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Assay Detail

CHEMBL4150992

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Binding
Inhibition of FAM-labeled ZBA248 binding to recombinant human BRD4 bromodomain 1 (44 to 168 residues) expressed in Rosetta2 Escherichia coli DE3 cells after 30 mins by fluorescence polarization assay
ChEMBL ↗
61
Total Activities
31
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bromodomain-containing protein 4 (CHEMBL1163125) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Discovery of CF53 as a Potent and Orally Bioavailable Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitor.
Zhao Y, Zhou B, Bai L, Liu L, Yang CY, Meagher JL, Stuckey JA, McEachern D, Przybranowski S, Wang M, Ran X, Aguilar A, Hu Y, Kampf JW, Li X, Zhao T, Li S, Wen B, Sun D, Wang S.
J Med Chem (2018) 61 : 6110 -6120
PubMed 30015487 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 7.76 8.70
Ki 30 8.28 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4166630 — — 2 9.30
CHEMBL4174669 — — 2 9.15
CHEMBL4172277 — — 2 9.10
CHEMBL4164015 — — 2 9.10
CHEMBL4164393 — — 2 9.00
CHEMBL4162784 — — 2 8.92
CHEMBL4168913 — — 2 8.77
CHEMBL4159422 — — 2 8.70
CHEMBL4173488 — — 2 8.70
CHEMBL4170044 — — 2 8.62
CHEMBL4163185 — — 2 8.59
CHEMBL4166235 — — 2 8.51
CHEMBL4174543 — — 2 8.47
CHEMBL4167996 — — 2 8.40
CHEMBL4171109 — — 2 8.36
CHEMBL4177214 — — 2 8.31
CHEMBL4161145 — — 2 8.31
CHEMBL4169068 — — 2 8.30
CHEMBL4172447 — — 2 8.26
CHEMBL4176849 — — 2 8.21
CHEMBL4175855 — — 2 8.20
CHEMBL4171228 — — 2 8.09
CHEMBL4164563 — — 2 7.80
CHEMBL4162046 — — 2 7.78
CHEMBL4160989 — — 2 7.67
CHEMBL4176107 — — 2 7.55
CHEMBL4165491 — — 2 7.51
CHEMBL4172728 — — 2 7.18
CHEMBL4169335 — — 2 7.11
CHEMBL4169373 — — 2 7.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4166630 — Ki = 0.5 nM 9.30
CHEMBL4174669 — Ki = 0.7 nM 9.15
CHEMBL4172277 — Ki = 0.8 nM 9.10
CHEMBL4164015 — Ki = 0.8 nM 9.10
CHEMBL4164393 — Ki = 1.0 nM 9.00
CHEMBL4162784 — Ki = 1.2 nM 8.92
CHEMBL4168913 — Ki = 1.7 nM 8.77
CHEMBL4159422 — Ki = 2.0 nM 8.70
CHEMBL4173488 — IC50 = 2.0 nM 8.70
CHEMBL4170044 — Ki = 2.4 nM 8.62
CHEMBL4163185 — Ki = 2.6 nM 8.59
CHEMBL4166235 — Ki = 3.1 nM 8.51
CHEMBL4174543 — Ki = 3.4 nM 8.47
CHEMBL4167996 — IC50 = 4.0 nM 8.40
CHEMBL4171109 — IC50 = 4.4 nM 8.36
CHEMBL4177214 — Ki = 4.9 nM 8.31
CHEMBL4161145 — IC50 = 4.9 nM 8.31
CHEMBL4169068 — IC50 = 5.0 nM 8.30
CHEMBL4172447 — IC50 = 5.5 nM 8.26
CHEMBL4176849 — IC50 = 6.1 nM 8.21
CHEMBL4166630 — IC50 = 6.1 nM 8.21
CHEMBL4164015 — IC50 = 6.1 nM 8.21
CHEMBL4175855 — Ki = 6.3 nM 8.20
CHEMBL4171228 — Ki = 8.2 nM 8.09
CHEMBL4174669 — IC50 = 9.1 nM 8.04
CHEMBL4172277 — IC50 = 9.4 nM 8.03
CHEMBL4164393 — IC50 = 9.8 nM 8.01
CHEMBL4162784 — IC50 = 10.5 nM 7.98
CHEMBL4168913 — IC50 = 11.8 nM 7.93
CHEMBL4159422 — IC50 = 12.8 nM 7.89
CHEMBL4170044 — IC50 = 13.8 nM 7.86
CHEMBL4163185 — IC50 = 14.3 nM 7.84
CHEMBL4166235 — IC50 = 15.8 nM 7.80
CHEMBL4164563 — Ki = 15.8 nM 7.80
CHEMBL4162046 — Ki = 16.7 nM 7.78
CHEMBL4174543 — IC50 = 16.8 nM 7.78
CHEMBL4177214 — IC50 = 20.8 nM 7.68
CHEMBL4160989 — Ki = 21.5 nM 7.67
CHEMBL4175855 — IC50 = 24.9 nM 7.60
CHEMBL4171228 — IC50 = 28.2 nM 7.55
CHEMBL4176107 — Ki = 28.4 nM 7.55
CHEMBL4165491 — Ki = 31.0 nM 7.51
CHEMBL4164563 — IC50 = 51.7 nM 7.29
CHEMBL4162046 — IC50 = 54.5 nM 7.26
CHEMBL4172728 — Ki = 66.5 nM 7.18
CHEMBL4160989 — IC50 = 68.0 nM 7.17
CHEMBL4169373 — Ki = 77.9 nM 7.11
CHEMBL4169335 — Ki = 78.0 nM 7.11
CHEMBL4176107 — IC50 = 87.6 nM 7.06
CHEMBL4165491 — IC50 = 95.2 nM 7.02