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Assay Detail

CHEMBL5225231

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Binding
Inhibition of PKR (unknown origin)
6
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Identification of potent and selective inhibitors of PKR via virtual screening and traditional design.
Cusack KP, Argiriadi MA, Gordon TD, Harris CM, Herold JM, Hoemann MZ, Yestrepsky BD.
Bioorg Med Chem Lett (2023) 79 : 129047 -129047
PubMed 36400288 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.33 6.94
EC50 2 7.23 7.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5279578 1 7.43
CHEMBL5286788 1 7.02
CHEMBL4281823 1 6.94
CHEMBL5271785 1 6.51
CHEMBL5266620 1 6.44
CHEMBL5280116 1 5.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5279578 EC50 = 37.0 nM 7.43
CHEMBL5286788 EC50 = 95.0 nM 7.02
CHEMBL4281823 IC50 = 116.0 nM 6.94
CHEMBL5271785 IC50 = 306.0 nM 6.51
CHEMBL5266620 IC50 = 364.0 nM 6.44
CHEMBL5280116 IC50 = 3880.0 nM 5.41