Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL1232461 (Bet inhibitor gsk525762, GSK-525762, GSK525762, GSK-525762A, GSK525762A, I-BET 762, Molibresib) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 |
---|---|---|---|---|---|---|---|---|
ATPase family AAA domain containing 2/ATPase family AAA domain-containing protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2150837] [GtoPdb: 2719] [UniProtKB: Q6PL18] | ||||||||
ChEMBL | Binding affinity to biotinylated ATAD2A (981 to 1108 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method | B | 5 | pKd | >10000 | nM | Kd | J Med Chem (2015) 58: 4927-4939 [PMID:26080064] |
bromodomain containing 2/Bromodomain-containing protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293289] [GtoPdb: 1944] [UniProtKB: P25440] | ||||||||
ChEMBL | Binding affinity to full length N-terminal His6-tagged-BRD2 bromodomain 1 (unknown origin) expressed in competent Escherichia coli BL21(DE3) cells by isothermal titration calorimetry | B | 6.64 | pKd | 230 | nM | Kd | J Med Chem (2016) 59: 1492-1500 [PMID:26367539] |
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 | 6.8 | pKd | 159 | nM | Kd | J Med Chem (2015) 58: 4927-4939 [PMID:26080064] |
ChEMBL | Binding affinity to human partial length BRD2-BD1 (K71 to N194 residues) expressed in bacterial expression system by BROMOscan method | B | 6.96 | pKd | 110 | nM | Kd | Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905] |
ChEMBL | Binding affinity to His6-tagged BRD2 expressed in Escherichia coli by isothermal colorimetric analysis | B | 7 | pKd | 101 | nM | Kd | J Med Chem (2012) 55: 587-596 [PMID:22136469] |
ChEMBL | Binding affinity to full length N-terminal His6-tagged-BRD2 bromodomain 2 (unknown origin) expressed in competent Escherichia coli BL21(DE3) cells by isothermal titration calorimetry | B | 7 | pKd | 100 | nM | Kd | J Med Chem (2016) 59: 1492-1500 [PMID:26367539] |
ChEMBL | Binding affinity to BRD2-BD1,2 by isothermal titration calorimetry | B | 7.21 | pKd | 61.3 | nM | Kd | Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554] |
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 | 7.34 | pKd | 45.4 | nM | Kd | J Med Chem (2015) 58: 4927-4939 [PMID:26080064] |
ChEMBL | Binding affinity to human partial length BRD2-BD2 (E348 to D455 residues) expressed in bacterial expression system by BROMOscan method | B | 7.6 | pKd | 25 | nM | Kd | Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905] |
ChEMBL | Binding affinity to human recombinant BRD2 BD1 (72 to 205 residues) by fluorescence polarization assay | B | 6.82 | pKi | 150 | nM | Ki | Eur J Med Chem (2019) 182: 111633-111633 [PMID:31461688] |
ChEMBL | Binding affinity to human recombinant BRD2 BD2 (349 to 460 residues) by fluorescence polarization assay | B | 7.13 | pKi | 74 | nM | Ki | Eur J Med Chem (2019) 182: 111633-111633 [PMID:31461688] |
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 | 7.25 | pKi | 56.8 | nM | Ki | J Med Chem (2015) 58: 4927-4939 [PMID:26080064] |
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 | 7.31 | pKi | 49.2 | nM | Ki | J Med Chem (2015) 58: 4927-4939 [PMID:26080064] |
ChEMBL | Inhibition of His6-tagged BRD2 expressed in Escherichia coli after 60 mins by fluorescence anisotropy assay | B | 6.09 | pIC50 | 810 | nM | IC50 | J Med Chem (2012) 55: 587-596 [PMID:22136469] |
ChEMBL | Inhibition of BRD2 (unknown origin) by fluorescence anisotrophy | B | 6.1 | pIC50 | 790 | nM | IC50 | J Med Chem (2015) 58: 1281-1297 [PMID:25559428] |
