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Assay Detail

CHEMBL4030910

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

Binding
Inhibition of human BRD9 (130 to 259 residues) expressed in Escherichia coli BL21 after 1 hr by BROMOscan assay
9
Total Activities
9
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

Bromodomain-containing protein 9 (CHEMBL3108640)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of a Chemical Probe for the Bromodomain and Plant Homeodomain Finger-Containing (BRPF) Family of Proteins.
Igoe N, Bayle ED, Tallant C, Fedorov O, Meier JC, Savitsky P, Rogers C, Morias Y, Scholze S, Boyd H, Cunoosamy D, Andrews DM, Cheasty A, Brennan PE, Müller S, Knapp S, Fish PV.
J Med Chem (2017) 60 : 6998 -7011
PubMed 28714688 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.86 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4103077 1 6.77
CHEMBL4102050 1 6.51
CHEMBL3752151 1 6.28
CHEMBL4076056 1 6.04
CHEMBL4067436 1 5.66
CHEMBL4102751 1 5.57
CHEMBL4065116 1 5.03
CHEMBL4072276 1 5.01
CHEMBL4059509 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4103077 IC50 = 170.0 nM 6.77
CHEMBL4102050 IC50 = 310.0 nM 6.51
CHEMBL3752151 IC50 = 520.0 nM 6.28
CHEMBL4076056 IC50 = 910.0 nM 6.04
CHEMBL4067436 IC50 = 2200.0 nM 5.66
CHEMBL4102751 IC50 = 2700.0 nM 5.57
CHEMBL4065116 IC50 = 9300.0 nM 5.03
CHEMBL4072276 IC50 = 9800.0 nM 5.01
CHEMBL4059509 IC50 > 100000.0 nM -