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Assay Detail

CHEMBL4411105

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

Binding
Inhibition of bovine GRK6 using tubulin as substrate measured after 4 hrs by [gamma-32P]-ATP assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 12 5.53 6.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4464632 1 6.39
CHEMBL4557065 1 5.75
CHEMBL4592746 1 5.60
CHEMBL4576822 1 5.58
CHEMBL4447191 1 5.11
CHEMBL4456130 1 4.75
CHEMBL4543927 1 -
CHEMBL4536595 1 -
CHEMBL4578499 1 -
CHEMBL4517792 1 -
CHEMBL4569321 1 -
CHEMBL4524355 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4464632 IC50 = 410.0 nM 6.39
CHEMBL4557065 IC50 = 1800.0 nM 5.75
CHEMBL4592746 IC50 = 2500.0 nM 5.60
CHEMBL4576822 IC50 = 2600.0 nM 5.58
CHEMBL4447191 IC50 = 7700.0 nM 5.11
CHEMBL4456130 IC50 = 18000.0 nM 4.75
CHEMBL4543927 IC50 > 100000.0 nM -
CHEMBL4536595 IC50 > 100000.0 nM -
CHEMBL4578499 IC50 > 100000.0 nM -
CHEMBL4517792 IC50 > 100000.0 nM -
CHEMBL4569321 IC50 > 100000.0 nM -
CHEMBL4524355 IC50 > 100000.0 nM -