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Assay Detail

CHEMBL4731348

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

Binding
Inhibition of recombinant human His-tagged 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 measured after 15 mins by ADP-Glo kinase 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 KIF18A Inhibitors for Treating Cancer.
Sabnis RW
ACS Med Chem Lett (2020) 11 : 2079 -2080
PubMed 33214814 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.86 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4755023 1 7.92
CHEMBL4784192 1 7.92
CHEMBL4777623 1 7.85
CHEMBL4752657 1 7.85
CHEMBL4777759 1 7.80
CHEMBL4746340 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4755023 IC50 = 12.0 nM 7.92
CHEMBL4784192 IC50 = 12.0 nM 7.92
CHEMBL4777623 IC50 = 14.0 nM 7.85
CHEMBL4752657 IC50 = 14.0 nM 7.85
CHEMBL4777759 IC50 = 16.0 nM 7.80
CHEMBL4746340 IC50 = 16.0 nM 7.80