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Assay Detail

CHEMBL4411103

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

Binding
Inhibition of bovine GRK1 using tubulin as substrate measured after 4 hrs by [gamma-32P]-ATP assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Rhodopsin kinase GRK1 (CHEMBL3879860)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Structure-Based Design of Selective, Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors.
Rowlands RA, Cato MC, Waldschmidt HV, Bouley RA, Chen Q, Avramova L, Larsen SD, Tesmer JJG, White AD.
ACS Med Chem Lett (2019) 10 : 1628 -1634
PubMed 31857838 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.90 6.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4456539 1 6.12
CHEMBL4475305 1 5.68
CHEMBL4449730 1 -
CHEMBL4464632 1 -
CHEMBL4543927 1 -
CHEMBL4450181 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4456539 IC50 = 760.0 nM 6.12
CHEMBL4475305 IC50 = 2100.0 nM 5.68
CHEMBL4449730 IC50 > 100000.0 nM -
CHEMBL4464632 IC50 > 100000.0 nM -
CHEMBL4543927 IC50 > 100000.0 nM -
CHEMBL4450181 IC50 > 100000.0 nM -