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Assay Detail

CHEMBL5261614

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

Binding
Binding affinity to ZsGreen fused-BRD9 (M1 to T597 residues) (unknown origin) expressed in human U2OS-C433 cells assessed as induction of protein bromodomain localization from chromatin by measuring formation of large nuclear puncta by fluorescence based assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U2OS
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance.
Crawford TD, Vartanian S, Côté A, Bellon S, Duplessis M, Flynn EM, Hewitt M, Huang HR, Kiefer JR, Murray J, Nasveschuk CG, Pardo E, Romero FA, Sandy P, Tang Y, Taylor AM, Tsui V, Wang J, Wang S, Zawadzke L, Albrecht BK, Magnuson SR, Cochran AG, Stokoe D.
Bioorg Med Chem Lett (2017) 27 : 3534 -3541
PubMed 28606761 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 7.25 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5279182 1 8.00
CHEMBL5268484 1 7.89
CHEMBL5268936 1 7.51
CHEMBL5289762 1 7.47
CHEMBL5280605 1 7.46
CHEMBL5284261 1 7.35
CHEMBL5285110 1 7.10
CHEMBL5282240 1 6.72
CHEMBL5286608 1 6.62
CHEMBL5270178 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5279182 EC50 = 10.0 nM 8.00
CHEMBL5268484 EC50 = 13.0 nM 7.89
CHEMBL5268936 EC50 = 31.0 nM 7.51
CHEMBL5289762 EC50 = 34.0 nM 7.47
CHEMBL5280605 EC50 = 35.0 nM 7.46
CHEMBL5284261 EC50 = 45.0 nM 7.35
CHEMBL5285110 EC50 = 79.0 nM 7.10
CHEMBL5282240 EC50 = 190.0 nM 6.72
CHEMBL5286608 EC50 = 240.0 nM 6.62
CHEMBL5270178 EC50 = 380.0 nM 6.42