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Assay Detail

CHEMBL5363603

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

Binding
Inhibition of p97 in human HeLa cells expressing UbG76V-GFP/ODD-Luc assessed as accumulation of Ub-GFP incubated for 6 hrs by confocal microscopic analysis
27
Total Activities
27
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 1,2,4-Triazole-Based p97 Inhibitors for the Treatment of Cancer.
LaPorte MG, Alverez C, Chatterley A, Kovaliov M, Carder EJ, Houghton MJ, Lim C, Miller ER, Samankumara LP, Liang M, Kerrigan K, Yue Z, Li S, Tomaino F, Wang F, Green N, Stott GM, Srivastava A, Chou TF, Wipf P, Huryn DM.
ACS Med Chem Lett (2023) 14 : 977 -985
PubMed 37465292 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 27 5.79 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5441034 1 6.64
CHEMBL5416704 1 6.44
CHEMBL5399073 1 6.44
CHEMBL5407869 1 6.19
CHEMBL5426088 1 6.09
CHEMBL5402777 1 6.09
CHEMBL5414510 1 6.05
CHEMBL5399688 1 6.03
CHEMBL5419713 1 5.89
CHEMBL5426808 1 5.89
CHEMBL5419453 1 5.82
CHEMBL5409286 1 5.75
CHEMBL2311578 1 5.75
CHEMBL5413736 1 5.72
CHEMBL5400436 1 5.62
CHEMBL5412023 1 5.60
CHEMBL5397160 1 5.57
CHEMBL5404554 1 5.57
CHEMBL5414204 1 5.57
CHEMBL5409495 1 5.35
CHEMBL5415233 1 4.96
CHEMBL5399682 1 4.33
CHEMBL5433131 1 -
CHEMBL5398304 1 -
CHEMBL5422339 1 -
CHEMBL5402921 1 -
CHEMBL5426923 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5441034 EC50 = 230.0 nM 6.64
CHEMBL5416704 EC50 = 360.0 nM 6.44
CHEMBL5399073 EC50 = 360.0 nM 6.44
CHEMBL5407869 EC50 = 640.0 nM 6.19
CHEMBL5426088 EC50 = 820.0 nM 6.09
CHEMBL5402777 EC50 = 820.0 nM 6.09
CHEMBL5414510 EC50 = 890.0 nM 6.05
CHEMBL5399688 EC50 = 940.0 nM 6.03
CHEMBL5419713 EC50 = 1300.0 nM 5.89
CHEMBL5426808 EC50 = 1300.0 nM 5.89
CHEMBL5419453 EC50 = 1500.0 nM 5.82
CHEMBL5409286 EC50 = 1800.0 nM 5.75
CHEMBL2311578 EC50 = 1800.0 nM 5.75
CHEMBL5413736 EC50 = 1900.0 nM 5.72
CHEMBL5400436 EC50 = 2400.0 nM 5.62
CHEMBL5412023 EC50 = 2500.0 nM 5.60
CHEMBL5397160 EC50 = 2700.0 nM 5.57
CHEMBL5404554 EC50 = 2700.0 nM 5.57
CHEMBL5414204 EC50 = 2700.0 nM 5.57
CHEMBL5409495 EC50 = 4500.0 nM 5.35
CHEMBL5415233 EC50 = 11000.0 nM 4.96
CHEMBL5399682 EC50 = 47000.0 nM 4.33
CHEMBL5433131 EC50 > 40000.0 nM -
CHEMBL5398304 EC50 > 40000.0 nM -
CHEMBL5422339 EC50 > 40000.0 nM -
CHEMBL5402921 EC50 > 40000.0 nM -
CHEMBL5426923 EC50 > 40000.0 nM -