(+)-JQ1 [Ligand Id: 7511] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1957266
  • bromodomain containing 1/Bromodomain-containing protein 1 in Human [ChEMBL: CHEMBL2176774] [GtoPdb: 2724] [UniProtKB: O95696]
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  • bromodomain containing 2/Bromodomain-containing protein 2 in Human [ChEMBL: CHEMBL1293289] [GtoPdb: 1944] [UniProtKB: P25440]
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  • bromodomain containing 3/Bromodomain-containing protein 3 in Human [ChEMBL: CHEMBL1795186] [GtoPdb: 2725] [UniProtKB: Q15059]
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  • bromodomain containing 4/Bromodomain-containing protein 4 in Human [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
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  • bromodomain testis associated/Bromodomain testis-specific protein in Human [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21]
  • bromodomain testis associated in Mouse [GtoPdb: 2729] [UniProtKB: Q91Y44]
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  • CREB binding protein/CREB-binding protein in Human [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793]
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  • Delta and Notch-like epidermal growth factor-related receptor in Human [ChEMBL: CHEMBL5291567] [UniProtKB: Q8NFT8]
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  • E1A binding protein p300/Histone acetyltransferase p300 in Human [ChEMBL: CHEMBL3784] [GtoPdb: 2735] [UniProtKB: Q09472]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
bromodomain containing 1/Bromodomain-containing protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2176774] [GtoPdb: 2724] [UniProtKB: O95696]
ChEMBL Inhibition of recombinant BRD1 (unknown origin) incubated for 120 mins by TR-FRET assay B 4.35 pIC50 44500 nM IC50 J Med Chem (2021) 64: 17413-17435 [PMID:34813314]
bromodomain containing 2/Bromodomain-containing protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293289] [GtoPdb: 1944] [UniProtKB: P25440]
ChEMBL Inhibition of human 6x-His-tagged BRD2 bromodomain 1 expressed in Escherichia coli B 6.89 pKd 130 nM Kd J Med Chem (2018) 61: 9316-9334 [PMID:30253095]
ChEMBL Affinity Biochemical interaction (Isothermal titration calorimetry (ITC)) EUB0000330a BRD2 B 6.89 pKd 128.4 nM Kd Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to BRD2-BD1 by isothermal titration calorimetry B 6.89 pKd 128.4 nM Kd Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554]
ChEMBL Binding affinity to His-tagged BRD2 bromodomain 2 (unknown origin) by SPR assay B 6.94 pKd 116 nM Kd Bioorg Med Chem (2018) 26: 25-36 [PMID:29170024]
ChEMBL Binding affinity to BRD2 bromodomain 2 (348 to 455 residues) (unknown origin) by ITC B 6.95 pKd 112.14 nM Kd Bioorg Med Chem (2018) 26: 25-36 [PMID:29170024]
ChEMBL Binding affinity to recombinant BRD2 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay B 7.11 pKd 78 nM Kd J Med Chem (2020) 63: 5242-5256 [PMID:32255647]
ChEMBL Binding affinity to recombinant BRD2 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay B 7.28 pKd 52 nM Kd J Med Chem (2020) 63: 5242-5256 [PMID:32255647]
ChEMBL Binding affinity to BRD2 D1 (unknown origin) assessed as dissociation constant by isothermal titration calorimetry B 7.47 pKd 34 nM Kd J Med Chem (2022) 65: 2342-2360 [PMID:35007061]
