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Assay Detail

CHEMBL5045929

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

Binding
Binding affinity to human TAF1 BD 2 (1501 to 1635 residues) transfected in Escherichia coli BL21 (DE3) assessed as dissociation constant by q-PCR based bromoscan assay
3
Total Activities
3
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

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
Kd 3 5.99 6.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4285417 CERALASERTIB 3.0 1 6.76
CHEMBL2325697 1 5.21
CHEMBL513909 BI-2536 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4285417 CERALASERTIB Kd = 175.0 nM 6.76
CHEMBL2325697 Kd = 6167.0 nM 5.21
CHEMBL513909 BI-2536 Kd - -