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: CHEMBL2393130 (Apabetalone, RVX-000222, RVX000222, RVX-208) |
---|
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 |
---|---|---|---|---|---|---|---|---|
bromodomain containing 2/Bromodomain-containing protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293289] [GtoPdb: 1944] [UniProtKB: P25440] | ||||||||
ChEMBL | Binding affinity to human BRD2 bromodomain 1 by isothermal titration calorimetry | B | 4.77 | pKd | 16900 | nM | Kd | J Med Chem (2016) 59: 1492-1500 [PMID:26367539] |
ChEMBL | Inhibition of human 6x-His-tagged BRD2 bromodomain 1 expressed in Escherichia coli | B | 5.24 | pKd | 5800 | nM | Kd | J Med Chem (2018) 61: 9316-9334 [PMID:30253095] |
ChEMBL | Binding affinity to human BRD2 bromodomain 1 expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetry | B | 5.24 | pKd | 5800 | nM | Kd | J Med Chem (2016) 59: 1492-1500 [PMID:26367539] |
ChEMBL | Binding affinity to recombinant BRD2 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay | B | 5.24 | pKd | 5780 | nM | Kd | J Med Chem (2020) 63: 5242-5256 [PMID:32255647] |
ChEMBL | Inhibition of recombinant human His6-tagged BRD2 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells | B | 5.24 | pKd | 5780 | nM | Kd | J Med Chem (2017) 60: 4533-4558 [PMID:28195723] |
ChEMBL | Binding affinity to recombinant BRD2 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay | B | 6.6 | pKd | 251 | nM | Kd | J Med Chem (2020) 63: 5242-5256 [PMID:32255647] |
ChEMBL | Inhibition of recombinant human His6-tagged BRD2 bromodomain 2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells | B | 6.6 | pKd | 251 | nM | Kd | J Med Chem (2017) 60: 4533-4558 [PMID:28195723] |
ChEMBL | Inhibition of human 6x-His-tagged BRD2 bromodomain 2 expressed in Escherichia coli | B | 6.6 | pKd | 250 | nM | Kd | J Med Chem (2018) 61: 9316-9334 [PMID:30253095] |
ChEMBL | Binding affinity to human BRD2 bromodomain 2 expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetry | B | 6.6 | pKd | 250 | nM | Kd | J Med Chem (2016) 59: 1492-1500 [PMID:26367539] |
ChEMBL | Binding affinity to human BRD2 bromodomain 2 by isothermal titration calorimetry | B | 6.69 | pKd | 206 | nM | Kd | J Med Chem (2016) 59: 1492-1500 [PMID:26367539] |
ChEMBL | Inhibition of BRD2 BD1 (unknown origin) after 1 hr by TR-FRET assay | B | 5.24 | pIC50 | 5780 | 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 | 5.24 | pIC50 | 5697 | nM | IC50 | J Med Chem (2022) 65: 2388-2408 [PMID:34982556] |
ChEMBL | Inhibition of BRD2 BD2 (unknown origin) after 1 hr by TR-FRET assay | B | 6.6 | pIC50 | 251 | nM | IC50 | Eur J Med Chem (2018) 151: 450-461 [PMID:29649741] |
ChEMBL | Binding affinity BRD2 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay | B | 6.61 | pIC50 | 246 | nM | IC50 | J Med Chem (2022) 65: 2388-2408 [PMID:34982556] |
GtoPdb | Measured using a TR-FRET assay to evaluate binding to BD2 of BRD2. | - | 7.05 | pIC50 | 90 | nM | IC50 | PLoS ONE (2013) 8: e83190 [PMID:24391744] |
bromodomain containing 3/Bromodomain-containing protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795186] [GtoPdb: 2725] [UniProtKB: Q15059] | ||||||||
ChEMBL | Inhibition of recombinant human His6-tagged BRD3 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells | B | 5.39 | pKd | 4065 | nM | Kd | J Med Chem (2017) 60: 4533-4558 [PMID:28195723] |
ChEMBL | Binding affinity to human BRD3 BD2 by ITC method | B | 5.4 | pKd | 4000 | nM | Kd | J Med Chem (2018) 61: 4317-4334 [PMID:29656650] |