ChEMBL Binding affinity to biotinylated BRD2 BD1 (72 to 205 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method B 7.83 pKd 14.7 nM Kd J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL Binding affinity to biotinylated BRD2 BD2 (349 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method B 8.21 pKd 6.2 nM Kd J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL Displacement of FAM-labeled ZBA248 from BRD2 BD1 (72 to 205 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay B 7.88 pKi 13.2 nM Ki J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD2 bromodomain 1 (72 to 205 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay B 7.88 pKi 13.2 nM Ki J Med Chem (2018) 61: 462-481 [PMID:28339196]
ChEMBL Displacement of FAM-labeled ZBA248 from BRD2 BD2 (349 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay B 7.9 pKi 12.5 nM Ki J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD2 bromodomain 2 (349 to 460 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay B 7.9 pKi 12.5 nM Ki J Med Chem (2018) 61: 462-481 [PMID:28339196]
ChEMBL Inhibition of recombinant BRD2 BD1 (unknown origin) incubated for 120 mins by TR-FRET assay B 6.41 pIC50 392 nM IC50 J Med Chem (2021) 64: 17413-17435 [PMID:34813314]
ChEMBL Inhibition of BRD2 BD1 (unknown origin) incubated for 2 hrs by TR-FRET assay B 6.73 pIC50 185 nM IC50 J Med Chem (2021) 64: 18025-18053 [PMID:34908415]
ChEMBL Inhibition of recombinant human BRD2 bromodomain 2 (342 to 460 residues) using biotin labeled peptide substrate preincubated for 15 mins followed by substrate addition measured after 1 hr by TR-FRET assay B 6.77 pIC50 170 nM IC50 Bioorg Med Chem (2018) 26: 25-36 [PMID:29170024]
ChEMBL Inhibition of human recombinant His-tagged BRD2 BD1 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay B 6.81 pIC50 155 nM IC50 J Med Chem (2020) 63: 3678-3700 [PMID:32153186]
ChEMBL Inhibition of BRD2 D1 (unknown origin) by competitive fluorescence anisotropy assay B 6.85 pIC50 140 nM IC50 J Med Chem (2022) 65: 2342-2360 [PMID:35007061]
ChEMBL Inhibition of BRD2 D2 (unknown origin) by competitive fluorescence anisotropy assay B 6.92 pIC50 120 nM IC50 J Med Chem (2022) 65: 2342-2360 [PMID:35007061]
ChEMBL Inhibition of recombinant BRD2 BD2 (unknown origin) incubated for 120 mins by TR-FRET assay B 6.95 pIC50 112 nM IC50 J Med Chem (2021) 64: 17413-17435 [PMID:34813314]
ChEMBL Inhibition of BRD2 BD1 (unknown origin) after 1 hr by TR-FRET assay B 7.11 pIC50 78 nM IC50 Eur J Med Chem (2018) 151: 450-461 [PMID:29649741]
ChEMBL Binding affinity BRD2 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay B 7.11 pIC50 77 nM IC50 J Med Chem (2022) 65: 2388-2408 [PMID:34982556]
ChEMBL Binding affinity BRD2 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay B 7.27 pIC50 54 nM IC50 J Med Chem (2022) 65: 2388-2408 [PMID:34982556]
ChEMBL Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD2 bromodomain 2 (349 to 460 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay B 7.27 pIC50 53.3 nM IC50 J Med Chem (2018) 61: 462-481 [PMID:28339196]
ChEMBL Inhibition of BRD2 BD2 (unknown origin) after 1 hr by TR-FRET assay B 7.28 pIC50 52 nM IC50 Eur J Med Chem (2018) 151: 450-461 [PMID:29649741]
ChEMBL Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD2 bromodomain 1 (72 to 205 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay B 7.44 pIC50 36.1 nM IC50 J Med Chem (2018) 61: 462-481 [PMID:28339196]
ChEMBL Inhibition of BRD2 BD2 (unknown origin) incubated for 2 hrs by TR-FRET assay B 7.49 pIC50 32 nM IC50 J Med Chem (2021) 64: 18025-18053 [PMID:34908415]
