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Assay Detail

CHEMBL4058652

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

Binding
Inhibition of CBP in human PBMC derived naive CD4-positive T cells assessed as decrease in FOXP3 mRNA level in Treg cells measured after 4 days by quantitative reverse transcriptase-PCR method
2
Total Activities
1
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

CREB-binding protein (CHEMBL5747)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP).
Romero FA, Murray J, Lai KW, Tsui V, Albrecht BK, An L, Beresini MH, de Leon Boenig G, Bronner SM, Chan EW, Chen KX, Chen Z, Choo EF, Clagg K, Clark K, Crawford TD, Cyr P, de Almeida Nagata D, Gascoigne KE, Grogan JL, Hatzivassiliou G, Huang W, Hunsaker TL, Kaufman S, Koenig SG, Li R, Li Y, Liang X, Liao J, Liu W, Ly J, Maher J, Masui C, Merchant M, Ran Y, Taylor AM, Wai J, Wang F, Wei X, Yu D, Zhu BY, Zhu X, Magnuson S.
J Med Chem (2017) 60 : 9162 -9183
PubMed 28892380 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.77 7.77
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4097025 2 7.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4097025 IC50 = 17.0 nM 7.77
CHEMBL4097025 Inhibition - % -