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Assay Detail

CHEMBL681450

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

Functional
Compound was tested for its ability to inhibit uptake of [3H]- GABA by cloned human GAT-1 transporter
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Sodium- and chloride-dependent GABA transporter 1 (CHEMBL1903)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

On the bioactive conformation of the gaba uptake inhibitor SK&F 89976-A
Murali Dhar T, Nakanishi H, Borden LA, Gluchowski C
Bioorg Med Chem Lett (1996) 6 : 1535 -1540
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.89 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38686 1 6.89
CHEMBL2093978 1 -
CHEMBL2094022 1 -
CHEMBL2093977 1 -
CHEMBL2094024 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38686 IC50 = 130.0 nM 6.89
CHEMBL2093978 IC50 = 632000.0 nM -
CHEMBL2094022 IC50 = 270000.0 nM -
CHEMBL2093977 IC50 = 809000.0 nM -
CHEMBL2094024 IC50 = 270000.0 nM -