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Assay Detail

CHEMBL4043637

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

Binding
Inhibition of mouse PKA using CREBtide as substrate after 30 mins in presence of ATP by ADP-Glo kinase assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine.
Waldschmidt HV, Homan KT, Cato MC, Cruz-Rodríguez O, Cannavo A, Wilson MW, Song J, Cheung JY, Koch WJ, Tesmer JJ, Larsen SD.
J Med Chem (2017) 60 : 3052 -3069
PubMed 28323425 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 4.48 4.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4083142 1 4.59
CHEMBL384073 GSK-180736A 1 4.52
CHEMBL4062790 1 4.32
CHEMBL4099398 1 -
CHEMBL4073639 1 -
CHEMBL4091281 1 -
CHEMBL4064274 1 -
CHEMBL4071638 1 -
CHEMBL4098656 1 -
CHEMBL4063014 1 -
CHEMBL4090923 1 -
CHEMBL4101136 1 -
CHEMBL4070885 1 -
CHEMBL1738878 1 -
CHEMBL4072898 1 -
CHEMBL4070290 1 -
CHEMBL4081802 1 -
CHEMBL4087244 1 -
CHEMBL4105100 1 -
CHEMBL4079362 1 -
CHEMBL4097393 1 -
CHEMBL4076529 1 -
CHEMBL4077197 1 -
CHEMBL4075712 1 -
CHEMBL4075475 1 -
CHEMBL4084465 1 -
CHEMBL4077459 1 -
CHEMBL4074476 1 -
CHEMBL4076131 1 -
CHEMBL4090144 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4083142 IC50 = 25800.0 nM 4.59
CHEMBL384073 GSK-180736A IC50 = 30000.0 nM 4.52
CHEMBL4062790 IC50 = 48200.0 nM 4.32
CHEMBL1738878 IC50 - -
CHEMBL490 PAROXETINE IC50 > 100000.0 nM -
CHEMBL4070885 IC50 > 100000.0 nM -
CHEMBL4101136 IC50 > 100000.0 nM -
CHEMBL4090923 IC50 > 100000.0 nM -
CHEMBL4063014 IC50 > 100000.0 nM -
CHEMBL4098656 IC50 > 100000.0 nM -
CHEMBL4071638 IC50 > 100000.0 nM -
CHEMBL4064274 IC50 > 100000.0 nM -
CHEMBL4091281 IC50 > 100000.0 nM -
CHEMBL4073639 IC50 > 100000.0 nM -
CHEMBL4099398 IC50 > 100000.0 nM -
CHEMBL4077133 IC50 > 100000.0 nM -
CHEMBL3809020 IC50 > 100000.0 nM -
CHEMBL1738877 IC50 - -
CHEMBL4072898 IC50 > 100000.0 nM -
CHEMBL4070290 IC50 > 100000.0 nM -
CHEMBL4081802 IC50 > 100000.0 nM -
CHEMBL4087244 IC50 > 100000.0 nM -
CHEMBL4105100 IC50 > 100000.0 nM -
CHEMBL4079362 IC50 > 100000.0 nM -
CHEMBL4097393 IC50 > 100000.0 nM -
CHEMBL4076529 IC50 > 100000.0 nM -
CHEMBL4077197 IC50 > 100000.0 nM -
CHEMBL4075712 IC50 > 100000.0 nM -
CHEMBL4075475 IC50 > 100000.0 nM -
CHEMBL4084465 IC50 > 100000.0 nM -
CHEMBL4077459 IC50 > 100000.0 nM -
CHEMBL4074476 IC50 > 100000.0 nM -
CHEMBL4076131 IC50 > 100000.0 nM -
CHEMBL4090144 IC50 > 100000.0 nM -