ChEMBL Inhibition of BRD2 BD1 (unknown origin) preincubated for 15 mins followed by peptide addition and measured after 60 mins by TR-FRET assay B 7.54 pIC50 29 nM IC50 Eur J Med Chem (2020) 208: 112780-112780 [PMID:32883643]
ChEMBL Inhibition of BRD2 (unknown origin) by TR-FRET assay B 7.72 pIC50 19 nM IC50 Medchemcomm (2019) 10: 974-984 [PMID:31303996]
ChEMBL Inhibition of human recombinant His-tagged BRD2 BD2 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay B 7.77 pIC50 17 nM IC50 J Med Chem (2020) 63: 3678-3700 [PMID:32153186]
ChEMBL Inhibition of BRD2 BD2 (unknown origin) preincubated for 15 mins followed by peptide addition and measured after 60 mins by TR-FRET assay B 8.17 pIC50 6.7 nM IC50 Eur J Med Chem (2020) 208: 112780-112780 [PMID:32883643]
ChEMBL Affinity Phenotypic Cellular interaction (Cell Proliferation (Cell TiterGlo assay Promega in NMC 11060 cells)) EUB0000330a BRD2 F 8.4 pIC50 4 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Affinity Phenotypic Cellular interaction (Cell Proliferation (Cell TiterGlo assay Promega in NMC 11060 cells)) EUB0000330a BRD2 F 8.4 pIC50 4 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of C-terminal His6-tagged BRD2 BD2 (unknown origin) using H-YSGRGK(Ac)GGK(Ac)GLGK(Ac)-GGAK(Ac)RHRK-Biotin-OH as substrate incubated for 1 hrs by HTRF assay B 8.41 pIC50 3.93 nM IC50 J Med Chem (2022) 65: 5760-5799 [PMID:35333526]
bromodomain containing 3/Bromodomain-containing protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795186] [GtoPdb: 2725] [UniProtKB: Q15059]
ChEMBL Affinity Biochemical interaction (Isothermal titration calorimetry (ITC)) EUB0000330a BRD3 B 7.09 pKd 82 nM Kd Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to BRD3-BD2 by isothermal titration calorimetry B 7.09 pKd 82 nM Kd Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554]
ChEMBL Inhibition of human 6x-His-tagged BRD3 bromodomain 2 expressed in Escherichia coli B 7.09 pKd 82 nM Kd J Med Chem (2018) 61: 9316-9334 [PMID:30253095]
ChEMBL Binding affinity to recombinant BRD3 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay B 7.09 pKd 81 nM Kd J Med Chem (2020) 63: 5242-5256 [PMID:32255647]
ChEMBL Binding affinity to recombinant BRD3 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay B 7.16 pKd 69 nM Kd J Med Chem (2020) 63: 5242-5256 [PMID:32255647]
ChEMBL Binding affinity to BRD3-BD1 by isothermal titration calorimetry B 7.23 pKd 59.5 nM Kd Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554]
ChEMBL Affinity Biochemical interaction (Isothermal titration calorimetry (ITC)) EUB0000330a BRD3 B 7.23 pKd 59.5 nM Kd Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of human 6x-His-tagged BRD3 bromodomain 1 expressed in Escherichia coli B 7.23 pKd 59 nM Kd J Med Chem (2018) 61: 9316-9334 [PMID:30253095]
ChEMBL Binding affinity to biotinylated BRD3 BD1 (24 to 144 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method B 7.87 pKd 13.6 nM Kd J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL Binding affinity to biotinylated BRD3 BD2 (306 to 417 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method B 7.93 pKd 11.7 nM Kd J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL Displacement of FAM-labeled ZBA248 from BRD3 BD2 (306 to 417 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay B 8.05 pKi 8.9 nM Ki J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD3 bromodomain 2 (306 to 417residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay B 8.05 pKi 8.9 nM Ki J Med Chem (2018) 61: 462-481 [PMID:28339196]
