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Assay Detail

CHEMBL4270233

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

Binding
Inhibition of human p97 in human HeLa cells harboring UbG76V-GFP assessed as accumulation of UbG76V after 1 hr by microscopic analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Transitional endoplasmic reticulum ATPase (CHEMBL1075145)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of Phenyl Indole Inhibitors of the AAA+ ATPase p97.
LaPorte MG, Burnett JC, Colombo R, Bulfer SL, Alverez C, Chou TF, Neitz RJ, Green N, Moore WJ, Yue Z, Li S, Arkin MR, Wipf P, Huryn DM.
ACS Med Chem Lett (2018) 9 : 1075 -1081
PubMed 30429948 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 5.13 5.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2311578 1 5.85
CHEMBL4280801 1 4.82
CHEMBL4288865 1 4.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2311578 EC50 = 1400.0 nM 5.85
CHEMBL4280801 EC50 = 15000.0 nM 4.82
CHEMBL4288865 EC50 = 19000.0 nM 4.72