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

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ChEMBL ligand: CHEMBL1957266
  • 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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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 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 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 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 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 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 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 (unknown origin) by TR-FRET assay B 7.72 pIC50 19 nM IC50 MedChemComm (2019) 10: 974-984
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]
bromodomain containing 3/Bromodomain-containing protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795186] [GtoPdb: 2725] [UniProtKB: Q15059]
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 BRD3-BD2 by isothermal titration calorimetry B 7.09 pKd 82 nM Kd Bioorg. Med. Chem. (2012) 20: 1887-1892 [PMID:22316554]
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 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 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 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 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 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
bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
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 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 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 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]
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
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 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-BD1 by isothermal titration calorimetry B 7.31 pKd 49 nM Kd Bioorg. Med. Chem. (2012) 20: 1878-1886 [PMID:22137933]
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 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 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 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 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
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 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 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 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 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 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 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 bromodomain1 (unknown origin) using peptide H4 as substrate incubated for 15 mins followed by substrate addition and measured after 1 hr by alphascreen assay B 7.06 pIC50 87 nM IC50 ACS Med Chem Lett (2019) 10: 1680-1685 [PMID:31857846]
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 7.06 pIC50 87 nM IC50 Bioorg Med Chem (2017) 25: 2482-2490 [PMID:28314513]
ChEMBL Inhibition of BRD4 in human HL60 cells assessed as reduction in C-myc production after 24 hrs by ELISA B 7.07 pIC50 86 nM IC50 Bioorg Med Chem (2017) 25: 3677-3684 [PMID:28549889]
ChEMBL Inhibition of biotinylated H4 K5,8,12,16Ac peptide binding to GST-tagged BRD4 bromodomain2 (unknown origin) measured after 60 mins by AlphaScreen assay B 7.1 pIC50 80 nM IC50 Bioorg Med Chem (2019) 27: 1871-1881 [PMID:30926312]
ChEMBL Inhibition of BRD4 bromodomain2 (unknown origin) using peptide H4 as substrate incubated for 15 mins followed by substrate addition and measured after 1 hr by alphascreen assay B 7.1 pIC50 79 nM IC50 ACS Med Chem Lett (2019) 10: 1680-1685 [PMID:31857846]
