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Assay Detail

CHEMBL5546191

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

Binding
Inhibition of GCN2 (unknown origin) using GFP-eIF2alpha as substrate incubated for 1.5 hrs in presence of ATP by plate reader analysis
16
Total Activities
16
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

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
IC50 16 7.30 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5571568 1 8.60
CHEMBL5574976 1 8.21
CHEMBL5569981 1 7.92
CHEMBL5571377 1 7.89
CHEMBL5591595 1 7.85
CHEMBL5579682 1 7.82
CHEMBL5590796 1 7.82
CHEMBL5593998 1 7.41
CHEMBL5575532 1 7.41
CHEMBL5574193 1 7.37
CHEMBL5574769 1 7.20
CHEMBL5593039 1 7.16
CHEMBL5590134 1 6.60
CHEMBL5567100 1 6.40
CHEMBL5590151 1 5.77
CHEMBL5570666 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5571568 IC50 = 2.5 nM 8.60
CHEMBL5574976 IC50 = 6.1 nM 8.21
CHEMBL5569981 IC50 = 12.0 nM 7.92
CHEMBL5571377 IC50 = 13.0 nM 7.89
CHEMBL5591595 IC50 = 14.0 nM 7.85
CHEMBL5579682 IC50 = 15.0 nM 7.82
CHEMBL5590796 IC50 = 15.0 nM 7.82
CHEMBL5593998 IC50 = 39.0 nM 7.41
CHEMBL5575532 IC50 = 39.0 nM 7.41
CHEMBL5574193 IC50 = 43.0 nM 7.37
CHEMBL5574769 IC50 = 63.0 nM 7.20
CHEMBL5593039 IC50 = 69.0 nM 7.16
CHEMBL5590134 IC50 = 250.0 nM 6.60
CHEMBL5567100 IC50 = 400.0 nM 6.40
CHEMBL5590151 IC50 = 1700.0 nM 5.77
CHEMBL5570666 IC50 = 3700.0 nM 5.43