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Assay Detail

CHEMBL3591182

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

Binding
Inhibition of mouse recombinant CLK2 expressed in Escherichia coli using RS peptide as substrate after 30 mins by scintillation counting analysis
13
Total Activities
13
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 CLK2 (CHEMBL1075281)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acids are selective inhibitors of DYRK1A.
Falke H, Chaikuad A, Becker A, Loaëc N, Lozach O, Abu Jhaisha S, Becker W, Jones PG, Preu L, Baumann K, Knapp S, Meijer L, Kunick C.
J Med Chem (2015) 58 : 3131 -3143
PubMed 25730262 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.42 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3589661 1 7.26
CHEMBL3589660 1 7.21
CHEMBL3589666 1 6.96
CHEMBL3589664 1 6.75
CHEMBL3589665 1 6.41
CHEMBL3589674 1 6.29
CHEMBL3589672 1 6.21
CHEMBL3589775 1 5.96
CHEMBL3589671 1 5.89
CHEMBL3589662 1 5.26
CHEMBL3589667 1 -
CHEMBL3589669 1 -
CHEMBL3589670 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3589661 IC50 = 55.0 nM 7.26
CHEMBL3589660 IC50 = 61.0 nM 7.21
CHEMBL3589666 IC50 = 110.0 nM 6.96
CHEMBL3589664 IC50 = 180.0 nM 6.75
CHEMBL3589665 IC50 = 390.0 nM 6.41
CHEMBL3589674 IC50 = 510.0 nM 6.29
CHEMBL3589672 IC50 = 610.0 nM 6.21
CHEMBL3589775 IC50 = 1100.0 nM 5.96
CHEMBL3589671 IC50 = 1300.0 nM 5.89
CHEMBL3589662 IC50 = 5500.0 nM 5.26
CHEMBL3589667 IC50 > 10000.0 nM -
CHEMBL3589669 IC50 > 10000.0 nM -
CHEMBL3589670 IC50 > 10000.0 nM -