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Assay Detail

CHEMBL1679957

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

Functional
Antagonist activity at human recombinant GABAb 1b/2 receptor expressed in Xenopus laevis oocytes co-expressing GIRK1/4 assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
2
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Oocyte
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

GABA-B receptor (CHEMBL2111463)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Novel Cyclic Phosphinic Acids as GABAC ρ Receptor Antagonists: Design, Synthesis, and Pharmacology.
Gavande N, Yamamoto I, Salam NK, Ai TH, Burden PM, Johnston GA, Hanrahan JR, Chebib M.
ACS Med Chem Lett (2011) 2 : 11 -16
PubMed 24900248 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.42 4.42
EC50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL112797 SGS-742 2.0 1 4.42
CHEMBL397209 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL112797 SGS-742 IC50 = 38000.0 nM 4.42
CHEMBL397209 EC50 = 500000.0 nM -