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Assay Detail

CHEMBL5224092

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

Functional
Induction of mitotic arrest in human OVCAR-3 cells assessed as p-histone H3 incubated for 24 hrs by mitotic - imaging assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type OVCAR-3
Confidence 1 — Organism
Curated By Autocuration

Target

OVCAR-3 (CHEMBL614213)
Type CELL-LINE
Organism Homo sapiens

Publication

Targeting the Mitotic Kinesin KIF18A in Chromosomally Unstable Cancers: Hit Optimization Toward an In Vivo Chemical Probe.
Tamayo NA, Bourbeau MP, Allen JR, Ashton KS, Chen JJ, Kaller MR, Nguyen TT, Nishimura N, Pettus LH, Walton M, Belmontes B, Moriguchi J, Chen K, McCarter JD, Hanestad K, Chung G, Ninniri MSS, Sun J, Poppe L, Spahr C, Hui J, Jia L, Wu T, Dahal UP, Edson KZ, Payton M.
J Med Chem (2022) 65 : 4972 -4990
PubMed 35286090 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 6.27 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5076091 1 7.96
CHEMBL4743666 1 7.80
CHEMBL5278809 1 7.55
CHEMBL5287177 1 7.50
CHEMBL5077043 1 7.37
CHEMBL5279604 1 7.32
CHEMBL5270982 1 7.12
CHEMBL5288088 1 6.75
CHEMBL5083562 1 6.72
CHEMBL5276902 1 6.64
CHEMBL5276935 1 6.35
CHEMBL5081638 1 5.99
CHEMBL5084830 1 5.73
CHEMBL5083490 1 5.65
CHEMBL5284647 1 5.58
CHEMBL5287687 1 5.57
CHEMBL5273486 1 5.37
CHEMBL5282084 1 5.33
CHEMBL5267992 1 5.26
CHEMBL5282512 1 5.20
CHEMBL5285875 1 4.83
CHEMBL5274941 1 4.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5076091 EC50 = 11.0 nM 7.96
CHEMBL4743666 EC50 = 16.0 nM 7.80
CHEMBL5278809 EC50 = 28.0 nM 7.55
CHEMBL5287177 EC50 = 32.0 nM 7.50
CHEMBL5077043 EC50 = 43.0 nM 7.37
CHEMBL5279604 EC50 = 48.0 nM 7.32
CHEMBL5270982 EC50 = 75.0 nM 7.12
CHEMBL5288088 EC50 = 177.0 nM 6.75
CHEMBL5083562 EC50 = 190.0 nM 6.72
CHEMBL5276902 EC50 = 228.0 nM 6.64
CHEMBL5276935 EC50 = 449.0 nM 6.35
CHEMBL5081638 EC50 = 1030.0 nM 5.99
CHEMBL5084830 EC50 = 1870.0 nM 5.73
CHEMBL5083490 EC50 = 2260.0 nM 5.65
CHEMBL5284647 EC50 = 2660.0 nM 5.58
CHEMBL5287687 EC50 = 2720.0 nM 5.57
CHEMBL5273486 EC50 = 4290.0 nM 5.37
CHEMBL5282084 EC50 = 4630.0 nM 5.33
CHEMBL5267992 EC50 = 5460.0 nM 5.26
CHEMBL5282512 EC50 = 6350.0 nM 5.20
CHEMBL5285875 EC50 = 14750.0 nM 4.83
CHEMBL5274941 EC50 = 45850.0 nM 4.34