ChEMBL | Inhibition of His6-tagged BRD2 expressed in Escherichia coli assessed as inhibition of binding to SGRG-K(Ac)-GG-K(Ac)-GLG-K(Ac)-GGA-K(Ac)-RHGSGSK-biotin after 1 hr by TR-FRET assay | B | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (2012) 55: 587-596 [PMID:22136469] |
ChEMBL | Displacement of acetylated histone peptide from BRD2-BD1,2 by FRET assay | B | 7.49 | pIC50 | 32.5 | nM | IC50 | Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554] |
ChEMBL | Displacement of tetra-acetylated H4 peptide from human Brd2 bromodomain BD12 after 1 hr by FRET analysis | B | 7.49 | pIC50 | 32.5 | nM | IC50 | J Med Chem (2011) 54: 3827-3838 [PMID:21568322] |
GtoPdb | Displacement of a tetra-acetylated histone H4 peptide from the tandem BET bromodomains of BRD2. | - | 7.49 | pIC50 | 32.5 | nM | IC50 | J Med Chem (2011) 54: 3827-38 [PMID:21568322] |
bromodomain containing 3/Bromodomain-containing protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795186] [GtoPdb: 2725] [UniProtKB: Q15059] | ||||||||
ChEMBL | Binding affinity to His6-tagged BRD3 expressed in Escherichia coli by isothermal colorimetric analysis | B | 7.05 | pKd | 89 | nM | Kd | J Med Chem (2012) 55: 587-596 [PMID:22136469] |
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 | 7.22 | pKd | 60.7 | nM | Kd | J Med Chem (2015) 58: 4927-4939 [PMID:26080064] |
ChEMBL | Binding affinity to BRD3-BD1,2 by isothermal titration calorimetry | B | 7.3 | pKd | 50.5 | nM | Kd | Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554] |
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 | 7.39 | pKd | 40.7 | nM | Kd | J Med Chem (2015) 58: 4927-4939 [PMID:26080064] |
ChEMBL | Binding affinity to human partial length BRD3-BD2 (G306 to P416 residues) expressed in bacterial expression system by BROMOscan method | B | 7.64 | pKd | 23 | nM | Kd | Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905] |
ChEMBL | Binding affinity to human partial length BRD3-BD1 (P24 to E144 residues) expressed in bacterial expression system by BROMOscan method | B | 7.66 | pKd | 22 | nM | Kd | Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905] |
ChEMBL | Binding affinity to human recombinant BRD3 BD2 (306 to 417 residues) by fluorescence polarization assay | B | 7.03 | pKi | 94 | nM | Ki | Eur J Med Chem (2019) 182: 111633-111633 [PMID:31461688] |
ChEMBL | Binding affinity to human recombinant BRD3 BD1 (24 to 144 residues) by fluorescence polarization assay | B | 7.16 | pKi | 68.5 | nM | Ki | Eur J Med Chem (2019) 182: 111633-111633 [PMID:31461688] |
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 | 7.27 | pKi | 53.9 | nM | Ki | 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 | 7.52 | pKi | 30.3 | nM | Ki | J Med Chem (2015) 58: 4927-4939 [PMID:26080064] |
ChEMBL | Inhibition of BRD3 (unknown origin) by fluorescence anisotrophy | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2015) 58: 1281-1297 [PMID:25559428] |
ChEMBL | Inhibition of His6-tagged BRD3 expressed in Escherichia coli after 60 mins by fluorescence anisotropy assay | B | 6.41 | pIC50 | 390 | nM | IC50 | J Med Chem (2012) 55: 587-596 [PMID:22136469] |
ChEMBL | Inhibition of His6-tagged BRD3 expressed in Escherichia coli assessed as inhibition of binding to SGRG-K(Ac)-GG-K(Ac)-GLG-K(Ac)-GGA-K(Ac)-RHGSGSK-biotin after 1 hr by TR-FRET assay | B | 6.8 | pIC50 | 160 | nM | IC50 | J Med Chem (2012) 55: 587-596 [PMID:22136469] |
