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Assay Detail

CHEMBL817276

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Functional
In vitro inhibition of [3H]GABA uptake determined
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Synthesis of novel gamma-aminobutyric acid (GABA) uptake inhibitors. 5.(1) Preparation and structure-activity studies of tricyclic analogues of known GABA uptake inhibitors.
Andersen KE, Sørensen JL, Lau J, Lundt BF, Petersen H, Huusfeldt PO, Suzdak PD, Swedberg MD.
J Med Chem (2001) 44 : 2152 -2163
PubMed 11405652 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.24 7.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL539775 1 7.06
CHEMBL542875 1 5.99
CHEMBL540029 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL539775 IC50 = 87.0 nM 7.06
CHEMBL542875 IC50 = 1031.0 nM 5.99
CHEMBL540029 IC50 = 2177.0 nM 5.66