ChEMBL | Inhibition of human 6x-His-tagged BRD3 bromodomain 1 expressed in Escherichia coli | B | 5.4 | pKd | 4000 | 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 | 5.4 | pKd | 3962 | 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 | 6.69 | pKd | 203 | nM | Kd | J Med Chem (2020) 63: 5242-5256 [PMID:32255647] |
ChEMBL | Inhibition of recombinant human His6-tagged BRD3 bromodomain 2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells | B | 6.71 | pKd | 195 | nM | Kd | J Med Chem (2017) 60: 4533-4558 [PMID:28195723] |
ChEMBL | Inhibition of human 6x-His-tagged BRD3 bromodomain 2 expressed in Escherichia coli | B | 6.72 | pKd | 190 | nM | Kd | J Med Chem (2018) 61: 9316-9334 [PMID:30253095] |
GtoPdb | AlphaScreen data for bromodomain 1 of BRD3. | - | 4.06 | pIC50 | 87000 | nM | IC50 | Proc Natl Acad Sci USA (2013) 110: 19754-9 [PMID:24248379] |
ChEMBL | Displacement of tetra-acetylated histone H4 peptide from recombinant human His-tagged BRD3 BD1 expressed in bacterial expression system by alphascreen assay | B | 4.06 | pIC50 | 87000 | nM | IC50 | J Med Chem (2019) 62: 11080-11107 [PMID:31789032] |
ChEMBL | Binding affinity to BRD3 BD1 (unknown origin) by alphascreen assay | B | 4.06 | pIC50 | 87000 | nM | IC50 | Eur J Med Chem (2021) 226: 113853-113853 [PMID:34547507] |
GtoPdb | AlphaScreen data assessing the bromodomain 2 domain of BRD3. | - | 5.31 | pIC50 | 4900 | nM | IC50 | Proc Natl Acad Sci USA (2013) 110: 19754-9 [PMID:24248379] |
ChEMBL | Inhibition of BRD3 BD1 (unknown origin) after 1 hr by TR-FRET assay | B | 5.4 | pIC50 | 3962 | nM | IC50 | Eur J Med Chem (2018) 151: 450-461 [PMID:29649741] |
ChEMBL | Binding affinity BRD3 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay | B | 5.41 | pIC50 | 3878 | nM | IC50 | J Med Chem (2022) 65: 2388-2408 [PMID:34982556] |
ChEMBL | Binding affinity to BRD3 BD2 (unknown origin) by alphascreen assay | B | 6.29 | pIC50 | 510 | nM | IC50 | Eur J Med Chem (2021) 226: 113853-113853 [PMID:34547507] |
ChEMBL | Displacement of tetra-acetylated histone H4 peptide from recombinant human His-tagged BRD3 BD2 expressed in bacterial expression system by alphascreen assay | B | 6.29 | pIC50 | 510 | nM | IC50 | J Med Chem (2019) 62: 11080-11107 [PMID:31789032] |
ChEMBL | Inhibition of human His-tagged BRD3 bromodomain 2 using biotin-H4K5acK8acK12acK16ac as substrate incubated for 30 mins by alphascreen assay | B | 6.29 | pIC50 | 510 | nM | IC50 | J Med Chem (2016) 59: 1565-1579 [PMID:26731490] |
GtoPdb | Measured using a TR-FRET assay to evaluate binding to BD2 of BRD3. | - | 6.55 | pIC50 | 280 | nM | IC50 | PLoS ONE (2013) 8: e83190 [PMID:24391744] |
ChEMBL | Binding affinity BRD3 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay | B | 6.66 | pIC50 | 217 | 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 | 6.69 | pIC50 | 203 | nM | IC50 | Eur J Med Chem (2018) 151: 450-461 [PMID:29649741] |
bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885] | ||||||||
ChEMBL | Binding affinity to human BRD4 bromodomain 1 by isothermal titration calorimetry | B | 5.05 | pKd | 8930 | nM | Kd | J Med Chem (2016) 59: 1492-1500 [PMID:26367539] |
ChEMBL | Inhibition of BRD4-BD1 (unknown origin) assessed as dissociation constant by ITC method | B | 5.39 | pKd | 4100 | nM | Kd | J Med Chem (2022) 65: 5660-5674 [PMID:35348328] |
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 | 5.94 | pKd | 1142 | nM | Kd | J Med Chem (2017) 60: 4533-4558 [PMID:28195723] |