ChEMBL Displacement of FAM-labeled ZBA248 from BRD3 BD1 (24 to 144 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay B 8.18 pKi 6.6 nM Ki J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD3 bromodomain 1 (24 to 144 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay B 8.18 pKi 6.6 nM Ki J Med Chem (2018) 61: 462-481 [PMID:28339196]
ChEMBL Inhibition of recombinant BRD3 BD1 (unknown origin) incubated for 120 mins by TR-FRET assay B 6.89 pIC50 129 nM IC50 J Med Chem (2021) 64: 17413-17435 [PMID:34813314]
ChEMBL Inhibition of BRD3 D2 (unknown origin) by competitive fluorescence anisotropy assay B 7.02 pIC50 96 nM IC50 J Med Chem (2022) 65: 2342-2360 [PMID:35007061]
ChEMBL Inhibition of BRD3 BD1 (unknown origin) after 1 hr by TR-FRET assay B 7.09 pIC50 81 nM IC50 Eur J Med Chem (2018) 151: 450-461 [PMID:29649741]
ChEMBL Inhibition of BRD3 D1 (unknown origin) by competitive fluorescence anisotropy assay B 7.1 pIC50 <80 nM IC50 J Med Chem (2022) 65: 2342-2360 [PMID:35007061]
ChEMBL Binding affinity BRD3 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay B 7.1 pIC50 79 nM IC50 J Med Chem (2022) 65: 2388-2408 [PMID:34982556]
ChEMBL Inhibition of BRD3 BD1 (unknown origin) incubated for 2 hrs by TR-FRET assay B 7.12 pIC50 76 nM IC50 J Med Chem (2021) 64: 18025-18053 [PMID:34908415]
ChEMBL Binding affinity BRD3 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay B 7.14 pIC50 72 nM IC50 J Med Chem (2022) 65: 2388-2408 [PMID:34982556]
ChEMBL Inhibition of BRD3 BD2 (unknown origin) after 1 hr by TR-FRET assay B 7.16 pIC50 69 nM IC50 Eur J Med Chem (2018) 151: 450-461 [PMID:29649741]
ChEMBL Inhibition of human recombinant His-tagged BRD3 BD1 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay B 7.19 pIC50 64 nM IC50 J Med Chem (2020) 63: 3678-3700 [PMID:32153186]
ChEMBL Inhibition of BRD3 BD2 (unknown origin) incubated for 2 hrs by TR-FRET assay B 7.21 pIC50 61 nM IC50 J Med Chem (2021) 64: 18025-18053 [PMID:34908415]
ChEMBL Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD3 bromodomain 2 (306 to 417residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay B 7.25 pIC50 56.7 nM IC50 J Med Chem (2018) 61: 462-481 [PMID:28339196]
ChEMBL Inhibition of recombinant BRD3 BD2 (unknown origin) incubated for 120 mins by TR-FRET assay B 7.28 pIC50 53 nM IC50 J Med Chem (2021) 64: 17413-17435 [PMID:34813314]
ChEMBL Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD3 bromodomain 1 (24 to 144 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay B 7.41 pIC50 39.1 nM IC50 J Med Chem (2018) 61: 462-481 [PMID:28339196]
ChEMBL Inhibition of human recombinant His-tagged BRD3 BD2 domain expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by AlphaScreen assay B 7.41 pIC50 39 nM IC50 J Med Chem (2020) 63: 3678-3700 [PMID:32153186]
ChEMBL Inhibition of BRD3 (unknown origin) by TR-FRET assay B 7.64 pIC50 23 nM IC50 Medchemcomm (2019) 10: 974-984 [PMID:31303996]
ChEMBL Inhibition of C-terminal His6-tagged BRD3 BD2 (unknown origin) using H-YSGRGK(Ac)GGK(Ac)GLGK(Ac)-GGAK(Ac)RHRK-Biotin-OH as substrate incubated for 1 hrs by HTRF assay B 8.31 pIC50 4.87 nM IC50 J Med Chem (2022) 65: 5760-5799 [PMID:35333526]
ChEMBL Affinity Phenotypic Cellular interaction (Cell Proliferation (Cell TiterGlo assay Promega in NMC 11060 cells)) EUB0000330a BRD3 F 8.4 pIC50 4 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Affinity Phenotypic Cellular interaction (Cell Proliferation (Cell TiterGlo assay Promega in NMC 11060 cells)) EUB0000330a BRD3 F 8.4 pIC50 4 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
