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Assay Detail

CHEMBL4331195

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Binding
Inhibition of xCT-mediated cystein/glutamate transporter (unknown origin) assessed as reduction in L-[14C]cyctein uptake
5
Total Activities
5
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 5 5.16 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL421 SULFASALAZINE 4.0 1 6.80
CHEMBL1834956 1 4.52
CHEMBL1834954 1 4.16
CHEMBL1834960 1 -
CHEMBL1834958 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL421 SULFASALAZINE IC50 = 160.0 nM 6.80
CHEMBL1834956 IC50 = 30000.0 nM 4.52
CHEMBL1834954 IC50 = 70000.0 nM 4.16
CHEMBL1834960 IC50 = 920000.0 nM -
CHEMBL1834958 IC50 = 700000.0 nM -