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Assay Detail

CHEMBL4379080

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

Binding
Inhibition of recombinant full length human PKG1alpha using RRRLSFAEPG as substrate incubated for 40 mins in presence of [gamma-33P]ATP and 10 uM ATP by radiometric scintillation counting analysis
1
Total Activities
1
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

cGMP-dependent protein kinase 1 (CHEMBL4273)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 4H-Chromen-4-one Derivatives as a New Class of Selective Rho Kinase (ROCK) Inhibitors, which Showed Potent Activity in ex Vivo Diabetic Retinopathy Models.
Zhao L, Li Y, Wang Y, Qiao Z, Miao Z, Yang J, Huang L, Tian C, Li L, Chen D, Yang S.
J Med Chem (2019) 62 : 10691 -10710
PubMed 31693351 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.29 6.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4438748 1 6.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4438748 IC50 = 517.0 nM 6.29