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Assay Detail

CHEMBL5378451

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Binding
Inhibition of human recombinant CLK3 assessed as incorporation of 33Pi using [gamma-33P]-ATP measured after 60 mins by microplate scintillation counting based radiometric analysis
16
Total Activities
16
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

Chemical, Biochemical, Cellular, and Physiological Characterization of Leucettinib-21, a Down Syndrome and Alzheimer's Disease Drug Candidate.
Lindberg MF, Deau E, Miege F, Greverie M, Roche D, George N, George P, Merlet L, Gavard J, Brugman SJT, Aret E, Tinnemans P, de Gelder R, Sadownik J, Verhofstad E, Sleegers D, Santangelo S, Dairou J, Fernandez-Blanco Á, Dierssen M, Krämer A, Knapp S, Meijer L.
J Med Chem (2023) 66 : 15648 -15670
PubMed 38051674 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.96 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5429359 1 6.66
CHEMBL5426285 5-(6-BENZOTHIAZOLYLMETHYLENE)-3,5-DIHYDRO-2-(((1S)-1-(METHOXYMETHYL)-3-METHYLBUTYL)AMINO)-4H-IMIDAZOL-4-ONE, (5Z)- 1.0 1 6.63
CHEMBL5412105 1 6.34
CHEMBL5085086 1 6.33
CHEMBL5408047 1 6.32
CHEMBL5432405 1 6.02
CHEMBL5406672 1 5.90
CHEMBL5433334 1 5.87
CHEMBL5403642 1 5.60
CHEMBL5430240 1 5.33
CHEMBL5424188 1 5.27
CHEMBL1802358 1 5.23
CHEMBL485053 LEUCETTAMINE B 1 -
CHEMBL5426979 1 -
CHEMBL5413380 1 -
CHEMBL5404093 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5429359 IC50 = 219.2 nM 6.66
CHEMBL5426285 5-(6-BENZOTHIAZOLYLMETHYLENE)-3,5-DIHYDRO-2-(((1S)-1-(METHOXYMETHYL)-3-METHYLBUTYL)AMINO)-4H-IMIDAZOL-4-ONE, (5Z)- IC50 = 232.0 nM 6.63
CHEMBL5412105 IC50 = 461.3 nM 6.34
CHEMBL5085086 IC50 = 465.7 nM 6.33
CHEMBL5408047 IC50 = 473.9 nM 6.32
CHEMBL5432405 IC50 = 946.8 nM 6.02
CHEMBL5406672 IC50 = 1259.0 nM 5.90
CHEMBL5433334 IC50 = 1357.0 nM 5.87
CHEMBL5403642 IC50 = 2518.0 nM 5.60
CHEMBL5430240 IC50 = 4688.0 nM 5.33
CHEMBL5424188 IC50 = 5317.0 nM 5.27
CHEMBL1802358 IC50 = 5840.0 nM 5.23
CHEMBL485053 LEUCETTAMINE B IC50 > 10000.0 nM -
CHEMBL5426979 IC50 > 10000.0 nM -
CHEMBL5413380 IC50 > 10000.0 nM -
CHEMBL5404093 IC50 > 10000.0 nM -