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Assay Detail

CHEMBL4359604

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Binding
Binding affinity to human partial length TAF1 bromodomain 2 (D1521 to D1656 residues) expressed in bacterial expression system by 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

Optimization of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode.
Lucas SCC, Atkinson SJ, Bamborough P, Barnett H, Chung CW, Gordon L, Mitchell DJ, Phillipou A, Prinjha RK, Sheppard RJ, Tomkinson NCO, Watson RJ, Demont EH.
J Med Chem (2020) 63 : 5212 -5241
PubMed 32321240 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 7.23 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4449894 1 7.80
CHEMBL4465880 1 7.20
CHEMBL4577486 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4449894 Kd = 15.85 nM 7.80
CHEMBL4465880 Kd = 63.1 nM 7.20
CHEMBL4577486 Kd = 199.53 nM 6.70