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Assay Detail

CHEMBL4269217

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Binding
Inhibition of recombinant full-length His6-tagged human P300 expressed in Baculovirus-infected Sf21 cells using histone as substrate after 10 mins in presence of [3H]-acetyl-CoA by autoradiographic analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf21
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone acetyltransferase p300 (CHEMBL3784)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and biological evaluation of thiobarbituric derivatives as potent p300/CBP inhibitors.
Lu W, Xiong H, Chen Y, Wang C, Zhang H, Xu P, Han J, Xiao S, Ding H, Chen Z, Lu T, Wang J, Zhang Y, Yue L, Liu YC, Zhang C, Yang Y, Jiang H, Chen K, Zhou B, Luo C.
Bioorg Med Chem (2018) 26 : 5397 -5407
PubMed 30297119 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.16 5.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL445599 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL445599 IC50 = 7000.0 nM 5.16