apabetalone [Ligand Id: 7034] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2393130 (Apabetalone, RVX-000222, RVX000222, RVX-208)
  • 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]
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  • CREB binding protein/CREB-binding protein in Human [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793]
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  • histone deacetylase 6/Histone deacetylase 6 in Human [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
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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 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]