Assay Detail

CHEMBL5150317

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Binding

Inhibition of GRK2 (unknown origin)

ChEMBL ↗

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Target

Beta-adrenergic receptor kinase 1 (CHEMBL4079) ↗

Open DB target context

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Beta-adrenergic receptor kinase 1 (CHEMBL4079) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Beta-adrenergic receptor kinase 1

CHEMBL4079

Anchored from Assay target.

Protein identity Beta-adrenergic receptor kinase 1

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

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

Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.

Xie Z, Yang X, Duan Y, Han J, Liao C.
J Med Chem (2021) 64 : 1283 -1345
PubMed 33481605 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	6.04	6.11

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL384073	GSK-180736A	—	1	6.11
CHEMBL490	PAROXETINE	4.0	1	5.96

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL384073	GSK-180736A	IC50	=	770.0	nM	6.11
CHEMBL490	PAROXETINE	IC50	=	1100.0	nM	5.96