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Assay Detail

CHEMBL5713043

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

Binding
Displacement of biotinylated peptide from recombinant His6-TEV fused human BAZ2A expressed in Escherichia coli incubated for 30 mins by AlphaScreen assay
21
Total Activities
21
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

Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.
Chen P, Chaikuad A, Bamborough P, Bantscheff M, Bountra C, Chung CW, Fedorov O, Grandi P, Jung D, Lesniak R, Lindon M, Müller S, Philpott M, Prinjha R, Rogers C, Selenski C, Tallant C, Werner T, Willson TM, Knapp S, Drewry DH.
J Med Chem (2016) 59 : 1410 -1424
PubMed 25799074 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.86 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3770199 1 6.80
CHEMBL3739699 1 6.40
CHEMBL3770277 1 6.26
CHEMBL3770214 1 6.24
CHEMBL3770847 1 6.14
CHEMBL3770738 1 6.05
CHEMBL3771216 1 6.00
CHEMBL3771080 1 5.96
CHEMBL3769753 1 5.92
CHEMBL3770155 1 5.92
CHEMBL3769588 1 5.85
CHEMBL1950956 1 5.82
CHEMBL3770449 1 5.77
CHEMBL3770410 1 5.75
CHEMBL3770112 1 5.75
CHEMBL3769769 1 5.48
CHEMBL3771370 1 5.39
CHEMBL3770493 1 5.39
CHEMBL3769490 1 5.14
CHEMBL3769417 1 5.07
CHEMBL3770550 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3770199 IC50 = 160.0 nM 6.80
CHEMBL3739699 IC50 = 400.0 nM 6.40
CHEMBL3770277 IC50 = 550.0 nM 6.26
CHEMBL3770214 IC50 = 580.0 nM 6.24
CHEMBL3770847 IC50 = 720.0 nM 6.14
CHEMBL3770738 IC50 = 890.0 nM 6.05
CHEMBL3771216 IC50 = 1000.0 nM 6.00
CHEMBL3771080 IC50 = 1100.0 nM 5.96
CHEMBL3769753 IC50 = 1200.0 nM 5.92
CHEMBL3770155 IC50 = 1200.0 nM 5.92
CHEMBL3769588 IC50 = 1400.0 nM 5.85
CHEMBL1950956 IC50 = 1500.0 nM 5.82
CHEMBL3770449 IC50 = 1700.0 nM 5.77
CHEMBL3770410 IC50 = 1800.0 nM 5.75
CHEMBL3770112 IC50 = 1800.0 nM 5.75
CHEMBL3769769 IC50 = 3300.0 nM 5.48
CHEMBL3771370 IC50 = 4100.0 nM 5.39
CHEMBL3770493 IC50 = 4100.0 nM 5.39
CHEMBL3769490 IC50 = 7200.0 nM 5.14
CHEMBL3769417 IC50 = 8600.0 nM 5.07
CHEMBL3770550 IC50 > 30000.0 nM -