ChEMBL | Binding affinity to human BRD4 BD1 by isothermal calorimetry analysis | B | 5.94 | pKd | 1142 | nM | Kd | J Med Chem (2020) 63: 5585-5623 [PMID:32324999] |
ChEMBL | Binding affinity to BRD4 BD1 (unknown origin) by isothermal titration calorimetry | B | 5.94 | pKd | 1142 | nM | Kd | Eur J Med Chem (2022) 227: 113953-113953 [PMID:34731760] |
ChEMBL | Binding affinity to human BRD4 BD1 assessed as dissociation constant by ITC analysis | B | 5.94 | pKd | 1142 | nM | Kd | Eur J Med Chem (2022) 238: 114423-114423 [PMID:35544982] |
ChEMBL | Binding affinity to recombinant BRD4 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay | B | 5.94 | pKd | 1142 | nM | Kd | J Med Chem (2020) 63: 5242-5256 [PMID:32255647] |
ChEMBL | Binding affinity to human BRD4 bromodomain 1 expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetry | B | 5.96 | pKd | 1100 | nM | Kd | J Med Chem (2016) 59: 1492-1500 [PMID:26367539] |
ChEMBL | Inhibition of human 6x-His-tagged BRD4 bromodomain 1 expressed in Escherichia coli | B | 5.96 | pKd | 1100 | nM | Kd | J Med Chem (2018) 61: 9316-9334 [PMID:30253095] |
ChEMBL | Binding affinity to BRD4 bromodomain 1 (unknown origin) by isothermal titration calorimetric analysis | B | 5.96 | pKd | 1100 | nM | Kd | J Med Chem (2016) 59: 1271-1298 [PMID:26572217] |
ChEMBL | Binding affinity to human BRD4 bromodomain 2 by isothermal titration calorimetry | B | 6.52 | pKd | 303 | nM | Kd | J Med Chem (2016) 59: 1492-1500 [PMID:26367539] |
ChEMBL | Inhibition of BRD4-BD2 (unknown origin) assessed as dissociation constant by ITC method | B | 6.7 | pKd | 200 | nM | Kd | J Med Chem (2022) 65: 5660-5674 [PMID:35348328] |
ChEMBL | Binding affinity to BRD4 bromodomain 2 (unknown origin) by isothermal titration calorimetric analysis | B | 6.85 | pKd | 140 | nM | Kd | J Med Chem (2016) 59: 1271-1298 [PMID:26572217] |
ChEMBL | Binding affinity to human BRD4 bromodomain 2 expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetry | B | 6.85 | pKd | 140 | nM | Kd | J Med Chem (2016) 59: 1492-1500 [PMID:26367539] |
ChEMBL | Binding affinity to BRD4 BD2 (unknown origin) | B | 6.87 | pKd | 135 | nM | Kd | Eur J Med Chem (2021) 213: 113137-113137 [PMID:33460833] |
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 | 6.87 | pKd | 135 | nM | Kd | J Med Chem (2017) 60: 4533-4558 [PMID:28195723] |
ChEMBL | Binding affinity to human BRD4 BD2 by isothermal calorimetry analysis | B | 6.87 | pKd | 135 | nM | Kd | J Med Chem (2020) 63: 5585-5623 [PMID:32324999] |
ChEMBL | Binding affinity to recombinant BRD4 BD2 (unknown origin) incubated for 1 hr by TR-FRET assay | B | 6.87 | pKd | 135 | nM | Kd | J Med Chem (2020) 63: 5242-5256 [PMID:32255647] |
ChEMBL | Binding affinity to N-terminal His-tagged BRD4 BD2 (unknown origin) by isothermal calorimetric titration assay | B | 6.87 | pKd | 135 | nM | Kd | J Med Chem (2020) 63: 9070-9092 [PMID:32691591] |
ChEMBL | Binding affinity to human BRD4 BD2 assessed as dissociation constant by ITC analysis | B | 6.87 | pKd | 135 | nM | Kd | Eur J Med Chem (2022) 238: 114423-114423 [PMID:35544982] |
ChEMBL | Binding affinity to BRD4 BD2 (unknown origin) by isothermal titration calorimetry | B | 6.87 | pKd | 135 | nM | Kd | Eur J Med Chem (2022) 227: 113953-113953 [PMID:34731760] |
ChEMBL | Inhibition of human 6x-His-tagged BRD4 bromodomain 2 expressed in Escherichia coli | B | 6.89 | pKd | 130 | nM | Kd | J Med Chem (2018) 61: 9316-9334 [PMID:30253095] |
