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Assay Detail

CHEMBL2443948

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Binding
Inhibition of HRI (unknown origin) assessed as EIF2AK1 phosphorylation
3
Total Activities
3
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

Publication

Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
Axten JM, Romeril SP, Shu A, Ralph J, Medina JR, Feng Y, Li WH, Grant SW, Heerding DA, Minthorn E, Mencken T, Gaul N, Goetz A, Stanley T, Hassell AM, Gampe RT, Atkins C, Kumar R.
ACS Med Chem Lett (2013) 4 : 964 -968
PubMed 24900593 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.99 7.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2441342 1 7.43
CHEMBL2441346 1 7.21
CHEMBL2441340 1 6.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2441342 IC50 = 37.0 nM 7.43
CHEMBL2441346 IC50 = 61.0 nM 7.21
CHEMBL2441340 IC50 = 460.0 nM 6.34