GtoPdb | Displacement of a tetra-acetylated histone H4 peptide from the tandem BET bromodomains of BRD3. | - | 7.37 | pIC50 | 42.2 | nM | IC50 | J Med Chem (2011) 54: 3827-38 [PMID:21568322] |
ChEMBL | Displacement of acetylated histone peptide from BRD3-BD1,2 by FRET assay | B | 7.37 | pIC50 | 42.4 | nM | IC50 | Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554] |
ChEMBL | Displacement of tetra-acetylated H4 peptide from human Brd3 bromodomain BD12 after 1 hr by FRET analysis | B | 7.37 | pIC50 | 42.4 | nM | IC50 | J Med Chem (2011) 54: 3827-3838 [PMID:21568322] |
bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885] | ||||||||
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 | pKd | 99.4 | nM | Kd | J Med Chem (2015) 58: 4927-4939 [PMID:26080064] |
ChEMBL | Binding affinity to N-terminal His6-tagged-BRD4 bromodomain 1 (unknown origin) expressed in competent Escherichia coli BL21(DE3) cells by isothermal titration calorimetry | B | 7.02 | pKd | 95 | nM | Kd | J Med Chem (2016) 59: 1492-1500 [PMID:26367539] |
ChEMBL | Binding affinity to N-terminal His6-tagged-BRD4 bromodomain 2 (unknown origin) expressed in competent Escherichia coli BL21(DE3) cells by isothermal titration calorimetry | B | 7.19 | pKd | 65 | nM | Kd | J Med Chem (2016) 59: 1492-1500 [PMID:26367539] |
ChEMBL | Binding affinity to BRD4-BD1,2 by isothermal titration calorimetry | B | 7.26 | pKd | 55.2 | nM | Kd | Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554] |
ChEMBL | Binding affinity to His6-tagged BRD4 expressed in Escherichia coli by isothermal colorimetric analysis | B | 7.31 | pKd | 49 | nM | Kd | J Med Chem (2012) 55: 587-596 [PMID:22136469] |
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 | 7.32 | pKd | 47.6 | nM | Kd | J Med Chem (2015) 58: 4927-4939 [PMID:26080064] |
ChEMBL | Binding affinity to human partial length BRD4-BD1 (N44 to E168 residues) expressed in bacterial expression system by BROMOscan method | B | 7.39 | pKd | 41 | nM | Kd | Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905] |
ChEMBL | Displacement of biotinylated acetylated peptide from recombinant human partial length BRD4 long isoform bromodomain 1/2 (N44 to E460 residues) expressed in Escherichia coli BL21 measured after 1 hr by Bromoscan method | B | 7.43 | pKd | 37 | nM | Kd | Bioorg Med Chem Lett (2018) 28: 3483-3488 [PMID:30268702] |
ChEMBL | Competitive binding affinity to human partial length BRD4 (BD1,2) (N44 to E460 residues) expressed in bacterial expression system by BROMOscan assay | B | 7.43 | pKd | 37 | nM | Kd | Bioorg Med Chem Lett (2019) 29: 1220-1226 [PMID:30905542] |
ChEMBL | Binding affinity to human partial length BRD4-BD2 (K333 to E460 residues) expressed in bacterial expression system by BROMOscan method | B | 7.72 | pKd | 19 | nM | Kd | Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905] |
ChEMBL | Inhibition of Cy5-linked JQ1 probe binding to recombinant human N-terminal TEV-cleavable hexa-histidine tagged BRD4 bromodomain1 after 60 mins by HTRF assay | B | 6.7 | pKi | 200 | nM | Ki | Bioorg Med Chem (2019) 27: 457-469 [PMID:30606676] |
ChEMBL | Inhibition of tetra-acetylated Histone H4 peptide binding to recombinant human N-terminal TEV-cleavable hexa-histidine tagged BRD4 bromodomain1 after 60 mins by ALPHA screen assay | B | 6.79 | pKi | 163 | nM | Ki | Bioorg Med Chem (2019) 27: 457-469 [PMID:30606676] |
ChEMBL | Inhibition of Cy5-linked JQ1 probe binding to recombinant human N-terminal TEV-cleavable hexa-histidine tagged BRD4 bromodomain2 after 60 mins by HTRF assay | B | 7.03 | pKi | 94 | nM | Ki | Bioorg Med Chem (2019) 27: 457-469 [PMID:30606676] |
