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Assay Detail

CHEMBL5378551

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Binding
Binding affinity to human CLK1 assessed as dissociation constant
2
Total Activities
2
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 CLK1 (CHEMBL4224)
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
Kd 2 8.74 9.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5426285 5-(6-BENZOTHIAZOLYLMETHYLENE)-3,5-DIHYDRO-2-(((1S)-1-(METHOXYMETHYL)-3-METHYLBUTYL)AMINO)-4H-IMIDAZOL-4-ONE, (5Z)- 1.0 1 9.41
CHEMBL1802358 1 8.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5426285 5-(6-BENZOTHIAZOLYLMETHYLENE)-3,5-DIHYDRO-2-(((1S)-1-(METHOXYMETHYL)-3-METHYLBUTYL)AMINO)-4H-IMIDAZOL-4-ONE, (5Z)- Kd = 0.388 nM 9.41
CHEMBL1802358 Kd = 8.51 nM 8.07