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 ITC analysis B 6.64 pKd 230 nM Kd Eur J Med Chem (2021) 222: 113588-113588 [PMID:34107385]
ChEMBL Binding affinity to BRD4 C-terminal bromodomain 2 H437D mutant (unknown origin) expressed in Escherichia coli Bl21(DE3) by fluorescence polarization assay B 6.7 pKd 200 nM Kd J Med Chem (2018) 61: 9316-9334 [PMID:30253095]
ChEMBL Binding affinity to BRD4 D2 (unknown origin) assessed as dissociation constant by isothermal titration calorimetry B 6.89 pKd 130 nM Kd J Med Chem (2022) 65: 2342-2360 [PMID:35007061]
ChEMBL Binding affinity to BRD4 C-terminal bromodomain 2 (unknown origin) expressed in Escherichia coli Bl21(DE3) B 6.92 pKd 120 nM Kd J Med Chem (2018) 61: 9316-9334 [PMID:30253095]
ChEMBL Binding affinity to human BRD4 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by isothermal titration calorimetry-based assay B 7 pKd 100 nM Kd J Med Chem (2018) 61: 504-513 [PMID:28595007]
ChEMBL Binding affinity to recombinant BRD4 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay B 7.04 pKd 92 nM Kd J Med Chem (2020) 63: 5242-5256 [PMID:32255647]
ChEMBL Binding affinity to human His6-tagged BRD4 BD1 (N44 to E168 residues) expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetry method B 7.04 pKd 92 nM Kd ACS Med Chem Lett (2018) 9: 262-267 [PMID:29541371]
ChEMBL Binding affinity to BRD4-BD2 by isothermal titration calorimetry B 7.05 pKd 90.1 nM Kd Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554]
ChEMBL Affinity Biochemical interaction (Isothermal titration calorimetry (ITC)) EUB0000330a BRD4 B 7.05 pKd 90.1 nM Kd Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of human 6x-His-tagged BRD4 bromodomain 2 expressed in Escherichia coli B 7.05 pKd 90 nM Kd J Med Chem (2018) 61: 9316-9334 [PMID:30253095]
ChEMBL Binding affinity to BRD4 BD2 domain (unknown origin) by isothermal titration calorimetry assay B 7.05 pKd 90 nM Kd Eur J Med Chem (2020) 207: 112750-112750 [PMID:32871345]
ChEMBL Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by ITC analysis B 7.15 pKd 71 nM Kd J Med Chem (2021) 64: 15772-15786 [PMID:34710325]
ChEMBL Binding affinity to recombinant BRD4 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay B 7.21 pKd 62 nM Kd J Med Chem (2020) 63: 5242-5256 [PMID:32255647]
ChEMBL Binding affinity to BRD4 by isothermal titration calorimetry B 7.22 pKd 60 nM Kd Bioorg Med Chem (2012) 20: 1878-1886 [PMID:22137933]
ChEMBL Binding affinity to BRD4 BD1 (unknown origin) assessed as dissociation constant by ITC analysis B 7.29 pKd 51 nM Kd Eur J Med Chem (2021) 222: 113588-113588 [PMID:34107385]
GtoPdb Displacement binding constant to recombinant BRD4-BD1 protein. - 7.3 pKd 50 nM Kd Nature (2010) 468: 1067-73 [PMID:20871596]
ChEMBL Binding affinity to BRD4 bromodomain 1 (unknown origin) by isothermal titration calorimetry B 7.3 pKd 50 nM Kd Medchemcomm (2018) 9: 1779-1802 [PMID:30542529]
ChEMBL Binding affinity to BRD4-BD1 by isothermal titration calorimetry B 7.31 pKd 49 nM Kd Bioorg Med Chem (2012) 20: 1878-1886 [PMID:22137933]
ChEMBL Inhibition of human 6x-His-tagged BRD4 bromodomain 1 expressed in Escherichia coli B 7.31 pKd 49 nM Kd J Med Chem (2018) 61: 9316-9334 [PMID:30253095]
ChEMBL Binding affinity to BRD4 isoform 1 B 7.31 pKd 49 nM Kd J Med Chem (2012) 55: 9393-9413 [PMID:22924434]
ChEMBL Binding affinity to BRD4-BD1 by isothermal titration calorimetry B 7.31 pKd 49 nM Kd Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554]