ChEMBL Inhibition of HSGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHRK(Biotin)-OH binding to recombinant human His6-tagged BRD4 bromodomain 1 expressed in Escherichia coli BL21 (DE3)-R3-pRARE2 cells preincubated for 30 mins followed by HSGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHRK(Biotin)-OH addition and measured after 30 mins by Alphascreen assay B 7.11 pIC50 77 nM IC50 J Med Chem (2020) 63: 3956-3975 [PMID:32208600]
ChEMBL Inhibition of human N-terminal BRD4 bromodomain expressed in Escherichia coli BL21(DE3) after 30 mins by luminescence proximity homogeneous assay B 7.11 pIC50 77 nM IC50 J. Med. Chem. (2012) 55: 587-596 [PMID:22136469]
ChEMBL Binding affinity to human BRD4 bromodomain 1 using H4Ac4 peptide by amplified luminescent proximity homogeneous assay B 7.11 pIC50 77 nM IC50 J. Med. Chem. (2013) 56: 3217-3227 [PMID:23517011]
ChEMBL Inhibition of BRD4 bromodomain 1 (unknown origin)-acetylated histone H4 interaction by luminescence proximity homogeneous assay B 7.11 pIC50 77 nM IC50 MedChemComm (2012) 3: 123-134
ChEMBL Displacement of H4(1-21)KAc5,8,12,16 peptide from BRD4 isoform 1 bead based amplified luminescent proximity homogeneous assay B 7.11 pIC50 77 nM IC50 J. Med. Chem. (2012) 55: 9393-9413 [PMID:22924434]
ChEMBL Inhibition of human His-tagged BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells using biotin-H4K5acK8acK12acK16ac as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by alphascreen assay B 7.11 pIC50 77 nM IC50 J. Med. Chem. (2016) 59: 1565-1579 [PMID:26731490]
ChEMBL Inhibition of BRD4(1) (unknown origin) B 7.11 pIC50 77 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 2931-2935 [PMID:27142751]
ChEMBL Inhibition of BRD4 bromodomain 1 (unknown origin) by alpha-screen method B 7.11 pIC50 77 nM IC50 MedChemComm (2018) 9: 1779-1802
ChEMBL Displacement of acetylated histone peptide from BRD4-BD1 by luminescence proximity homogenous assay B 7.11 pIC50 77 nM IC50 Bioorg. Med. Chem. (2012) 20: 1887-1892 [PMID:22316554]
ChEMBL Inhibition of recombinant human His6-tagged BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells preincubated for 30 mins followed by H4K5acK8acK12acK16ac peptide substrate addition after 30 mins by alphascreen assay B 7.11 pIC50 77 nM IC50 J Med Chem (2017) 60: 4533-4558 [PMID:28195723]
ChEMBL Binding affinity to first bromodomain of BRD4 B 7.11 pIC50 77 nM IC50 ACS Med. Chem. Lett. (2012) 3: 691-694 [PMID:24900532]
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 7.11 pIC50 77 nM IC50 Bioorg Med Chem (2018) 26: 2937-2957 [PMID:29776834]
ChEMBL Inhibition of BRD4 bromodomain-1 (unknown origin) by AlphaScreen assay B 7.11 pIC50 77 nM IC50 Eur J Med Chem (2018) 152: 542-559 [PMID:29758518]
ChEMBL Inhibition of JQ1-FITC binding to His6-tagged BRD4-BD1 (unknown origin) expressed in Escherichia coli BL21 (DE3)-codon plus-RIL cells incubated in dark for 4 hrs by fluorescence anisotropy assay B 7.15 pIC50 70 nM IC50 Eur J Med Chem (2017) 137: 176-195 [PMID:28586718]
ChEMBL Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrs B 7.16 pIC50 69 nM IC50 ACS Med. Chem. Lett. (2013) 4: 835-840 [PMID:24900758]
ChEMBL Inhibition of human recombinant His-tagged BRD4 BD2 domain using H-SGRGK(Ac)GGK(Ac)GLGK-(Ac)GGAK(Ac)RHRK(Biotin)-OH as substrate preincubated with enzyme for 30 mins followed by substrate addition measured after 30 mins by AlphaScreen assay B 7.16 pIC50 69 nM IC50 J Med Chem (2020) 63: 3678-3700 [PMID:32153186]
ChEMBL Inhibition of BRD4 BD2 (unknown origin) after 1 hr by TR-FRET assay B 7.21 pIC50 62 nM IC50 Eur J Med Chem (2018) 151: 450-461 [PMID:29649741]
ChEMBL Inhibition of BRD4-BD1 in human Raji cells assessed as downregulation of MYC gene expression by PCR method B 7.22 pIC50 60 nM IC50 Bioorg Med Chem Lett (2018) 28: 1811-1816 [PMID:29657099]
