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Assay Detail

CHEMBL5546197

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

Binding
Activation of GCN2 in HEK293 cells transfected with ATF4 response element preincubated for 30 mins followed by halofuginone addition and measured after 6 hrs by One-Glo reagent based plate reader assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

eIF-2-alpha kinase GCN2 (CHEMBL5358)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of HC-7366: An Orally Bioavailable and Efficacious GCN2 Kinase Activator.
Thomson CG, Aicher TD, Cheng W, Du H, Dudgeon C, Li AH, Li B, Lightcap E, Luo D, Mulvihill M, Pan P, Rahemtulla BF, Rigby AC, Sherborne B, Sood S, Surguladze D, Talbot EPA, Tameire F, Taylor S, Wang Y, Wojnarowicz P, Xiao F, Ramurthy S.
J Med Chem (2024) 67 : 5259 -5271
PubMed 38530741 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 6.85 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5571568 1 7.89
CHEMBL5574976 1 7.34
CHEMBL5569981 1 7.14
CHEMBL5591595 1 6.96
CHEMBL5593998 1 6.92
CHEMBL5590796 1 6.85
CHEMBL5579682 1 6.80
CHEMBL5571377 1 6.80
CHEMBL5593039 1 6.62
CHEMBL5574193 1 6.36
CHEMBL5575532 1 6.34
CHEMBL5574769 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5571568 EC50 = 13.0 nM 7.89
CHEMBL5574976 EC50 = 46.0 nM 7.34
CHEMBL5569981 EC50 = 72.0 nM 7.14
CHEMBL5591595 EC50 = 110.0 nM 6.96
CHEMBL5593998 EC50 = 120.0 nM 6.92
CHEMBL5590796 EC50 = 140.0 nM 6.85
CHEMBL5579682 EC50 = 160.0 nM 6.80
CHEMBL5571377 EC50 = 160.0 nM 6.80
CHEMBL5593039 EC50 = 240.0 nM 6.62
CHEMBL5574193 EC50 = 440.0 nM 6.36
CHEMBL5575532 EC50 = 460.0 nM 6.34
CHEMBL5574769 EC50 = 750.0 nM 6.12