ChEMBL | Binding affinity to human recombinant BRD4 BD1 (44 to 168 residues) by fluorescence polarization assay | B | 7.13 | pKi | 73.5 | nM | Ki | Eur J Med Chem (2019) 182: 111633-111633 [PMID:31461688] |
ChEMBL | Binding affinity to human recombinant BRD4 BD2 (333 to 460 residues) by fluorescence polarization assay | B | 7.18 | pKi | 65.8 | nM | Ki | Eur J Med Chem (2019) 182: 111633-111633 [PMID:31461688] |
ChEMBL | Displacement of Alexa647-labeled JQ1 derivative from wild type BRD4 tandem domain (44 to 460 residues) (unknown origin) incubated for 1 hr by fluorescence polarization assay | B | 7.3 | pKi | 50.12 | nM | Ki | J Med Chem (2016) 59: 7801-7817 [PMID:27528113] |
ChEMBL | Displacement of Alexa647-labeled JQ1 derivative from wild type BRD4 bromodomain 1 (44 to 460 residues) N140A mutant (unknown origin) incubated for 1 hr by fluorescence polarization assay | B | 7.3 | pKi | 50.12 | nM | Ki | J Med Chem (2016) 59: 7801-7817 [PMID:27528113] |
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 | pKi | 46.4 | nM | Ki | J Med Chem (2017) 60: 3887-3901 [PMID:28463487] |
ChEMBL | Displacement of Alexa647-labeled JQ1 derivative from wild type BRD4 bromodomain 2 (44 to 460 residues) N433A mutant (unknown origin) incubated for 1 hr by fluorescence polarization assay | B | 7.4 | pKi | 39.81 | nM | Ki | J Med Chem (2016) 59: 7801-7817 [PMID:27528113] |
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 | 7.41 | pKi | 38.8 | nM | Ki | J Med Chem (2015) 58: 4927-4939 [PMID:26080064] |
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 | 7.49 | pKi | 32.3 | nM | Ki | J Med Chem (2015) 58: 4927-4939 [PMID:26080064] |
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 | 7.64 | pKi | 23 | nM | Ki | J Med Chem (2017) 60: 3887-3901 [PMID:28463487] |
ChEMBL | Inhibition of His6-tagged BRD4 expressed in Escherichia coli after 60 mins by fluorescence anisotropy assay | B | 6.13 | pIC50 | 740 | nM | IC50 | J Med Chem (2012) 55: 587-596 [PMID:22136469] |
ChEMBL | Inhibition of BRD4 bromodomain-1 (unknown origin) by FRET assay | B | 6.2 | pIC50 | 631 | nM | IC50 | Eur J Med Chem (2018) 152: 542-559 [PMID:29758518] |
ChEMBL | Binding affinity to His6-tagged BRD4 (unknown origin) after 60 mins by fluorescence anisotropy binding Assay | B | 6.2 | pIC50 | 630.96 | nM | IC50 | J Med Chem (2013) 56: 7501-7515 [PMID:24015967] |
ChEMBL | Inhibition of BRD4 in human whole blood assessed as reduction in LPS-induced IL-6 secretion preincubated for 30 mins followed by LPS stimulation and measured after 24 hrs by MSD assay | B | 6.2 | pIC50 | 630.96 | nM | IC50 | J Med Chem (2021) 64: 12200-12227 [PMID:34387088] |
ChEMBL | Inhibition of BRD4 (unknown origin) | B | 6.2 | pIC50 | 630 | nM | IC50 | Bioorg Med Chem (2018) 26: 3399-3405 [PMID:29764756] |
ChEMBL | Inhibition of BRD4 (unknown origin) by fluorescence anisotrophy | B | 6.2 | pIC50 | 630 | nM | IC50 | J Med Chem (2015) 58: 1281-1297 [PMID:25559428] |
ChEMBL | Inhibition of BRD4-BD1 (unknown origin) by TR-FRET assay | B | 6.23 | pIC50 | 590 | nM | IC50 | Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905] |
ChEMBL | Inhibition of BRD4 in human MM1S cells assessed as down regulation of c-Myc expression after 1 hr by Western blot analysis | B | 6.48 | pIC50 | 329 | nM | IC50 | Medchemcomm (2018) 9: 1779-1802 [PMID:30542529] |
