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Assay Detail

CHEMBL832370

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

Binding
In vitro inhibitory activity against [3H]-GABA transport in rat cerebrocortical membranes in the presence of NNC-711 (100 uM); Phase 1
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Expert

Target

GABA transporter (CHEMBL2111478)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Novel secoergoline derivatives inhibit both GABA and glutamate uptake in rat brain homogenates: synthesis, in vitro pharmacology, and modeling.
Héja L, Kovács I, Szárics E, Incze M, Temesváriné-Major E, Dörnyei G, Peredy-Kajtár M, Gács-Baitz E, Szántay C, Kardos J.
J Med Chem (2004) 47 : 5620 -5629
PubMed 15509161 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.51 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL534702 1 8.43
CHEMBL540611 1 7.36
CHEMBL558391 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL534702 IC50 = 3.7 nM 8.43
CHEMBL540611 IC50 = 44.0 nM 7.36
CHEMBL558391 IC50 = 180.0 nM 6.75