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Assay Detail

CHEMBL785010

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

Functional
Inhibition of high affinity neuronal GABA uptake by synaptosomes of rat brain membrane
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Brain
Subcellular Synaptosomes
Confidence 5 — Multiple protein complex / RNA
Curated By Expert

Target

GABA transporter (CHEMBL2111478)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Hydroxy- and amino-substituted piperidinecarboxylic acids as gamma-aminobutyric acid agonists and uptake inhibitors.
Jacobsen P, Labouta IM, Schaumburg K, Falch E, Krogsgaard-Larsen P.
J Med Chem (1982) 25 : 1157 -1162
PubMed 6292417 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.29 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL96 GAMMA-AMINOBUTYRIC ACID 1.0 1 5.70
CHEMBL277498 NIPECOTIC ACID 1 5.22
CHEMBL277372 1 4.96
CHEMBL429974 1 -
CHEMBL280511 1 -
CHEMBL16132 1 -
CHEMBL15851 1 -
CHEMBL279998 ISONIPECOTIC ACID 1 -
CHEMBL16226 1 -
CHEMBL16357 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL96 GAMMA-AMINOBUTYRIC ACID IC50 = 2000.0 nM 5.70
CHEMBL277498 NIPECOTIC ACID IC50 = 6000.0 nM 5.22
CHEMBL277372 IC50 = 11000.0 nM 4.96
CHEMBL429974 IC50 = 240000.0 nM -
CHEMBL280511 IC50 > 300000.0 nM -
CHEMBL16132 IC50 > 300000.0 nM -
CHEMBL15851 IC50 = 173000.0 nM -
CHEMBL279998 ISONIPECOTIC ACID IC50 > 300000.0 nM -
CHEMBL16226 IC50 = 203000.0 nM -
CHEMBL16357 IC50 > 300000.0 nM -