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Assay Detail

CHEMBL5376084

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

Functional
Induction of ferroptosis in GPX4-dependent human HT-1080 cells assessed as cell viability incubated for 6 hrs by time-course cell viability assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HT-1080
Confidence 1 — Organism
Curated By Autocuration

Target

HT-1080 (CHEMBL614580)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of a Potent Chloroacetamide GPX4 Inhibitor with Bioavailability to Enable Target Engagement in Mice, a Potential Tool Compound for Inducing Ferroptosis <i>In Vivo</i>.
Randolph JT, O'Connor MJ, Han F, Hutchins CW, Siu YA, Cho M, Zheng Y, Hickson JA, Markley JL, Manaves V, Algire M, Baker KA, Chapman AM, Gopalakrishnan SM, Panchal SC, Foster-Duke K, Stolarik DF, Kempf-Grote A, Dammeier D, Fossey S, Sun Q, Sun C, Shen Y, Dart MJ, Kati WM, Lai A, Firestone AJ, Kort ME.
J Med Chem (2023) 66 : 3852 -3865
PubMed 36877935 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.00 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4747331 1 7.22
CHEMBL5428657 1 6.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4747331 EC50 = 60.0 nM 7.22
CHEMBL5428657 EC50 = 170.0 nM 6.77