ChEMBL Inhibition of N-terminal His-tagged BRD4 (BD1) (unknown origin) using biotinylated tetra-acetylated histone H4 peptide after 30 mins by alpha-screen assay B 7.22 pIC50 60 nM IC50 J Med Chem (2018) 61: 8202-8211 [PMID:30165024]
ChEMBL Inhibition of BRD4(1) (unknown origin) incubated for 4 hrs by (+)-JQ1 fluorescent ligand based fluorescence anisotrophy B 7.24 pIC50 58 nM IC50 J. Med. Chem. (2015) 58: 1281-1297 [PMID:25559428]
ChEMBL Displacement of (+)-JQ1 from 6H-Thr BRD4 Y97A mutant BD2 (unknown origin) after 30 mins by TR-FRET assay B 7.3 pIC50 50.12 nM IC50 J Med Chem (2018) 61: 4317-4334 [PMID:29656650]
ChEMBL Inhibition of N-terminal His-tagged BRD4 (BD1/BD2) (unknown origin) using biotinylated tetra-acetylated histone H4 peptide after 30 mins by alpha-screen assay B 7.3 pIC50 50 nM IC50 J Med Chem (2018) 61: 8202-8211 [PMID:30165024]
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 7.33 pIC50 46.7 nM IC50 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 7.33 pIC50 46.7 nM IC50 J Med Chem (2017) 60: 3887-3901 [PMID:28463487]
ChEMBL Displacement of tetra-acetylated histone H4 peptide (1-21) from recombinant human N-terminal His-tagged BRD4 BD1 (44 to 170 residues) expressed in Escherichia coli incubated for 30 mins followed by further incubation with tetra-acetylated histone H4 peptide (1-21) for 30 mins by Alphascreen assay B 7.37 pIC50 42.24 nM IC50 J Med Chem (2019) 62: 11080-11107 [PMID:31789032]
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 7.37 pIC50 42.2 nM IC50 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 7.37 pIC50 42.2 nM IC50 J Med Chem (2018) 61: 462-481 [PMID:28339196]
ChEMBL Inhibition of N-terminal His-tagged BRD4 (BD2) (unknown origin) using biotinylated tetra-acetylated histone H4 peptide after 30 mins by alpha-screen assay B 7.4 pIC50 40 nM IC50 J Med Chem (2018) 61: 8202-8211 [PMID:30165024]
ChEMBL Inhibition of recombinant human His-tagged BRD4 bromodomain 1/2 (2 to 1362 residues) expressed in s9f insect cells using biotinylated H4(1 to 21)K5/8/12/16Ac peptide as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by Alpha screen assay B 7.4 pIC50 40 nM IC50 Eur J Med Chem (2019) 179: 502-514 [PMID:31276895]
ChEMBL Displacement of (+)-JQ1 from 6H-Thr BRD4 Y390A mutant BD1 (unknown origin) after 30 mins by TR-FRET assay B 7.4 pIC50 39.81 nM IC50 J Med Chem (2018) 61: 4317-4334 [PMID:29656650]
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 7.45 pIC50 35.7 nM IC50 J. Med. Chem. (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL Inhibition of recombinant human His6-tagged BRD4 bromodomain 2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells preincubated for 30 mins followed by HSGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHRK(Biotin)-OH peptide substrate addition after 30 mins by alphascreen assay B 7.48 pIC50 33 nM IC50 J Med Chem (2017) 60: 4533-4558 [PMID:28195723]
ChEMBL Displacement of acetylated histone peptide from BRD4-BD2 by luminescence proximity homogenous assay B 7.48 pIC50 33 nM IC50 Bioorg. Med. Chem. (2012) 20: 1887-1892 [PMID:22316554]
ChEMBL Inhibition of human C-terminal BRD4 bromodomain expressed in Escherichia coli BL21(DE3) after 30 mins by luminescence proximity homogeneous assay B 7.48 pIC50 33 nM IC50 J. Med. Chem. (2012) 55: 587-596 [PMID:22136469]
ChEMBL Inhibition of BRD4 bromodomain 2 (unknown origin)-acetylated histone H4 interaction by luminescence proximity homogeneous assay B 7.48 pIC50 33 nM IC50 MedChemComm (2012) 3: 123-134
ChEMBL Inhibition of BRD4 (unknown origin) B 7.48 pIC50 33 nM IC50 Bioorg Med Chem Lett (2017) 27: 4051-4055 [PMID:28765013]
