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Assay Detail

CHEMBL5519218

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

Binding
Inhibition of N-terminal 6His-TEV-tagged recombinant human GPX4-U46C-C10A-C66A mutant (Met1 to Phe170 residues) expressed in Escherichia coli BL21 (DE3) cells incubated for 20 mins by fluorescence polarization based high-throughput screening assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of GPX4 inhibitors through FP-based high-throughput screening.
Cao Y, Wu B, Xu Y, Wang M, Wu X, Liang X, Lin J, Li Z, Lin H, Luo C, Chen S.
Eur J Med Chem (2024) 265 : 116044 -116044
PubMed 38145603 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.27 5.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL487894 DIPYRONE SODIUM 1 5.85
CHEMBL5083184 1 5.34
CHEMBL442687 TIOXOLONE 2.0 1 5.29
CHEMBL4218391 1 5.18
CHEMBL1486563 1 5.12
CHEMBL1473252 SODIUM TANSHINONE IIA SULFONATE 2.0 1 4.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL487894 DIPYRONE SODIUM IC50 = 1400.0 nM 5.85
CHEMBL5083184 IC50 = 4580.0 nM 5.34
CHEMBL442687 TIOXOLONE IC50 = 5180.0 nM 5.29
CHEMBL4218391 IC50 = 6540.0 nM 5.18
CHEMBL1486563 IC50 = 7520.0 nM 5.12
CHEMBL1473252 SODIUM TANSHINONE IIA SULFONATE IC50 = 13850.0 nM 4.86