Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3631402

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

Binding
Inhibition of Xct in human CCF-STTG1 cells assessed as glutamate release after 2 hrs by fluorometry
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CCF-STTG1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Incorporation of metabolically stable ketones into a small molecule probe to increase potency and water solubility.
Larraufie MH, Yang WS, Jiang E, Thomas AG, Slusher BS, Stockwell BR.
Bioorg Med Chem Lett (2015) 25 : 4787 -4792
PubMed 26231156 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.34 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3629669 1 8.40
CHEMBL3629579 1 8.00
CHEMBL3629668 1 8.00
CHEMBL3629578 1 7.70
CHEMBL3629576 1 7.52
CHEMBL3629671 1 7.52
CHEMBL3629577 1 7.40
CHEMBL3629575 1 7.22
CHEMBL3629670 1 7.00
CHEMBL401989 ERASTIN 1 6.70
CHEMBL3629580 1 6.52
CHEMBL3629574 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3629669 IC50 = 4.0 nM 8.40
CHEMBL3629579 IC50 = 10.0 nM 8.00
CHEMBL3629668 IC50 = 10.0 nM 8.00
CHEMBL3629578 IC50 = 20.0 nM 7.70
CHEMBL3629576 IC50 = 30.0 nM 7.52
CHEMBL3629671 IC50 = 30.0 nM 7.52
CHEMBL3629577 IC50 = 40.0 nM 7.40
CHEMBL3629575 IC50 = 60.0 nM 7.22
CHEMBL3629670 IC50 = 100.0 nM 7.00
CHEMBL401989 ERASTIN IC50 = 200.0 nM 6.70
CHEMBL3629580 IC50 = 300.0 nM 6.52
CHEMBL3629574 IC50 = 800.0 nM 6.10