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Assay Detail

CHEMBL5353382

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

Binding
Inhibition of human GRK2
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

Target

Beta-adrenergic receptor kinase 1 (CHEMBL4079)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Targeting GRK2 and GRK5 for treating chronic degenerative diseases: Advances and future perspectives.
Zhang Y, Zhang J, Wang J, Chen H, Ouyang L, Wang Y.
Eur J Med Chem (2022) 243 : 114668 -114668
PubMed 36055000 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.04 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5414047 1 7.75
CHEMBL4090144 1 7.52
CHEMBL490 PAROXETINE 4.0 1 5.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5414047 IC50 = 18.0 nM 7.75
CHEMBL4090144 IC50 = 30.0 nM 7.52
CHEMBL490 PAROXETINE IC50 = 1380.0 nM 5.86