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Assay Detail

CHEMBL4829967

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of N-terminal GST-tagged human BPTF (2914 to 3037 residues) expressed in Escherichia coli BL21-CodonPlus (DE3) cells by HTRF assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Nucleosome-remodeling factor subunit BPTF (CHEMBL3085621)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of High-Affinity Inhibitors of the BPTF Bromodomain.
Lu T, Lu H, Duan Z, Wang J, Han J, Xiao S, Chen H, Jiang H, Chen Y, Yang F, Li Q, Chen D, Lin J, Li B, Jiang H, Chen K, Lu W, Lin H, Luo C.
J Med Chem (2021) 64 : 12075 -12088
PubMed 34375106 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.72 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4860578 1 7.80
CHEMBL4873042 1 7.57
CHEMBL4870170 1 7.54
CHEMBL4867072 1 7.49
CHEMBL4868713 1 7.43
CHEMBL4866637 1 7.23
CHEMBL4851594 1 7.23
CHEMBL4862619 1 7.20
CHEMBL4852588 1 6.94
CHEMBL4853486 1 6.84
CHEMBL4861221 1 6.80
CHEMBL4863921 1 6.54
CHEMBL4861375 1 6.16
CHEMBL4872350 1 5.77
CHEMBL4872974 1 5.68
CHEMBL4863800 1 5.11
CHEMBL4875586 1 4.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4860578 IC50 = 16.0 nM 7.80
CHEMBL4873042 IC50 = 26.9 nM 7.57
CHEMBL4870170 IC50 = 28.8 nM 7.54
CHEMBL4867072 IC50 = 32.7 nM 7.49
CHEMBL4868713 IC50 = 36.9 nM 7.43
CHEMBL4866637 IC50 = 58.6 nM 7.23
CHEMBL4851594 IC50 = 59.3 nM 7.23
CHEMBL4862619 IC50 = 63.8 nM 7.20
CHEMBL4852588 IC50 = 113.8 nM 6.94
CHEMBL4853486 IC50 = 145.4 nM 6.84
CHEMBL4861221 IC50 = 157.3 nM 6.80
CHEMBL4863921 IC50 = 287.6 nM 6.54
CHEMBL4861375 IC50 = 698.3 nM 6.16
CHEMBL4872350 IC50 = 1700.0 nM 5.77
CHEMBL4872974 IC50 = 2100.0 nM 5.68
CHEMBL4863800 IC50 = 7800.0 nM 5.11
CHEMBL4875586 IC50 = 14700.0 nM 4.83