ChEMBL Inhibition of human recombinant N-terminal 6his-tagged BRD4 expressed in Escherichia coli BL21(DE3) using H4 peptide as substrate by alphascreen assay B 7.48 pIC50 33 nM IC50 Bioorg Med Chem Lett (2019) 29: 126577-126577 [PMID:31421967]
ChEMBL Inhibition of BRD4-BD1 (unknown origin) incubated for 1 hr by AlphaScreen biotin-JQ1 competition assay B 7.49 pIC50 32 nM IC50 J Med Chem (2018) 61: 7785-7795 [PMID:30125504]
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 7.54 pIC50 28.7 nM IC50 J. Med. Chem. (2015) 58: 4927-4939 [PMID:26080064]
ChEMBL Displacement of 5-FITC labelled (+)-JQ1 from His6-tagged human BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3) )-codon plus-RIL cells incubated for 4 hrs in dark condition by fluorescence anisotropy binding assay B 7.55 pIC50 28.5 nM IC50 J Med Chem (2019) 62: 8642-8663 [PMID:31490070]
ChEMBL Displacement of FITC-JQ1 from His6-tagged BRD4 bromodomain-1 (unknown origin) expressed in Escherichia coli BL21(DE3) after 4 hrs by fluorescence anisotropy method B 7.55 pIC50 28.5 nM IC50 Eur J Med Chem (2018) 150: 156-175 [PMID:29525435]
ChEMBL Displacement of 5-FITC labelled (+)-JQ1 from His6-tagged human BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3) )-codon plus-RIL cells incubated for 4 hrs in dark condition by fluorescence anisotropy binding assay B 7.55 pIC50 28.5 nM IC50 J Med Chem (2019) 62: 8642-8663 [PMID:31490070]
ChEMBL Displacement of tetra-acetylated histone H4 peptide (1-21) from recombinant human N-terminal His-tagged BRD4 BD2 (349 to 460 residues) expressed in Escherichia coli incubated for 30 mins followed by further incubation with tetra-acetylated histone H4 peptide (1-21) for 30 mins by Alphascreen assay B 7.61 pIC50 24.71 nM IC50 J Med Chem (2019) 62: 11080-11107 [PMID:31789032]
ChEMBL Displacement of biotinylated tetra-acetylated histone H4 from human his-tagged BRD4 bromodomain1 by alphascreen assay B 7.62 pIC50 24 nM IC50 J. Med. Chem. (2016) 59: 1271-1298 [PMID:26572217]
ChEMBL Inhibition of His-FLAG-tagged BRD4 binding domain1 (unknown origin) binding to H4-TetraAc-biotin peptide after 20 mins by AlphaLISA B 7.62 pIC50 24 nM IC50 ACS Med. Chem. Lett. (2013) 4: 835-840 [PMID:24900758]
ChEMBL Binding affinity to human BRD4 BD1 (44 to 168 residues) by fluorescence polarization assay B 7.66 pIC50 22 nM IC50 J Med Chem (2018) 61: 6685-6704 [PMID:30019901]
ChEMBL Inhibition of human recombinant His-tagged BRD4 BD1 domain using H-SGRGK(Ac)GGK(Ac)GLGK-(Ac)GGAK(Ac)RHRK(Biotin)-OH as substrate preincubated with enzyme for 30 mins followed by substrate addition measured after 30 mins by AlphaScreen assay B 7.66 pIC50 22 nM IC50 J Med Chem (2020) 63: 3678-3700 [PMID:32153186]
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 7.68 pIC50 21 nM IC50 Eur J Med Chem (2016) 121: 294-299 [PMID:27266999]
ChEMBL Alpha Assay: BRD4(1): Assays were performed as described previously with minor modifications from the manufacturer's protocol (PerkinElmer, USA). All reagents were diluted in 50 mM HEPES, 100 mM NaCl, 0.1% BSA, pH 7.4 supplemented with 0.05% CHAPS and allowed to equilibrate to room temperature prior to addition to plates. A 24-point 1:2 serial dilution of the ligands was prepared over the range of 150-0 μM and 4 μl transferred to low-volume 384-well plates (ProxiPlate™-384 Plus, PerkinElmer, USA), followed by 4 μl of HIS-tagged protein (BRD4/1, 250 nM, BRD4/2 and CREBBP, 2000 nM). Plates were sealed and incubated at room temperature for 30 minutes, before the addition of 4 μl of biotinylated peptide at equimolar concentration to the protein [peptide for BRD4(1) & BRD4(2): H4K5acK8acK12acK16ac, H-SGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHRK(Biotin)-OH (SEQ ID NO: 5); peptide for CREBBP: