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Assay Detail

CHEMBL4310225

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

Binding
Inhibition of recombinant His-tagged BRD9 (unknown origin) after 10 mins by TR-FRET assay
27
Total Activities
27
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

GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1-like.
Wang S, Tsui V, Crawford TD, Audia JE, Burdick DJ, Beresini MH, Côté A, Cummings R, Duplessis M, Flynn EM, Hewitt MC, Huang HR, Jayaram H, Jiang Y, Joshi S, Murray J, Nasveschuk CG, Pardo E, Poy F, Romero FA, Tang Y, Taylor AM, Wang J, Xu Z, Zawadzke LE, Zhu X, Albrecht BK, Magnuson SR, Bellon S, Cochran AG.
J Med Chem (2018) 61 : 9301 -9315
PubMed 30289257 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 5.82 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4436408 1 6.64
CHEMBL4453202 1 6.21
CHEMBL4513694 1 6.12
CHEMBL4441257 1 6.07
CHEMBL4448345 1 6.06
CHEMBL4572531 1 6.05
CHEMBL4470836 1 6.05
CHEMBL4586175 1 6.02
CHEMBL4483624 1 6.00
CHEMBL4465624 1 6.00
CHEMBL4436158 1 5.85
CHEMBL4455513 1 5.85
CHEMBL4520419 1 5.85
CHEMBL4463398 1 5.82
CHEMBL4483679 1 5.80
CHEMBL4440829 1 5.80
CHEMBL4566599 1 5.77
CHEMBL4518929 1 5.77
CHEMBL4466746 1 5.75
CHEMBL4459660 1 5.70
CHEMBL4459431 1 5.68
CHEMBL4437997 1 5.66
CHEMBL4468549 1 5.66
CHEMBL4445482 1 5.62
CHEMBL4448723 1 5.52
CHEMBL4463538 1 5.02
CHEMBL4534244 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4436408 IC50 = 230.0 nM 6.64
CHEMBL4453202 IC50 = 620.0 nM 6.21
CHEMBL4513694 IC50 = 750.0 nM 6.12
CHEMBL4441257 IC50 = 860.0 nM 6.07
CHEMBL4448345 IC50 = 880.0 nM 6.06
CHEMBL4572531 IC50 = 900.0 nM 6.05
CHEMBL4470836 IC50 = 890.0 nM 6.05
CHEMBL4586175 IC50 = 960.0 nM 6.02
CHEMBL4483624 IC50 = 1000.0 nM 6.00
CHEMBL4465624 IC50 = 1000.0 nM 6.00
CHEMBL4436158 IC50 = 1400.0 nM 5.85
CHEMBL4455513 IC50 = 1400.0 nM 5.85
CHEMBL4520419 IC50 = 1400.0 nM 5.85
CHEMBL4463398 IC50 = 1500.0 nM 5.82
CHEMBL4483679 IC50 = 1600.0 nM 5.80
CHEMBL4440829 IC50 = 1600.0 nM 5.80
CHEMBL4566599 IC50 = 1700.0 nM 5.77
CHEMBL4518929 IC50 = 1700.0 nM 5.77
CHEMBL4466746 IC50 = 1800.0 nM 5.75
CHEMBL4459660 IC50 = 2000.0 nM 5.70
CHEMBL4459431 IC50 = 2100.0 nM 5.68
CHEMBL4437997 IC50 = 2200.0 nM 5.66
CHEMBL4468549 IC50 = 2200.0 nM 5.66
CHEMBL4445482 IC50 = 2400.0 nM 5.62
CHEMBL4448723 IC50 = 3000.0 nM 5.52
CHEMBL4463538 IC50 = 9500.0 nM 5.02
CHEMBL4534244 IC50 = 18000.0 nM 4.75