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Assay Detail

CHEMBL4409976

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

Binding
Inhibition of recombinant human His-tagged Eg5 (1 to 368 residues) assessed as reduction in ATPase activity by Bradford reagent based assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Kinesin-like protein KIF11 (CHEMBL4581)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and bioactivity of dihydropyrimidine derivatives as kinesin spindle protein inhibitors.
Tawfik HO, El-Moselhy TF, El-Din NS, El-Hamamsy MH.
Bioorg Med Chem (2019) 27 : 115126 -115126
PubMed 31648875 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.13 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1213953 1 7.00
CHEMBL394880 DIMETHYLENASTRON 1 6.70
CHEMBL236789 MONASTROL 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1213953 IC50 = 100.0 nM 7.00
CHEMBL394880 DIMETHYLENASTRON IC50 = 200.0 nM 6.70
CHEMBL236789 MONASTROL IC50 = 20000.0 nM 4.70