ChEMBL Binding affinity to BRD4 (unknown origin) B 7.31 pKd 49 nM Kd Bioorg Med Chem Lett (2020) 30: 126958-126958 [PMID:32019712]
ChEMBL Binding affinity to BRD4 BD1 domain (unknown origin) by isothermal titration calorimetry assay B 7.31 pKd 49 nM Kd Eur J Med Chem (2020) 207: 112750-112750 [PMID:32871345]
ChEMBL Affinity Biochemical interaction (Isothermal titration calorimetry (ITC)) EUB0000330a BRD4 B 7.31 pKd 49 nM Kd Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by MST assay B 7.46 pKd 35 nM Kd J Med Chem (2021) 64: 15772-15786 [PMID:34710325]
ChEMBL Binding affinity to human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells by isothermal titration calorimetry B 7.47 pKd 34 nM Kd J Med Chem (2016) 59: 1565-1579 [PMID:26731490]
ChEMBL Binding affinity towards BRD4-BD1 (unknown origin) measured by isothermal titration calorimetry (ITC) method B 7.57 pKd 27.2 nM Kd ACS Med Chem Lett (2022) 13: 1621-1627 [PMID:36262390]
ChEMBL Binding affinity to BRD4 D1 (unknown origin) assessed as dissociation constant by isothermal titration calorimetry B 7.72 pKd 19 nM Kd J Med Chem (2022) 65: 2342-2360 [PMID:35007061]
ChEMBL Binding affinity to human BRD4 BD1 (N44 to E168 aa residues) by bromoKdELECT Discover assay B 7.89 pKd 13 nM Kd J Med Chem (2020) 63: 15603-15620 [PMID:33275431]
ChEMBL Binding affinity to biotinylated BRD4 BD1 (44 to 168 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method B 7.89 pKd 12.8 nM Kd J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by qPCR assay B 8.09 pKd 8.2 nM Kd J Med Chem (2021) 64: 15772-15786 [PMID:34710325]
ChEMBL Binding affinity to biotinylated BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method B 8.17 pKd 6.7 nM Kd J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL Binding affinity to human N-terminal His6-tagged BRD4 BD1-BD2 (K57 to K550 residues) after 1 hr using alexa-647 conjugated probe by TR-FRET assay B 7.11 pKi 77 nM Ki J Med Chem (2017) 60: 8369-8384 [PMID:28949521]
ChEMBL Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD4 bromodomain 1 (44 to 168 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay B 7.83 pKi 14.9 nM Ki J Med Chem (2018) 61: 462-481 [PMID:28339196]
ChEMBL Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 1 (44 to 168 residues) expressed in Rosetta2 DE3 cells after 30 mins by Flourescence polarization assay B 7.83 pKi 14.9 nM Ki J Med Chem (2017) 60: 3887-3901 [PMID:28463487]
ChEMBL Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 2 (333 to 460 residues) expressed in Rosetta2 DE3 cells after 30 mins by Flourescence polarization assay B 7.92 pKi 12 nM Ki J Med Chem (2017) 60: 3887-3901 [PMID:28463487]
ChEMBL Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD4 bromodomain 2 (333 to 460 residues) (unknown origin) expressed in Escherichia coli Rosetta2 DE3 after 30 mins by fluorescence polarization assay B 7.92 pKi 12 nM Ki J Med Chem (2018) 61: 462-481 [PMID:28339196]
ChEMBL Displacement of FAM-labeled ZBA248 from BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay B 7.97 pKi 10.7 nM Ki J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL Displacement of FAM-labeled ZBA248 from BRD4 BD1 (44 to 168 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay B 8.12 pKi 7.6 nM Ki J Med Chem (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL Binding affinity to human BRD4 BD1 (44 to 168 residues) by fluorescence polarization assay B 8.28 pKi 5.3 nM Ki J Med Chem (2018) 61: 6685-6704 [PMID:30019901]
