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Assay Detail

CHEMBL4310227

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

Binding
Inhibition of recombinant His-tagged CBP (unknown origin) after 10 mins by TR-FRET assay
8
Total Activities
8
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

GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1-like.
Wang S, Tsui V, Crawford TD, Audia JE, Burdick DJ, Beresini MH, Côté A, Cummings R, Duplessis M, Flynn EM, Hewitt MC, Huang HR, Jayaram H, Jiang Y, Joshi S, Murray J, Nasveschuk CG, Pardo E, Poy F, Romero FA, Tang Y, Taylor AM, Wang J, Xu Z, Zawadzke LE, Zhu X, Albrecht BK, Magnuson SR, Bellon S, Cochran AG.
J Med Chem (2018) 61 : 9301 -9315
PubMed 30289257 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.25 6.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4436408 1 6.25
CHEMBL4436158 1 -
CHEMBL4466746 1 -
CHEMBL4483624 1 -
CHEMBL4518929 1 -
CHEMBL4572531 1 -
CHEMBL4470836 1 -
CHEMBL4463398 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4436408 IC50 = 560.0 nM 6.25
CHEMBL4436158 IC50 > 20000.0 nM -
CHEMBL4466746 IC50 > 20000.0 nM -
CHEMBL4483624 IC50 > 20000.0 nM -
CHEMBL4518929 IC50 > 20000.0 nM -
CHEMBL4572531 IC50 > 20000.0 nM -
CHEMBL4470836 IC50 > 20000.0 nM -
CHEMBL4463398 IC50 > 20000.0 nM -