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Assay Detail

CHEMBL4714848

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

Binding
Inhibition of recombinant His-tagged human KIF18A (1 to 467 residues) expressed in baculovirus expression system assessed as inhibition of microtubule-stimulated ATPase activity preincubated for 15 mins followed by ATP addition and further incubated for 15 mins and measured after 80 mins by ADP-Glo reagent based assay
6
Total Activities
6
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 KIF18A (CHEMBL4523403)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel Amide Compounds as KIF18A Inhibitors for Treating Cancer.
Sabnis RW.
ACS Med Chem Lett (2021) 12 : 690 -691
PubMed 34055211 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.62 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4776977 1 7.92
CHEMBL4757053 1 7.58
CHEMBL4759372 1 7.58
CHEMBL4743666 1 7.57
CHEMBL4765048 1 7.54
CHEMBL4786845 1 7.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4776977 IC50 = 12.0 nM 7.92
CHEMBL4757053 IC50 = 26.0 nM 7.58
CHEMBL4759372 IC50 = 26.0 nM 7.58
CHEMBL4743666 IC50 = 27.0 nM 7.57
CHEMBL4765048 IC50 = 29.0 nM 7.54
CHEMBL4786845 IC50 = 29.0 nM 7.54