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ChEMBL ligand: CHEMBL2393130 (Apabetalone, RVX000222, RVX-000222, RVX-208) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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] |
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 | 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 | 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 | 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 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 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 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 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 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 | 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 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 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 human BRD4 BD2 by isothermal calorimetry analysis | B | 6.87 | pKd | 135 | nM | Kd | J Med Chem (2020) 63: 5585-5623 [PMID:32324999] |
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 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 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 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 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] |
ChEMBL data shown on this page come from version 32:
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]