ChEMBL | Displacement of APC-labeled biotinylated-avidin from Euphorium-chelated recombinant human N-terminal GST-tagged 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 | 6.49 | pIC50 | 320 | nM | IC50 | Bioorg Med Chem (2020) 28: 115601-115601 [PMID:32631570] |
ChEMBL | Inhibition of BRD4 in human PBMC assessed as reduction in LPS-induced IL-6 secretion incubated for 18 to 24 hrs by MSD assay | B | 6.5 | pIC50 | 316.23 | nM | IC50 | J Med Chem (2021) 64: 12200-12227 [PMID:34387088] |
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 | 6.59 | pIC50 | 260 | nM | IC50 | Eur J Med Chem (2017) 137: 176-195 [PMID:28586718] |
ChEMBL | Inhibition of His6-tagged BRD4-BD12 expressed in Escherichia coli assessed as inhibition of binding to SGRG-K(Ac)-GG-K(Ac)-GLG-K(Ac)-GGA-K(Ac)-RHGSGSK-biotin after 1 hr by TR-FRET assay | B | 6.72 | pIC50 | 190 | nM | IC50 | J Med Chem (2012) 55: 587-596 [PMID:22136469] |
ChEMBL | Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrs | B | 6.72 | pIC50 | 190 | nM | IC50 | ACS Med Chem Lett (2013) 4: 835-840 [PMID:24900758] |
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 | 6.81 | pIC50 | 156 | nM | IC50 | J Med Chem (2015) 58: 4927-4939 [PMID:26080064] |
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 | 6.84 | pIC50 | 145 | nM | IC50 | J Med Chem (2017) 60: 3887-3901 [PMID:28463487] |
ChEMBL | Inhibition of BRD4-BD1 in human Raji cells assessed as downregulation of MYC gene expression by PCR method | B | 6.88 | pIC50 | 132 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 1811-1816 [PMID:29657099] |
ChEMBL | Inhibition of His-FLAG-tagged BRD4 binding domain1 (unknown origin) binding to H4-TetraAc-biotin peptide after 20 mins by AlphaLISA | B | 6.92 | pIC50 | 120 | nM | IC50 | ACS Med Chem Lett (2013) 4: 835-840 [PMID:24900758] |
ChEMBL | Displacement of biotinylated tetra-acetylated histone H4 from human his-tagged BRD4 bromodomain1 by FRET assay | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (2016) 59: 1271-1298 [PMID:26572217] |
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 | 7.01 | pIC50 | 98.4 | nM | IC50 | J Med Chem (2015) 58: 4927-4939 [PMID:26080064] |
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 | 7.03 | pIC50 | 93.4 | nM | IC50 | Eur J Med Chem (2018) 150: 156-175 [PMID:29525435] |
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 | 7.11 | pIC50 | 77.5 | nM | IC50 | J Med Chem (2017) 60: 3887-3901 [PMID:28463487] |
ChEMBL | Inhibition of His-tagged human BRD4-BD1 using H4K5acK8acK12acK16ac as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by AlphaScreen assay | B | 7.17 | pIC50 | 68 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 1811-1816 [PMID:29657099] |
ChEMBL | Inhibition of BRD4 BD1-BD2 (unknown origin) using tetraacetylated histone peptide as substrate after 2 hrs by alphascreen assay | B | 7.21 | pIC50 | 61 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4606-4613 [PMID:28939121] |
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 | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2018) 61: 8202-8211 [PMID:30165024] |
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 | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2018) 61: 8202-8211 [PMID:30165024] |
GtoPdb | Displacement of a tetra-acetylated histone H4 peptide from the tandem BET bromodomains of BRD4. | - | 7.44 | pIC50 | 36.1 | nM | IC50 | J Med Chem (2011) 54: 3827-38 [PMID:21568322] |
ChEMBL | Displacement of tetra-acetylated H4 peptide from human Brd4 bromodomain BD12 after 1 hr by FRET analysis | B | 7.44 | pIC50 | 36.1 | nM | IC50 | J Med Chem (2011) 54: 3827-3838 [PMID:21568322] |
