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Assay Detail

CHEMBL2032664

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

Binding
Inhibition of human recombinant CDK5/p25 using [gamma 33P]ATP after 30 mins by scintillation counting
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Cyclin-dependent kinase 5/CDK5 activator 1 (CHEMBL1907600)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Synthesis, biological evaluation, and molecular modeling of natural and unnatural flavonoidal alkaloids, inhibitors of kinases.
Nguyen TB, Lozach O, Surpateanu G, Wang Q, Retailleau P, Iorga BI, Meijer L, Guéritte F.
J Med Chem (2012) 55 : 2811 -2819
PubMed 22352892 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.40 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2029619 1 7.40
CHEMBL2029615 1 7.30
CHEMBL428690 ALVOCIDIB 3.0 1 7.22
CHEMBL2029617 1 7.05
CHEMBL2029622 1 6.57
CHEMBL2029621 1 6.28
CHEMBL2029618 1 6.24
CHEMBL2029614 1 6.02
CHEMBL2029620 1 5.96
CHEMBL489967 1 5.77
CHEMBL2029623 1 5.68
CHEMBL523951 1 5.26
CHEMBL2029616 1 -
CHEMBL490159 BUCHENAVIANINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2029619 IC50 = 40.0 nM 7.40
CHEMBL2029615 IC50 = 50.0 nM 7.30
CHEMBL428690 ALVOCIDIB IC50 = 60.0 nM 7.22
CHEMBL2029617 IC50 = 90.0 nM 7.05
CHEMBL2029622 IC50 = 270.0 nM 6.57
CHEMBL2029621 IC50 = 520.0 nM 6.28
CHEMBL2029618 IC50 = 570.0 nM 6.24
CHEMBL2029614 IC50 = 950.0 nM 6.02
CHEMBL2029620 IC50 = 1100.0 nM 5.96
CHEMBL489967 IC50 = 1700.0 nM 5.77
CHEMBL2029623 IC50 = 2100.0 nM 5.68
CHEMBL523951 IC50 = 5500.0 nM 5.26
CHEMBL2029616 IC50 > 10000.0 nM -
CHEMBL490159 BUCHENAVIANINE IC50 > 10000.0 nM -