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Assay Detail

CHEMBL866255

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

Functional
Inhibition of potassium-evoked [3H]norepinephrine release from rat neocortex
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Neocortex
Confidence 9 — Direct single protein target
Curated By Expert

Target

Voltage-dependent calcium channel subunit alpha-2/delta-1 (CHEMBL3420)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Carboxylate bioisosteres of gabapentin.
Burgos-Lepley CE, Thompson LR, Kneen CO, Osborne SA, Bryans JS, Capiris T, Suman-Chauhan N, Dooley DJ, Donovan CM, Field MJ, Vartanian MG, Kinsora JJ, Lotarski SM, El-Kattan A, Walters K, Cherukury M, Taylor CP, Wustrow DJ, Schwarz JB.
Bioorg Med Chem Lett (2006) 16 : 2333 -2336
PubMed 15946842 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.15 5.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL378552 1 5.24
CHEMBL940 GABAPENTIN 4.0 1 5.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL378552 IC50 = 5700.0 nM 5.24
CHEMBL940 GABAPENTIN IC50 = 8900.0 nM 5.05