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Assay Detail

CHEMBL832348

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

Binding
Concentration required for inhibition of cyclin-dependent kinase 5 was measured by scintillation proximity assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Cyclin-dependent kinase 5 (CHEMBL4036)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer's disease.
Helal CJ, Sanner MA, Cooper CB, Gant T, Adam M, Lucas JC, Kang Z, Kupchinsky S, Ahlijanian MK, Tate B, Menniti FS, Kelly K, Peterson M.
Bioorg Med Chem Lett (2004) 14 : 5521 -5525
PubMed 15482916 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 6.88 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL186342 1 8.30
CHEMBL186898 1 8.15
CHEMBL364213 1 8.10
CHEMBL363954 1 8.00
CHEMBL186470 1 7.92
CHEMBL184404 1 7.89
CHEMBL187256 1 7.89
CHEMBL187903 1 7.89
CHEMBL186240 1 7.80
CHEMBL365855 1 7.60
CHEMBL186371 1 7.39
CHEMBL359591 1 7.36
CHEMBL187015 1 7.36
CHEMBL364338 1 7.32
CHEMBL426972 1 7.19
CHEMBL186511 1 7.19
CHEMBL185734 1 7.04
CHEMBL186510 1 6.99
CHEMBL185470 1 6.74
CHEMBL363283 1 6.72
CHEMBL363711 1 6.49
CHEMBL186846 1 6.41
CHEMBL185498 1 6.21
CHEMBL186201 1 6.05
CHEMBL188172 1 5.94
CHEMBL186934 1 5.80
CHEMBL186120 1 5.80
CHEMBL186932 1 5.49
CHEMBL363252 1 5.40
CHEMBL434917 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL186342 IC50 = 5.0 nM 8.30
CHEMBL186898 IC50 = 7.0 nM 8.15
CHEMBL364213 IC50 = 8.0 nM 8.10
CHEMBL363954 IC50 = 10.0 nM 8.00
CHEMBL186470 IC50 = 12.0 nM 7.92
CHEMBL184404 IC50 = 13.0 nM 7.89
CHEMBL187256 IC50 = 13.0 nM 7.89
CHEMBL187903 IC50 = 13.0 nM 7.89
CHEMBL186240 IC50 = 16.0 nM 7.80
CHEMBL365855 IC50 = 25.0 nM 7.60
CHEMBL186371 IC50 = 41.0 nM 7.39
CHEMBL359591 IC50 = 44.0 nM 7.36
CHEMBL187015 IC50 = 44.0 nM 7.36
CHEMBL364338 IC50 = 48.0 nM 7.32
CHEMBL186511 IC50 = 64.0 nM 7.19
CHEMBL426972 IC50 = 64.0 nM 7.19
CHEMBL185734 IC50 = 91.0 nM 7.04
CHEMBL186510 IC50 = 102.0 nM 6.99
CHEMBL185470 IC50 = 183.0 nM 6.74
CHEMBL363283 IC50 = 190.0 nM 6.72
CHEMBL363711 IC50 = 321.0 nM 6.49
CHEMBL186846 IC50 = 390.0 nM 6.41
CHEMBL185498 IC50 = 621.0 nM 6.21
CHEMBL186201 IC50 = 900.0 nM 6.05
CHEMBL188172 IC50 = 1150.0 nM 5.94
CHEMBL186934 IC50 = 1570.0 nM 5.80
CHEMBL186120 IC50 = 1600.0 nM 5.80
CHEMBL186932 IC50 = 3270.0 nM 5.49
CHEMBL363252 IC50 = 3990.0 nM 5.40
CHEMBL434917 IC50 = 4580.0 nM 5.34
CHEMBL186847 IC50 = 6530.0 nM 5.18
CHEMBL362369 IC50 = 7670.0 nM 5.12