ChEMBL | Displacement of acetylated histone peptide from BRD4-BD1,2 by FRET assay | B | 7.44 | pIC50 | 36.1 | nM | IC50 | Bioorg Med Chem (2012) 20: 1887-1892 [PMID:22316554] |
ChEMBL | Binding affinity to human BRD4 1/2 bromodomain by FRET assay | B | 7.44 | pIC50 | 36 | nM | IC50 | J Med Chem (2013) 56: 3217-3227 [PMID:23517011] |
ChEMBL | Inhibition of human His-tagged BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by FRET assay | B | 7.44 | pIC50 | 36 | nM | IC50 | J Med Chem (2016) 59: 1565-1579 [PMID:26731490] |
ChEMBL | Inhibition of human His-tagged BRD4 bromodomain 2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by FRET assay | B | 7.44 | pIC50 | 36 | nM | IC50 | J Med Chem (2016) 59: 1565-1579 [PMID:26731490] |
ChEMBL | Inhibition of recombinant full length human N-terminal His6-tagged BRD4 (2 to 1362 residues) expressed in baculovirus infected insect cells using histone H4 peptide as substrate by alpha screen assay | B | 7.49 | pIC50 | 32.5 | nM | IC50 | Eur J Med Chem (2019) 163: 281-294 [PMID:30529546] |
ChEMBL | Displacement of tetra-acetylated Histone H4 peptide from BRD4 (unknown origin) incubated for 1 hr by FRET analysis | B | 7.49 | pIC50 | 32.5 | nM | IC50 | J Med Chem (2020) 63: 14243-14275 [PMID:32870008] |
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 | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2018) 61: 8202-8211 [PMID:30165024] |
GtoPdb | Measured in a ApoA1 reporter gene assay. | - | 6.15 | pEC50 | 700 | nM | EC50 | J Med Chem (2011) 54: 3827-38 [PMID:21568322] |
ChEMBL | Inhibition of BRD4 in human PBMC assessed as reduction in LPS-induced TNFalpha secretion preincubated for 1 hr followed by LPS-stimulation and measured after 20 hrs by magnetic beads technique based assay | B | 6.36 | pEC50 | 440 | nM | EC50 | Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905] |
bromodomain testis associated/Bromodomain testis-specific protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21] | ||||||||
ChEMBL | Binding affinity to human partial length BRDT-BD1 (N21 to E137 residues) expressed in bacterial expression system by BROMOscan method | B | 6.95 | pKd | 112 | nM | Kd | Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905] |
ChEMBL | Binding affinity to human partial length BRDT-BD2 (K250 to E382 residues) expressed in bacterial expression system by BROMOscan method | B | 7.22 | pKd | 60 | nM | Kd | Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905] |
CREB binding protein/CREB-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793] | ||||||||
ChEMBL | Binding affinity to human partial length CREBBP (R1081 to G1197 residues) expressed in bacterial expression system by BROMOscan method | B | 4.08 | pKd | 83000 | nM | Kd | Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905] |
ChEMBL | Binding affinity to biotinylated CREBBP (1043 to 1159 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method | B | 5 | pKd | >10000 | nM | Kd | J Med Chem (2015) 58: 4927-4939 [PMID:26080064] |
E1A binding protein p300/Histone acetyltransferase p300 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3784] [GtoPdb: 2735] [UniProtKB: Q09472] | ||||||||
ChEMBL | Binding affinity to human partial length EP300 (A1040 to G1161 residues) expressed in bacterial expression system by BROMOscan method | B | 4.15 | pKd | 71000 | nM | Kd | Bioorg Med Chem (2021) 34: 116015-116015 [PMID:33549905] |
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]