Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3419225

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

Binding
Displacement of H3K14Ac from BAZ2B (unknown origin) preincubated for 30 mins with non-biotinylated peptide followed by addition of biotinylated peptide measured after 30 mins by AlphaScreen assay
12
Total Activities
12
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

Publication

Structure enabled design of BAZ2-ICR, a chemical probe targeting the bromodomains of BAZ2A and BAZ2B.
Drouin L, McGrath S, Vidler LR, Chaikuad A, Monteiro O, Tallant C, Philpott M, Rogers C, Fedorov O, Liu M, Akhtar W, Hayes A, Raynaud F, Müller S, Knapp S, Hoelder S.
J Med Chem (2015) 58 : 2553 -2559
PubMed 25719566 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.72 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4296718 1 6.75
CHEMBL3415184 1 6.11
CHEMBL3415185 1 6.10
CHEMBL3415182 1 5.97
CHEMBL3415186 1 5.61
CHEMBL3415177 1 5.36
CHEMBL3415179 1 5.28
CHEMBL3415176 1 4.58
CHEMBL3415178 1 -
CHEMBL3415180 1 -
CHEMBL3415181 1 -
CHEMBL3415183 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4296718 IC50 = 180.0 nM 6.75
CHEMBL3415184 IC50 = 770.0 nM 6.11
CHEMBL3415185 IC50 = 790.0 nM 6.10
CHEMBL3415182 IC50 = 1070.0 nM 5.97
CHEMBL3415186 IC50 = 2450.0 nM 5.61
CHEMBL3415177 IC50 = 4400.0 nM 5.36
CHEMBL3415179 IC50 = 5250.0 nM 5.28
CHEMBL3415176 IC50 = 26000.0 nM 4.58
CHEMBL3415178 IC50 > 50000.0 nM -
CHEMBL3415180 IC50 > 50000.0 nM -
CHEMBL3415181 IC50 > 50000.0 nM -
CHEMBL3415183 IC50 > 50000.0 nM -