Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5588798

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

Binding
Inhibition of Aurora A-TPX2 protein-protein interaction in human HeLa cells assessed as mislocalization of aurora A by measuring displacement from spindle incubated for 2 hrs by Hoechst/DAPI staining based imaging analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Aurora kinase A/Targeting protein for Xklp2 (CHEMBL3883304)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Selective Aurora A-TPX2 Interaction Inhibitors Have <i>In Vivo</i> Efficacy as Targeted Antimitotic Agents.
Stockwell SR, Scott DE, Fischer G, Guarino E, Rooney TPC, Feng TS, Moschetti T, Srinivasan R, Alza E, Asteian A, Dagostin C, Alcaide A, Rocaboy M, Blaszczyk B, Higueruelo A, Wang X, Rossmann M, Perrior TR, Blundell TL, Spring DR, McKenzie G, Abell C, Skidmore J, Venkitaraman AR, Hyvönen M.
J Med Chem (2024) 67 : 15521 -15536
PubMed 39190548 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 5.36 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5596916 1 5.89
CHEMBL5598288 1 5.66
CHEMBL5596260 1 5.46
CHEMBL5597168 1 5.26
CHEMBL5597404 1 5.21
CHEMBL5596300 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5596916 EC50 = 1300.0 nM 5.89
CHEMBL5598288 EC50 = 2200.0 nM 5.66
CHEMBL5596260 EC50 = 3500.0 nM 5.46
CHEMBL5597168 EC50 = 5500.0 nM 5.26
CHEMBL5597404 EC50 = 6100.0 nM 5.21
CHEMBL5596300 EC50 = 20000.0 nM 4.70