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Assay Detail

CHEMBL2182312

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

Binding
Inhibition of mouse recombinant GST-tagged CLK1 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting
3
Total Activities
3
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

Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.
Tahtouh T, Elkins JM, Filippakopoulos P, Soundararajan M, Burgy G, Durieu E, Cochet C, Schmid RS, Lo DC, Delhommel F, Oberholzer AE, Pearl LH, Carreaux F, Bazureau JP, Knapp S, Meijer L.
J Med Chem (2012) 55 : 9312 -9330
PubMed 22998443 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.16 7.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL485053 LEUCETTAMINE B 1 7.18
CHEMBL1802358 1 7.15
CHEMBL269538 HARMINE 1.0 1 7.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL485053 LEUCETTAMINE B IC50 = 66.0 nM 7.18
CHEMBL1802358 IC50 = 71.0 nM 7.15
CHEMBL269538 HARMINE IC50 = 72.0 nM 7.14