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Assay Detail

CHEMBL4810445

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

Binding
Inhibition of recombinant full length human GRK7 using casein as substrate incubated for 40 mins in presence of [gamma-33ATP] by scintillation counting based radiometry assay
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

Rhodopsin kinase GRK7 (CHEMBL1075133)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, Synthesis, and Characterization of 4-Aminoquinazolines as Potent Inhibitors of the G Protein-Coupled Receptor Kinase 6 (GRK6) for the Treatment of Multiple Myeloma.
Uehling DE, Joseph B, Chung KC, Zhang AX, Ler S, Prakesch MA, Poda G, Grouleff J, Aman A, Kiyota T, Leung-Hagesteijn C, Konda JD, Marcellus R, Griffin C, Subramaniam R, Abibi A, Strathdee CA, Isaac MB, Al-Awar R, Tiedemann RE.
J Med Chem (2021) 64 : 11129 -11147
PubMed 34291633 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.82 8.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4877302 1 8.19
CHEMBL4854871 1 7.82
CHEMBL4847703 1 7.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4877302 IC50 = 6.4 nM 8.19
CHEMBL4854871 IC50 = 15.0 nM 7.82
CHEMBL4847703 IC50 = 36.0 nM 7.44