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Assay Detail

CHEMBL833497

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

Binding
Inhibition of human cyclin-dependent kinase 1
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Cyclin-dependent kinase 1 (CHEMBL308)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors.
Kuo GH, Wang A, Emanuel S, Deangelis A, Zhang R, Connolly PJ, Murray WV, Gruninger RH, Sechler J, Fuentes-Pesquera A, Johnson D, Middleton SA, Jolliffe L, Chen X.
J Med Chem (2005) 48 : 1886 -1900
PubMed 15771433 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.09 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL300389 1 7.77
CHEMBL177434 1 6.30
CHEMBL178484 1 5.65
CHEMBL355578 1 5.62
CHEMBL368786 1 5.09
CHEMBL177688 1 -
CHEMBL368997 1 -
CHEMBL177548 1 -
CHEMBL369217 1 -
CHEMBL178743 1 -
CHEMBL177384 1 -
CHEMBL177806 1 -
CHEMBL368936 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL300389 IC50 = 17.0 nM 7.77
CHEMBL177434 IC50 = 500.0 nM 6.30
CHEMBL178484 IC50 = 2220.0 nM 5.65
CHEMBL355578 IC50 = 2400.0 nM 5.62
CHEMBL368786 IC50 = 8080.0 nM 5.09
CHEMBL177688 IC50 > 10000.0 nM -
CHEMBL368997 IC50 > 10000.0 nM -
CHEMBL177548 IC50 > 10000.0 nM -
CHEMBL369217 IC50 > 10000.0 nM -
CHEMBL178743 IC50 > 10000.0 nM -
CHEMBL177384 IC50 > 10000.0 nM -
CHEMBL177806 IC50 > 10000.0 nM -
CHEMBL368936 IC50 > 10000.0 nM -