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Assay Detail

CHEMBL4425852

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

Binding
Inhibition of recombinant His-tagged TAF1 isoform-2 (unknown origin) using biotinylated ligand incubated for 10 mins by TR-FRET assay
5
Total Activities
5
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

Transcription initiation factor TFIID subunit 1 (CHEMBL3217390)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains.
Crawford TD, Tsui V, Flynn EM, Wang S, Taylor AM, Côté A, Audia JE, Beresini MH, Burdick DJ, Cummings R, Dakin LA, Duplessis M, Good AC, Hewitt MC, Huang HR, Jayaram H, Kiefer JR, Jiang Y, Murray J, Nasveschuk CG, Pardo E, Poy F, Romero FA, Tang Y, Wang J, Xu Z, Zawadzke LE, Zhu X, Albrecht BK, Magnuson SR, Bellon S, Cochran AG.
J Med Chem (2016) 59 : 5391 -5402
PubMed 27219867 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.34 7.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4436158 1 7.34
CHEMBL4436408 1 7.23
CHEMBL4519632 1 6.39
CHEMBL4460783 1 6.11
CHEMBL4553271 1 4.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4436158 IC50 = 46.0 nM 7.34
CHEMBL4436408 IC50 = 59.0 nM 7.23
CHEMBL4519632 IC50 = 410.0 nM 6.39
CHEMBL4460783 IC50 = 770.0 nM 6.11
CHEMBL4553271 IC50 = 23700.0 nM 4.62