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Assay Detail

CHEMBL2172944

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Binding
Inhibition of c-MER
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase Mer (CHEMBL5331)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK).
Axten JM, Medina JR, Feng Y, Shu A, Romeril SP, Grant SW, Li WH, Heerding DA, Minthorn E, Mencken T, Atkins C, Liu Q, Rabindran S, Kumar R, Hong X, Goetz A, Stanley T, Taylor JD, Sigethy SD, Tomberlin GH, Hassell AM, Kahler KM, Shewchuk LM, Gampe RT.
J Med Chem (2012) 55 : 7193 -7207
PubMed 22827572 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.32 6.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2171124 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2171124 IC50 = 474.0 nM 6.32