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Assay Detail

CHEMBL5142216

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

Binding
Binding affinity to human SMARCA2 (S1337 to Q1486 residues) expressed in bacterial expression system by bromoscan assay
5
Total Activities
5
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

Probable global transcription activator SNF2L2 (CHEMBL2362979)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1.
Taylor AM, Bailey C, Belmont LD, Campbell R, Cantone N, Côté A, Crawford TD, Cummings R, DeMent K, Duplessis M, Flynn M, Good AC, Huang HR, Joshi S, Leblanc Y, Murray J, Nasveschuk CG, Neiss A, Poy F, Romero FA, Sandy P, Tang Y, Tsui V, Zawadzke L, Sims RJ, Audia JE, Bellon SF, Magnuson SR, Albrecht BK, Cochran AG.
J Med Chem (2022) 65 : 11177 -11186
PubMed 35930799 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 5 6.91 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5207330 1 7.80
CHEMBL3752911 1 7.75
CHEMBL5177096 1 7.15
CHEMBL5183240 1 6.47
CHEMBL5194650 1 5.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5207330 Kd = 16.0 nM 7.80
CHEMBL3752911 Kd = 18.0 nM 7.75
CHEMBL5177096 Kd = 71.0 nM 7.15
CHEMBL5183240 Kd = 340.0 nM 6.47
CHEMBL5194650 Kd = 4400.0 nM 5.36