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Assay Detail

CHEMBL3864384

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

Binding
Displacement of biotinylated ligand from CBP (unknown origin) by TR-FRET assay
4
Total Activities
4
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

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

Publication

Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.
Crawford TD, Romero FA, Lai KW, Tsui V, Taylor AM, de Leon Boenig G, Noland CL, Murray J, Ly J, Choo EF, Hunsaker TL, Chan EW, Merchant M, Kharbanda S, Gascoigne KE, Kaufman S, Beresini MH, Liao J, Liu W, Chen KX, Chen Z, Conery AR, Côté A, Jayaram H, Jiang Y, Kiefer JR, Kleinheinz T, Li Y, Maher J, Pardo E, Poy F, Spillane KL, Wang F, Wang J, Wei X, Xu Z, Xu Z, Yen I, Zawadzke L, Zhu X, Bellon S, Cummings R, Cochran AG, Albrecht BK, Magnuson S.
J Med Chem (2016) 59 : 10549 -10563
PubMed 27682507 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.71 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3622373 1 7.52
CHEMBL3963965 1 6.72
CHEMBL3774655 1 6.36
CHEMBL3752296 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3622373 IC50 = 30.0 nM 7.52
CHEMBL3963965 IC50 = 190.0 nM 6.72
CHEMBL3774655 IC50 = 440.0 nM 6.36
CHEMBL3752296 IC50 = 580.0 nM 6.24