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Assay Detail

CHEMBL1072820

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Binding
Competitive inhibition of [3H]L-glutamate uptake at amino acid transport system xc- in human SNB19 cells by liquid scintillation counting
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SNB-19
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Isoxazole analogues bind the system xc- transporter: structure-activity relationship and pharmacophore model.
Patel SA, Rajale T, O'Brien E, Burkhart DJ, Nelson JK, Twamley B, Blumenfeld A, Szabon-Watola MI, Gerdes JM, Bridges RJ, Natale NR.
Bioorg Med Chem (2010) 18 : 202 -213
PubMed 19932968 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 4.23 4.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL600474 1 4.28
CHEMBL863 CYSTEINE 4.0 1 4.23
CHEMBL601837 1 4.22
CHEMBL604574 1 4.19
CHEMBL606915 1 -
CHEMBL591770 1 -
CHEMBL590556 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL600474 Ki = 52000.0 nM 4.28
CHEMBL863 CYSTEINE Ki = 59000.0 nM 4.23
CHEMBL601837 Ki = 60000.0 nM 4.22
CHEMBL604574 Ki = 64000.0 nM 4.19
CHEMBL606915 Ki = 113000.0 nM -
CHEMBL591770 Ki = 117000.0 nM -
CHEMBL590556 Ki = 147000.0 nM -