H3K36ac, Biotin-KSAPATGGVK(Ac)KPHRYRPGT-OH (SEQ ID NO: 6) (Cambridge Research Biochemicals, UK)]. Plates were sealed and incubated for a further 30 minutes, before the addition of 4 μl of streptavidin-coated donor beads (25 μg/ml) and 4 μl nickel chelate acceptor beads (25 μg/ml) under low light conditions. Plates were foil-sealed to protect from light, incubated at room temperature for 60 minutes and read on a PHERAstar FS plate reader (BMG Labtech, Germany) using an AlphaScreen 680 excitation/570 emission filter set. IC50 values were calculated in Prism 5 (GraphPad Software, USA) after normalization against corresponding DMSO controls and are given as the final concentration of compound in the 20 μl reaction volume. B 7.74 pIC50 18 nM IC50 US-9320741-B2. Compositions and methods for treating neoplasia, inflammatory disease and other disorders (2016)
ChEMBL Alpha Assay: BRD4(2): Assays were performed as described previously with minor modifications from the manufacturer's protocol (PerkinElmer, USA). All reagents were diluted in 50 mM HEPES, 100 mM NaCl, 0.1% BSA, pH 7.4 supplemented with 0.05% CHAPS and allowed to equilibrate to room temperature prior to addition to plates. A 24-point 1:2 serial dilution of the ligands was prepared over the range of 150-0 μM and 4 μl transferred to low-volume 384-well plates (ProxiPlate™-384 Plus, PerkinElmer, USA), followed by 4 μl of HIS-tagged protein (BRD4/1, 250 nM, BRD4/2 and CREBBP, 2000 nM). Plates were sealed and incubated at room temperature for 30 minutes, before the addition of 4 μl of biotinylated peptide at equimolar concentration to the protein [peptide for BRD4(1) & BRD4(2): H4K5acK8acK12acK16ac, H-SGRGK(Ac)GGK(Ac)GLGK(Ac)GGAK(Ac)RHRK(Biotin)-OH (SEQ ID NO: 5); peptide for CREBBP: H3K36ac, Biotin-KSAPATGGVK(Ac)KPHRYRPGT-OH (SEQ ID NO: 6) (Cambridge Research Biochemicals, UK)]. Plates were sealed and incubated for a further 30 minutes, before the addition of 4 μl of streptavidin-coated donor beads (25 μg/ml) and 4 μl nickel chelate acceptor beads (25 μg/ml) under low light conditions. Plates were foil-sealed to protect from light, incubated at room temperature for 60 minutes and read on a PHERAstar FS plate reader (BMG Labtech, Germany) using an AlphaScreen 680 excitation/570 emission filter set. IC50 values were calculated in Prism 5 (GraphPad Software, USA) after normalization against corresponding DMSO controls and are given as the final concentration of compound in the 20 μl reaction volume. B 7.85 pIC50 14 nM IC50 US-9320741-B2. Compositions and methods for treating neoplasia, inflammatory disease and other disorders (2016)
ChEMBL Inhibition of BRD4 bromodomain-1 (unknown origin) by europium based LANCE TR-FRET assay B 8.1 pIC50 8 nM IC50 Bioorg. Med. Chem. (2015) 23: 953-959 [PMID:25678016]
ChEMBL Inhibition of BRD4 in human H1299 cells assessed as decrease in HPV LCR-E2-EP400-mediated transcriptional repression after 24 hrs by Bright-Glo luciferase reporter gene assay B 6.82 pEC50 153 nM EC50 J Med Chem (2017) 60: 8369-8384 [PMID:28949521]
ChEMBL Inhibition of BRD4 in human MX1 cells assessed as decrease in cell proliferation after 3 days by Celltiter-Glo assay B 6.84 pEC50 144 nM EC50 MedChemComm (2019) 10: 974-984
ChEMBL Inhibition of BRD4 in human H1229 cells transfected with HPV-E2 assessed as transrepression of HPV-long control region by luciferase reporter assay B 7.19 pEC50 64 nM EC50 MedChemComm (2019) 10: 974-984
bromodomain testis associated/Bromodomain testis-specific protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21]
ChEMBL Binding affinity to recombinant BRDT BD2 (unknown origin) incubated for 1 hr by TR-FRET assay B 6.66 pKd 217 nM Kd J Med Chem (2020) 63: 5242-5256 [PMID:32255647]
ChEMBL