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Assay Detail

CHEMBL5165906

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

Binding
Inhibition of recombinant mouse CLK1 expressed in bacteria using GRSRSRSRSRSR as substrate in presence of ATP measured after 30 mins by ADP-Glo assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Dual specificity protein kinase CLK1 (CHEMBL1075280)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity.
Zeinyeh W, Esvan YJ, Josselin B, Defois M, Baratte B, Knapp S, Chaikuad A, Anizon F, Giraud F, Ruchaud S, Moreau P.
Eur J Med Chem (2022) 236 : 114369 -114369
PubMed 35447555 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.14 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5178368 1 8.10
CHEMBL5186093 1 7.70
CHEMBL5188318 1 7.43
CHEMBL5177344 1 7.14
CHEMBL5194011 1 7.05
CHEMBL5186471 1 7.04
CHEMBL5196946 1 6.83
CHEMBL5183366 1 6.66
CHEMBL5181620 1 6.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5178368 IC50 = 8.0 nM 8.10
CHEMBL5186093 IC50 = 20.0 nM 7.70
CHEMBL5188318 IC50 = 37.0 nM 7.43
CHEMBL5177344 IC50 = 72.0 nM 7.14
CHEMBL5194011 IC50 = 90.0 nM 7.05
CHEMBL5186471 IC50 = 92.0 nM 7.04
CHEMBL5196946 IC50 = 148.0 nM 6.83
CHEMBL5183366 IC50 = 221.0 nM 6.66
CHEMBL5181620 IC50 = 445.0 nM 6.35