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Assay Detail

CHEMBL679655

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

Binding
Inhibition of [3H]CGP-27492 binding to Gamma-aminobutyric acid type B receptor of rat cortex
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 7 — Homologous single protein target
Curated By Expert

Target

GABA B receptor (CHEMBL2111474)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
Froestl W, Mickel SJ, Hall RG, von Sprecher G, Strub D, Baumann PA, Brugger F, Gentsch C, Jaekel J, Olpe HR.
J Med Chem (1995) 38 : 3297 -3312
PubMed 7650684 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.84 10.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL112710 1 10.80
CHEMBL112203 1 8.27
CHEMBL96 GAMMA-AMINOBUTYRIC ACID 1.0 1 7.77
CHEMBL301742 ARBACLOFEN 3.0 1 7.50
CHEMBL701 BACLOFEN 4.0 1 6.97
CHEMBL325921 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL112710 IC50 = 0.016 nM 10.80
CHEMBL112203 IC50 = 5.4 nM 8.27
CHEMBL96 GAMMA-AMINOBUTYRIC ACID IC50 = 17.0 nM 7.77
CHEMBL301742 ARBACLOFEN IC50 = 32.0 nM 7.50
CHEMBL701 BACLOFEN IC50 = 107.0 nM 6.97
CHEMBL325921 IC50 = 1979.0 nM 5.70