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Assay Detail

CHEMBL971700

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

Binding
Inhibition of CDK1/Cyclin B by radiometric assay
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 1/cyclin B1 (CHEMBL1907602)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design.
Wyatt PG, Woodhead AJ, Berdini V, Boulstridge JA, Carr MG, Cross DM, Davis DJ, Devine LA, Early TR, Feltell RE, Lewis EJ, McMenamin RL, Navarro EF, O'Brien MA, O'Reilly M, Reule M, Saxty G, Seavers LC, Smith DM, Squires MS, Trewartha G, Walker MT, Woolford AJ.
J Med Chem (2008) 51 : 4986 -4999
PubMed 18656911 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.02 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL518383 1 8.00
CHEMBL498659 1 7.42
CHEMBL457177 1 7.35
CHEMBL456963 1 7.26
CHEMBL445813 AT-7519 2.0 1 6.72
CHEMBL507167 1 6.36
CHEMBL457388 1 6.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL518383 IC50 = 10.0 nM 8.00
CHEMBL498659 IC50 = 38.0 nM 7.42
CHEMBL457177 IC50 = 45.0 nM 7.35
CHEMBL456963 IC50 = 55.0 nM 7.26
CHEMBL445813 AT-7519 IC50 = 190.0 nM 6.72
CHEMBL507167 IC50 = 440.0 nM 6.36
CHEMBL457388 IC50 = 980.0 nM 6.01