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Assay Detail

CHEMBL5045950

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

Binding
Binding affinity to TAF1 in HEK293T cells assessed as increase in TAF1 level by ITDR analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromodomain.
Karim RM, Yang L, Chen L, Bikowitz MJ, Lu J, Grassie D, Shultz ZP, Lopchuk JM, Chen J, Schönbrunn E.
J Med Chem (2022) 65 : 4182 -4200
PubMed 35191694 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.60 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4086276 1 7.16
CHEMBL4463538 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4086276 EC50 = 70.0 nM 7.16
CHEMBL4463538 EC50 = 920.0 nM 6.04