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Assay Detail

CHEMBL4032874

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Binding
Inhibition of P300/CBP in human MV4-11 cells assessed as reduction in MYC expression after 4 hrs by luminescence based assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

CREB-binding protein/Histone acetyltransferase p300 (CHEMBL3883300)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors.
Bronner SM, Murray J, Romero FA, Lai KW, Tsui V, Cyr P, Beresini MH, de Leon Boenig G, Chen Z, Choo EF, Clark KR, Crawford TD, Jayaram H, Kaufman S, Li R, Li Y, Liao J, Liang X, Liu W, Ly J, Maher J, Wai J, Wang F, Zheng A, Zhu X, Magnuson S.
J Med Chem (2017) 60 : 10151 -10171
PubMed 29155580 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 6.66 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4095153 1 7.92
CHEMBL4061254 1 7.28
CHEMBL4073812 1 6.44
CHEMBL4072630 1 6.00
CHEMBL4065346 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4095153 EC50 = 12.0 nM 7.92
CHEMBL4061254 EC50 = 53.0 nM 7.28
CHEMBL4073812 EC50 = 360.0 nM 6.44
CHEMBL4072630 EC50 = 1000.0 nM 6.00
CHEMBL4065346 EC50 = 2200.0 nM 5.66