ChEMBL Inhibition of BRD4 (unknown origin) by biotinylated-JQ1 based AlphaScreen BRD binding assay B 4.09 pIC50 81500 nM IC50 J Med Chem (2014) 57: 9019-9027 [PMID:25314271]
ChEMBL Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced ISG56 RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis B 5.79 pIC50 1630 nM IC50 Eur J Med Chem (2018) 151: 450-461 [PMID:29649741]
ChEMBL Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced IL-8 RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis B 5.82 pIC50 1510 nM IC50 Eur J Med Chem (2018) 151: 450-461 [PMID:29649741]
ChEMBL Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced grobeta RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis B 5.83 pIC50 1490 nM IC50 Eur J Med Chem (2018) 151: 450-461 [PMID:29649741]
ChEMBL Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced ISG54 RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis B 5.86 pIC50 1380 nM IC50 Eur J Med Chem (2018) 151: 450-461 [PMID:29649741]
ChEMBL Inhibition of BRD4 in poly(I:C)-stimulated human SAECs TLR3-inducible IL-6 gene expression pre-incubated for 24 hrs before poly(I:C) stimulation for 4 hrs by qRT-PCR analysis B 5.99 pIC50 1020 nM IC50 J Med Chem (2020) 63: 5242-5256 [PMID:32255647]
ChEMBL Inhibition of BRD4 in poly(I:C)-stimulated human SAECs TLR3-inducible CIG5 gene expression pre-incubated for 24 hrs before poly(I:C) stimulation for 4 hrs by qRT-PCR analysis B 6.02 pIC50 950 nM IC50 J Med Chem (2020) 63: 5242-5256 [PMID:32255647]
ChEMBL Inhibition of recombinant human N-terminal His-tagged BRD4 bromodomain 1 (49 to 170 residues) expressed in Escherichia coli using biotinylated peptide containing acetylated lysine as substrate pretreated for 15 mins followed by substrate addition after 1 hr by TR-FRET assay B 6.09 pIC50 820 nM IC50 Bioorg Med Chem (2017) 25: 3677-3684 [PMID:28549889]
ChEMBL Displacement of Fl-JQ1 from BRD4 C-terminal bromodomain 2 H437D mutant (unknown origin) expressed in Escherichia coli Bl21(DE3) by fluorescence polarization assay B 6.23 pIC50 590 nM IC50 J Med Chem (2018) 61: 9316-9334 [PMID:30253095]
ChEMBL Inhibition of BRD4 bromodomain 2 (unknown origin) expressed in Escherichia coli Bl21(DE3) by fluorescence anisotropy B 6.31 pIC50 490 nM IC50 J Med Chem (2018) 61: 9316-9334 [PMID:30253095]
ChEMBL Inhibition of BRD4-BD1 (unknown origin) using C-terminal biotinylated tetra-acetylated histone H4 peptide as substrate incubated for 2.5 hrs by alphascreen assay B 6.43 pIC50 370 nM IC50 Bioorg Med Chem (2021) 55: 116592-116592 [PMID:34999525]
ChEMBL Inhibition of fluorescent-tagged ligand from nanoLuc fused full length BRD4 (unknown origin) expressed in 293T cells by luciferase reporter gene based BRET engagement assay B 6.52 pIC50 300 nM IC50 J Med Chem (2018) 61: 9301-9315 [PMID:30289257]
ChEMBL Displacement of APC-labeled biotinylated-avidin from Euphorium-chelated recombinant human BRD4 bromodomain 1 expressed in Escherichia coli preincubated for 15 mins followed by APC-labeled biotinylated-avidin addition and measured after 1 hr under dark condition by TR-FRET assay B 6.7 pIC50 199 nM IC50 J Med Chem (2020) 63: 7186-7210 [PMID:32453591]
ChEMBL Inhibition of biotinylated H4 K5,8,12,16Ac peptide binding to GST-tagged BRD4 bromodomain1 (unknown origin) measured after 60 mins by AlphaScreen assay B 6.77 pIC50 170 nM IC50 Bioorg Med Chem (2019) 27: 1871-1881 [PMID:30926312]
ChEMBL Inhibition of BRD4 (unknown origin) by TR-FRET assay B 6.84 pIC50 144 nM IC50 Medchemcomm (2019) 10: 974-984 [PMID:31303996]
