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

CHEMBL828392

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

Functional
Inhibition of [3H]leucine uptake into CHO cells by L-amino acid transporters
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Structure-activity relationships of pregabalin and analogues that target the alpha(2)-delta protein.
Belliotti TR, Capiris T, Ekhato IV, Kinsora JJ, Field MJ, Heffner TG, Meltzer LT, Schwarz JB, Taylor CP, Thorpe AJ, Vartanian MG, Wise LD, Zhi-Su T, Weber ML, Wustrow DJ.
J Med Chem (2005) 48 : 2294 -2307
PubMed 15801823 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 4.34 4.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL365562 1 4.55
CHEMBL940 GABAPENTIN 4.0 1 4.52
CHEMBL190656 1 4.22
CHEMBL435129 1 4.05
CHEMBL1059 PREGABALIN 4.0 1 -
CHEMBL167003 1 -
CHEMBL190074 1 -
CHEMBL363579 1 -
CHEMBL363611 1 -
CHEMBL193353 1 -
CHEMBL364743 1 -
CHEMBL192532 1 -
CHEMBL365160 1 -
CHEMBL363005 1 -
CHEMBL190602 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL365562 IC50 = 28000.0 nM 4.55
CHEMBL940 GABAPENTIN IC50 = 30000.0 nM 4.52
CHEMBL190656 IC50 = 60000.0 nM 4.22
CHEMBL435129 IC50 = 89000.0 nM 4.05
CHEMBL1059 PREGABALIN IC50 = 158000.0 nM -
CHEMBL167003 IC50 = 355000.0 nM -
CHEMBL190074 IC50 = 142000.0 nM -
CHEMBL363579 IC50 = 146000.0 nM -
CHEMBL363611 IC50 > 10000000.0 nM -
CHEMBL193353 IC50 = 117000.0 nM -
CHEMBL364743 IC50 > 100000000.0 nM -
CHEMBL192532 IC50 > 8300000.0 nM -
CHEMBL365160 IC50 > 8300000.0 nM -
CHEMBL363005 IC50 > 10000000.0 nM -
CHEMBL190602 IC50 = 157000.0 nM -