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Assay Detail

CHEMBL5550422

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 incubated for 30 mins in presence of ATP by ADP-Glo kinase assay
8
Total Activities
8
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 1H-pyrrolo[3,2-g]isoquinolines.
Defois M, Josselin B, Brindeau P, Krämer A, Knapp S, Anizon F, Giraud F, Ruchaud S, Moreau P.
Bioorg Med Chem (2024) 100 : 117619 -117619
PubMed 38320389 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.51 6.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5562930 1 6.86
CHEMBL5571626 1 6.74
CHEMBL5574139 1 6.69
CHEMBL5564481 1 6.58
CHEMBL5569099 1 6.44
CHEMBL5181620 1 6.35
CHEMBL5594716 1 6.25
CHEMBL5570490 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5562930 IC50 = 139.0 nM 6.86
CHEMBL5571626 IC50 = 182.0 nM 6.74
CHEMBL5574139 IC50 = 205.0 nM 6.69
CHEMBL5564481 IC50 = 265.0 nM 6.58
CHEMBL5569099 IC50 = 360.0 nM 6.44
CHEMBL5181620 IC50 = 445.0 nM 6.35
CHEMBL5594716 IC50 = 564.0 nM 6.25
CHEMBL5570490 IC50 = 693.0 nM 6.16