ChEMBL Displacement of APC-labeled biotinylated-avidin from Euphorium-chelated recombinant human BRD4 bromodomain 2 expressed in Escherichia coli preincubated for 15 mins followed by APC-labeled biotinylated-avidin addition and measured after 1 hr under dark condition by TR-FRET assay B 6.9 pIC50 126 nM IC50 J Med Chem (2020) 63: 7186-7210 [PMID:32453591]
ChEMBL Displacement of FITC-conjugated JQ1 from BRD4 BD2 (unknown origin) expressed in Escherichia coli BL21-DE3 rosetta cells incubated for 15 mins by competitive fluorescence polarization assay B 6.91 pIC50 123 nM IC50 J Med Chem (2021) 64: 11637-11650 [PMID:34279939]
ChEMBL Inhibition of His6-tagged human BRD4 bromodomain-1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) using biotinylated-H4KAc4 as substrate by AlphaScreen assay B 6.92 pIC50 120 nM IC50 Eur J Med Chem (2018) 152: 542-559 [PMID:29758518]
ChEMBL Inhibition of human His6-tagged BRD4 bromodomain 1 (N44 to E168 residues) expressed in Escherichia coli BL21(DE3) cells using biotin-H4KAc4 as substrate incubated for 2 hrs by alphascreen assay B 6.92 pIC50 120 nM IC50 J Med Chem (2016) 59: 1565-1579 [PMID:26731490]
ChEMBL Inhibition of human His6-tagged BRD4 BD1 (N44 to E168 residues) expressed in Escherichia coli BL21 (DE3) cells using H-SGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHRK-Biotin-OH as substrate after 2.5 hrs by AlphaScreen assay B 6.92 pIC50 120 nM IC50 ACS Med Chem Lett (2018) 9: 262-267 [PMID:29541371]
ChEMBL Inhibition of BRD4 D2 (unknown origin) by competitive fluorescence anisotropy assay B 7.03 pIC50 94 nM IC50 J Med Chem (2022) 65: 2342-2360 [PMID:35007061]
ChEMBL Inhibition of BRD4 BD1 (unknown origin) after 1 hr by TR-FRET assay B 7.04 pIC50 92 nM IC50 Eur J Med Chem (2018) 151: 450-461 [PMID:29649741]
ChEMBL Inhibition of BRD4 D1 (unknown origin) by competitive fluorescence anisotropy assay B 7.04 pIC50 <92 nM IC50 J Med Chem (2022) 65: 2342-2360 [PMID:35007061]
ChEMBL Binding affinity recombinant human BRD4 BD1 (42 to 168 residues) expressed in Escherichia coli BL21(DE3) incubated for 1 hr by TR-FRET assay B 7.04 pIC50 92 nM IC50 J Med Chem (2022) 65: 2388-2408 [PMID:34982556]
ChEMBL Inhibition of BRD4 BD1 (unknown origin) incubated for 2 hrs by TR-FRET assay B 7.04 pIC50 92 nM IC50 J Med Chem (2021) 64: 18025-18053 [PMID:34908415]
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 7.04 pIC50 91 nM IC50 Eur J Med Chem (2016) 121: 294-299 [PMID:27266999]
ChEMBL Inhibition of BRD4 bromodomain 1/2 (unknown origin) by alphascreen assay B 7.05 pIC50 90 nM IC50 Bioorg Med Chem Lett (2019) 29: 126577-126577 [PMID:31421967]
ChEMBL Inhibition of human BRD4 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 by bromodomain alphascreen peptide displacement assay B 7.05 pIC50 90 nM IC50 Bioorg Med Chem Lett (2016) 26: 2931-2935 [PMID:27142751]
ChEMBL Inhibition of recombinant BRD4 BD2 (unknown origin) incubated for 120 mins by TR-FRET assay B 7.05 pIC50 89 nM IC50 J Med Chem (2021) 64: 17413-17435 [PMID:34813314]
ChEMBL Inhibition of BRD4-BD1 (44 to 168 residues) (unknown origin) using histone H4 peptide as substrate preincubated for 15 mins followed by addition of substrate measured after 60 mins by AlphaScreen assay B 7.06 pIC50 88 nM IC50 Bioorg Med Chem (2017) 25: 2482-2490 [PMID:28314513]
ChEMBL Inhibition of BRD4-BD2 (333 to 460 residues) (unknown origin) using histone H4 peptide as substrate preincubated for 15 mins followed by addition of substrate measured after 60 mins by AlphaScreen assay B