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Assay Detail

CHEMBL4670873

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

Binding
Inhibition of GPX4 in human LOX IMVI cells assessed as ferroptosis-mediated cell death measured as cell viability in presence of ferrostatin-1
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Structure-activity relationships of GPX4 inhibitor warheads.
Eaton JK,Furst L,Cai LL,Viswanathan VS,Schreiber SL
Bioorg Med Chem Lett (2020) 30 : 127538 -127538
PubMed 32920142 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 48 5.04 5.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4800659 1 5.85
CHEMBL1499544 1 5.66
CHEMBL4779501 1 5.44
CHEMBL4747331 1 5.42
CHEMBL4757878 1 5.38
CHEMBL4765119 1 5.32
CHEMBL4748785 1 5.28
CHEMBL4758051 1 4.72
CHEMBL4792343 1 4.70
CHEMBL4758630 1 4.62
CHEMBL4794855 1 4.58
CHEMBL4764852 1 4.52
CHEMBL1578061 1 4.52
CHEMBL4783507 1 4.48
CHEMBL4741344 1 -
CHEMBL4779048 1 -
CHEMBL4788956 1 -
CHEMBL4762626 1 -
CHEMBL4758354 1 -
CHEMBL4761247 1 -
CHEMBL4780613 1 -
CHEMBL4781918 1 -
CHEMBL4791648 1 -
CHEMBL1951048 1 -
CHEMBL1469676 1 -
CHEMBL4757990 1 -
CHEMBL4756558 1 -
CHEMBL4761568 1 -
CHEMBL4796262 1 -
CHEMBL4793839 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4800659 EC50 = 1400.0 nM 5.85
CHEMBL1499544 EC50 = 2200.0 nM 5.66
CHEMBL4779501 EC50 = 3600.0 nM 5.44
CHEMBL4747331 EC50 = 3800.0 nM 5.42
CHEMBL4757878 EC50 = 4200.0 nM 5.38
CHEMBL4765119 EC50 = 4800.0 nM 5.32
CHEMBL4748785 EC50 = 5200.0 nM 5.28
CHEMBL4758051 EC50 = 19000.0 nM 4.72
CHEMBL4792343 EC50 = 19800.0 nM 4.70
CHEMBL4758630 EC50 = 24000.0 nM 4.62
CHEMBL4794855 EC50 = 26000.0 nM 4.58
CHEMBL4764852 EC50 = 30000.0 nM 4.52
CHEMBL1578061 EC50 = 30000.0 nM 4.52
CHEMBL4783507 EC50 = 33000.0 nM 4.48
CHEMBL4744602 EC50 > 33000.0 nM -
CHEMBL4778553 EC50 > 33000.0 nM -
CHEMBL4785072 EC50 > 33000.0 nM -
CHEMBL4760983 EC50 > 33000.0 nM -
CHEMBL4780750 EC50 > 33000.0 nM -
CHEMBL4751224 EC50 > 33000.0 nM -
CHEMBL4781953 EC50 > 33000.0 nM -
CHEMBL4755063 EC50 > 33000.0 nM -
CHEMBL4742976 EC50 > 33000.0 nM -
CHEMBL4753730 EC50 > 33000.0 nM -
CHEMBL4753327 EC50 > 33000.0 nM -
CHEMBL4785219 EC50 > 33000.0 nM -
CHEMBL4800033 EC50 > 33000.0 nM -
CHEMBL4798158 EC50 > 33000.0 nM -
CHEMBL4740507 EC50 > 33000.0 nM -
CHEMBL4745951 EC50 > 33000.0 nM -
CHEMBL4747623 EC50 > 33000.0 nM -
CHEMBL4781918 EC50 > 33000.0 nM -
CHEMBL4793839 EC50 > 33000.0 nM -
CHEMBL4796262 EC50 > 33000.0 nM -
CHEMBL4761568 EC50 > 33000.0 nM -
CHEMBL4756558 EC50 > 33000.0 nM -
CHEMBL4757990 EC50 > 33000.0 nM -
CHEMBL1469676 EC50 > 33000.0 nM -
CHEMBL1951048 EC50 > 33000.0 nM -
CHEMBL4791648 EC50 > 33000.0 nM -
CHEMBL4784730 EC50 > 333000.0 nM -
CHEMBL4780613 EC50 > 33000.0 nM -
CHEMBL4761247 EC50 > 33000.0 nM -
CHEMBL4758354 EC50 > 33000.0 nM -
CHEMBL4762626 EC50 > 33000.0 nM -
CHEMBL4788956 EC50 > 33000.0 nM -
CHEMBL4779048 EC50 > 33000.0 nM -
CHEMBL4741344 EC50 > 333000.0 nM -