ChEMBL | Inhibition of BRD4 (unknown origin) | B | 4.9 | pIC50 | 12700 | nM | IC50 | Eur J Med Chem (2022) 230: 114094-114094 [PMID:34998039] |
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 | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2016) 121: 294-299 [PMID:27266999] |
ChEMBL | Inhibition of His/thioredoxin-tagged human recombinant BRD4 bromodomain-1 (43 to 166 residues) expressed in Escherichia coli BL21 Star (DE3) pre-incubated for 30 mins followed by biotinylated histone peptide H4 addition measured after 30 mins by AlphaScreen assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 9990-10012 [PMID:29172540] |
ChEMBL | Displacement of (+)-JQ1 from 6H-Thr BRD4 Y390A mutant BD1 (unknown origin) after 30 mins by TR-FRET assay | B | 5.2 | pIC50 | 6309.57 | nM | IC50 | J Med Chem (2018) 61: 4317-4334 [PMID:29656650] |
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 | 5.41 | pIC50 | 3850 | 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 | 5.43 | pIC50 | 3730 | 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 | 5.48 | pIC50 | 3290 | nM | IC50 | J Med Chem (2020) 63: 5242-5256 [PMID:32255647] |
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 | 5.51 | pIC50 | 3100 | nM | IC50 | Bioorg Med Chem (2019) 27: 1871-1881 [PMID:30926312] |
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 | 5.56 | pIC50 | 2740 | 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 | 5.58 | pIC50 | 2630 | nM | IC50 | Eur J Med Chem (2018) 151: 450-461 [PMID:29649741] |
ChEMBL | Inhibition of GST-tagged BRD4 bromodomain (unknown origin) using biotinylated histone H4KAc peptide (1 to 21 residues) as substrate by HTRF assay | B | 5.61 | pIC50 | 2450 | nM | IC50 | J Med Chem (2020) 63: 3678-3700 [PMID:32153186] |
ChEMBL | Inhibition of human BRD4 bromo domain 1 | B | 5.7 | pIC50 | 1985 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4051-4055 [PMID:28765013] |
ChEMBL | Displacement of tetra-acetylated histone H4 peptide from recombinant human N-terminal His-tagged BRD4 BD1 incubated for 2 hrs by TR-FRET assay | B | 5.74 | pIC50 | 1800 | nM | IC50 | J Med Chem (2019) 62: 11080-11107 [PMID:31789032] |
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 | 5.78 | pIC50 | 1660 | nM | IC50 | J Med Chem (2020) 63: 5242-5256 [PMID:32255647] |
ChEMBL | Displacement of (+)-JQ1 from 6H-Thr BRD4 Y97A mutant BD2 (unknown origin) after 30 mins by TR-FRET assay | B | 5.8 | pIC50 | 1584.89 | nM | IC50 | J Med Chem (2018) 61: 4317-4334 [PMID:29656650] |
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 | 5.94 | pIC50 | 1151 | nM | IC50 | J Med Chem (2022) 65: 2388-2408 [PMID:34982556] |
ChEMBL | Inhibition of BRD4 BD1 (unknown origin) after 1 hr by TR-FRET assay | B | 5.94 | pIC50 | 1142 | nM | IC50 | Eur J Med Chem (2018) 151: 450-461 [PMID:29649741] |
ChEMBL | Inhibition of BRD4 bromodomain-1 (unknown origin) by europium based LANCE TR-FRET assay | B | 6.19 | pIC50 | 645 | nM | IC50 | Bioorg Med Chem (2015) 23: 953-959 [PMID:25678016] |
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 | 6.21 | pIC50 | 610 | nM | IC50 | Eur J Med Chem (2016) 121: 294-299 [PMID:27266999] |
ChEMBL | Inhibition of human BRD4 bromodomain2 by Alphascreen assay | B | 6.29 | pIC50 | 510 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4051-4055 [PMID:28765013] |
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 | 6.29 | pIC50 | 510 | nM | IC50 | Eur J Med Chem (2019) 163: 281-294 [PMID:30529546] |
