 | nM | Kd | J Med Chem (2012) 55: 9831-9837 [PMID:23095041] |
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]