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Assay Detail

CHEMBL4666141

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 [gamma-33P]ATP
10
Total Activities
10
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

New pyrido[3,4-g]quinazoline derivatives as CLK1 and DYRK1A inhibitors: synthesis, biological evaluation and binding mode analysis.
Tazarki H,Zeinyeh W,Esvan YJ,Knapp S,Chatterjee D,Schröder M,Joerger AC,Khiari J,Josselin B,Baratte B,Bach S,Ruchaud S,Anizon F,Giraud F,Moreau P
Eur J Med Chem (2019) 166 : 304 -317
PubMed 30731399 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.95 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4778413 1 7.75
CHEMBL4784564 1 7.21
CHEMBL4763099 1 6.93
CHEMBL4791275 1 6.92
CHEMBL4759771 1 6.92
CHEMBL4780720 1 6.90
CHEMBL4785650 1 6.88
CHEMBL4794934 1 6.80
CHEMBL4755373 1 6.68
CHEMBL4748345 1 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4778413 IC50 = 18.0 nM 7.75
CHEMBL4784564 IC50 = 62.0 nM 7.21
CHEMBL4763099 IC50 = 117.0 nM 6.93
CHEMBL4791275 IC50 = 120.0 nM 6.92
CHEMBL4759771 IC50 = 120.0 nM 6.92
CHEMBL4780720 IC50 = 125.0 nM 6.90
CHEMBL4785650 IC50 = 133.0 nM 6.88
CHEMBL4794934 IC50 = 160.0 nM 6.80
CHEMBL4755373 IC50 = 210.0 nM 6.68
CHEMBL4748345 IC50 = 290.0 nM 6.54