ChEMBL | Inhibition of human recombinant N-terminal 6his-tagged BRD4 bromodomain 2 expressed in Escherichia coli BL21(DE3) using using H4 peptide as substrate by alphascreen assay | B | 6.29 | pIC50 | 510 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126577-126577 [PMID:31421967] |
ChEMBL | Inhibition of BRD4 (unknown origin) | B | 6.85 | pIC50 | 140 | nM | IC50 | Eur J Med Chem (2020) 186: 111852-111852 [PMID:31759729] |
ChEMBL | Inhibition of BRD4 BD2 (unknown origin) after 1 hr by TR-FRET assay | B | 6.87 | pIC50 | 135 | nM | IC50 | Eur J Med Chem (2018) 151: 450-461 [PMID:29649741] |
ChEMBL | Binding affinity human BRD4 BD2 incubated for 1 hr by TR-FRET assay | B | 6.88 | pIC50 | 132 | nM | IC50 | J Med Chem (2022) 65: 2388-2408 [PMID:34982556] |
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 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem (2019) 27: 1871-1881 [PMID:30926312] |
ChEMBL | Inhibition of human BRD4 bromo domain 2 | B | 7.17 | pIC50 | 67 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4051-4055 [PMID:28765013] |
ChEMBL | Inhibition of BRD4 bromodomain 2 (unknown origin) incubated for 30 mins by ELISA | B | 7.36 | pIC50 | 43.8 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 2168-2172 [PMID:31257080] |
ChEMBL | Displacement of tetra-acetylated histone H4 peptide from recombinant human N-terminal His-tagged BRD4 BD2 incubated for 2 hrs by TR-FRET assay | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2019) 62: 11080-11107 [PMID:31789032] |
GtoPdb | Measured using a TR-FRET assay to evaluate binding to BD2 of BRD4. | - | 7.4 | pIC50 | 40 | nM | IC50 | PLoS ONE (2013) 8: e83190 [PMID:24391744] |
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 BD1 (unknown origin) incubated for 1 hr by TR-FRET assay | B | 5.32 | pKd | 4836 | nM | Kd | J Med Chem (2020) 63: 5242-5256 [PMID:32255647] |
ChEMBL | Binding affinity to recombinant BRDT BD2 (unknown origin) incubated for 1 hr by TR-FRET assay | B | 6.15 | pKd | 708 | nM | Kd | J Med Chem (2020) 63: 5242-5256 [PMID:32255647] |
ChEMBL | Binding affinity BRDT BD1 (unknown origin) incubated for 1 hr by TR-FRET assay | B | 5.3 | pIC50 | 5027 | nM | IC50 | J Med Chem (2022) 65: 2388-2408 [PMID:34982556] |
ChEMBL | Inhibition of BRDT BD1 (unknown origin) after 1 hr by TR-FRET assay | B | 5.32 | pIC50 | 4836 | nM | IC50 | Eur J Med Chem (2018) 151: 450-461 [PMID:29649741] |
ChEMBL | Inhibition of BRDT BD2 (unknown origin) after 1 hr by TR-FRET assay | B | 6.15 | pIC50 | 708 | nM | IC50 | Eur J Med Chem (2018) 151: 450-461 [PMID:29649741] |
ChEMBL | Binding affinity BRDT BD2 (unknown origin) incubated for 1 hr by TR-FRET assay | B | 6.16 | pIC50 | 696 | nM | IC50 | J Med Chem (2022) 65: 2388-2408 [PMID:34982556] |
CREB binding protein/CREB-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793] | ||||||||
ChEMBL | Binding affinity to recombinant CBP (unknown origin) incubated for 1 hr by TR-FRET assay | B | 5 | pKd | >10000 | nM | Kd | J Med Chem (2020) 63: 5242-5256 [PMID:32255647] |
ChEMBL | Inhibition of CBP (unknown origin) after 1 hr by TR-FRET assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2018) 151: 450-461 [PMID:29649741] |
ChEMBL | Binding affinity CBP (unknown origin) incubated for 1 hr by TR-FRET assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 2388-2408 [PMID:34982556] |
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
ChEMBL | Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 with custom peptide substrate | B | 5.77 | pIC50 | 1689 | nM | IC50 | HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]