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Assay Detail

CHEMBL876996

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

Binding
Inhibition of Cyclin-dependent kinase 5-p25nck5a
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Crystal structure of a human cyclin-dependent kinase 6 complex with a flavonol inhibitor, fisetin.
Lu H, Chang DJ, Baratte B, Meijer L, Schulze-Gahmen U.
J Med Chem (2005) 48 : 737 -743
PubMed 15689157 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.52 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL428690 ALVOCIDIB 3.0 1 6.77
CHEMBL31574 FISETIN 2.0 1 6.24
CHEMBL28 APIGENIN 1 5.80
CHEMBL117 CHRYSIN 1 5.51
CHEMBL151 LUTEOLIN 2.0 1 5.42
CHEMBL50 QUERCETIN 3.0 1 4.64
CHEMBL150 KAEMPFEROL 1.0 1 4.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL428690 ALVOCIDIB IC50 = 170.0 nM 6.77
CHEMBL31574 FISETIN IC50 = 570.0 nM 6.24
CHEMBL28 APIGENIN IC50 = 1600.0 nM 5.80
CHEMBL117 CHRYSIN IC50 = 3100.0 nM 5.51
CHEMBL151 LUTEOLIN IC50 = 3800.0 nM 5.42
CHEMBL50 QUERCETIN IC50 = 23000.0 nM 4.64
CHEMBL150 KAEMPFEROL IC50 = 51000.0 nM 4.29