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Assay Detail

CHEMBL657263

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

Binding
Ability to inhibit cyclin-dependent kinase 2-cyclin A.
25
Total Activities
25
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 2/cyclin A (CHEMBL2094128)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

A catch-and-release strategy for the combinatorial synthesis of 4-acylamino-1,3-thiazoles as potential CDK5 inhibitors.
Larsen SD, Stachew CF, Clare PM, Cubbage JW, Leach KL.
Bioorg Med Chem Lett (2003) 13 : 3491 -3495
PubMed 14505655 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 4.66 5.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL116949 1 5.30
CHEMBL333136 1 5.22
CHEMBL119812 1 5.00
CHEMBL327004 1 5.00
CHEMBL115625 1 5.00
CHEMBL119143 1 5.00
CHEMBL117950 1 4.82
CHEMBL334091 1 4.70
CHEMBL119796 1 4.70
CHEMBL115650 1 4.70
CHEMBL115429 1 4.70
CHEMBL115472 1 4.52
CHEMBL116017 1 4.52
CHEMBL116615 1 4.46
CHEMBL118685 1 4.40
CHEMBL116339 1 4.22
CHEMBL117906 1 4.16
CHEMBL117778 1 4.05
CHEMBL119041 1 4.05
CHEMBL119530 1 -
CHEMBL332112 1 -
CHEMBL117779 1 -
CHEMBL325452 1 -
CHEMBL117800 1 -
CHEMBL118043 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL116949 IC50 = 5000.0 nM 5.30
CHEMBL333136 IC50 = 6000.0 nM 5.22
CHEMBL119812 IC50 = 10000.0 nM 5.00
CHEMBL327004 IC50 = 10000.0 nM 5.00
CHEMBL115625 IC50 = 10000.0 nM 5.00
CHEMBL119143 IC50 = 10000.0 nM 5.00
CHEMBL117950 IC50 = 15000.0 nM 4.82
CHEMBL334091 IC50 = 20000.0 nM 4.70
CHEMBL119796 IC50 = 20000.0 nM 4.70
CHEMBL115650 IC50 = 20000.0 nM 4.70
CHEMBL115429 IC50 = 20000.0 nM 4.70
CHEMBL115472 IC50 = 30000.0 nM 4.52
CHEMBL116017 IC50 = 30000.0 nM 4.52
CHEMBL116615 IC50 = 35000.0 nM 4.46
CHEMBL118685 IC50 = 40000.0 nM 4.40
CHEMBL116339 IC50 = 60000.0 nM 4.22
CHEMBL117906 IC50 = 70000.0 nM 4.16
CHEMBL117778 IC50 = 90000.0 nM 4.05
CHEMBL119041 IC50 = 90000.0 nM 4.05
CHEMBL119530 IC50 > 100000.0 nM -
CHEMBL332112 IC50 > 100000.0 nM -
CHEMBL117779 IC50 > 100000.0 nM -
CHEMBL325452 IC50 > 100000.0 nM -
CHEMBL117800 IC50 > 100000.0 nM -
CHEMBL118043 IC50 > 100000.0 nM -