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Assay Detail

CHEMBL1014617

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

Binding
Displacement of [3H]leucine from Large neutral amino acids transporter system L in CHO cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cricetulus griseus
Cell Type CHO
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Oxadiazolone bioisosteres of pregabalin and gabapentin.
Wustrow DJ, Belliotti TR, Capiris T, Kneen CO, Bryans JS, Field MJ, Williams D, El-Kattan A, Buchholz L, Kinsora JJ, Lotarski SM, Vartanian MG, Taylor CP, Donevan SD, Thorpe AJ, Schwarz JB.
Bioorg Med Chem Lett (2009) 19 : 247 -250
PubMed 19010672 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 4.52 4.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL940 GABAPENTIN 4.0 1 4.52
CHEMBL1059 PREGABALIN 4.0 1 -
CHEMBL258019 1 -
CHEMBL404384 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL940 GABAPENTIN IC50 = 30000.0 nM 4.52
CHEMBL1059 PREGABALIN IC50 = 158000.0 nM -
CHEMBL258019 IC50 > 10000000.0 nM -
CHEMBL404384 IC50 > 10000000.0 nM -