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Assay Detail

CHEMBL4331196

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Binding
Inhibition of cystine/glutamate antiporter system xc- in human HT1080 cells assessed as reduction in L-[3,3'-14C]-cystine uptake in presence of Na+ free uptake buffer by scintillation counting assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cystine/glutamate transporter (CHEMBL1075149)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and development of small molecule modulators targeting glutamine metabolism.
Li L, Meng Y, Li Z, Dai W, Xu X, Bi X, Bian J.
Eur J Med Chem (2019) 163 : 215 -242
PubMed 30522056 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.70 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL401989 ERASTIN 1 6.70
CHEMBL421 SULFASALAZINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL401989 ERASTIN IC50 = 200.0 nM 6.70
CHEMBL421 SULFASALAZINE IC50 = 450000.0 nM -