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Assay Detail

CHEMBL3875860

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

Binding
Inhibition of GST-tagged human recombinant CLK3 expressed in Escherichia coli using RS peptide as substrate incubated for 30 mins in presence of [gamma-33 P] ATP by liquid scintillation counting analysis
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Dual specificity protein kinase CLK3 (CHEMBL4226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Further investigation of Paprotrain: Towards the conception of selective and multi-targeted CNS kinase inhibitors.
Labrière C, Lozach O, Blairvacq M, Meijer L, Guillou C.
Eur J Med Chem (2016) 124 : 920 -934
PubMed 27676471 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.72 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3885431 1 6.75
CHEMBL3883660 1 6.72
CHEMBL3884821 1 6.50
CHEMBL3883639 1 6.15
CHEMBL3883820 1 5.75
CHEMBL3883448 1 5.21
CHEMBL3884627 1 5.21
CHEMBL3884015 1 5.17
CHEMBL3885328 1 5.16
CHEMBL3885335 1 5.16
CHEMBL3885360 1 5.10
CHEMBL3884932 1 -
CHEMBL3885036 1 -
CHEMBL3884845 1 -
CHEMBL3885316 1 -
CHEMBL3753668 1 -
CHEMBL3883414 1 -
CHEMBL3884250 1 -
CHEMBL3884570 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3885431 IC50 = 180.0 nM 6.75
CHEMBL3883660 IC50 = 190.0 nM 6.72
CHEMBL3884821 IC50 = 320.0 nM 6.50
CHEMBL3883639 IC50 = 710.0 nM 6.15
CHEMBL3883820 IC50 = 1800.0 nM 5.75
CHEMBL3883448 IC50 = 6100.0 nM 5.21
CHEMBL3884627 IC50 = 6100.0 nM 5.21
CHEMBL3884015 IC50 = 6800.0 nM 5.17
CHEMBL3885328 IC50 = 7000.0 nM 5.16
CHEMBL3885335 IC50 = 7000.0 nM 5.16
CHEMBL3885360 IC50 = 8000.0 nM 5.10
CHEMBL3884932 IC50 - -
CHEMBL3885036 IC50 > 10000.0 nM -
CHEMBL3884845 IC50 - -
CHEMBL3885316 IC50 > 10000.0 nM -
CHEMBL3753668 IC50 > 10000.0 nM -
CHEMBL3883414 IC50 > 10000.0 nM -
CHEMBL3884250 IC50 > 10000.0 nM -
CHEMBL3884570 IC50 > 10000.0 nM -