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Assay Detail

CHEMBL679643

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

Binding
In vitro displacement of [3H]GABA from Gamma-aminobutyric acid type B receptor sites in rat brain membranes
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Biological activity of 3-aminopropyl (methyl) phosphinic acid, a potent and selective GABAB agonist with CNS activity
Howson W, Mistry J, Broekman m, Hills JM
Bioorg Med Chem Lett (1993) 3 : 515 -518
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.75 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL112710 1 9.00
CHEMBL112203 1 8.52
CHEMBL701 BACLOFEN 4.0 1 7.52
CHEMBL96 GAMMA-AMINOBUTYRIC ACID 1.0 1 7.22
CHEMBL113571 1 6.00
CHEMBL149082 TRAMIPROSATE 3.0 1 5.70
CHEMBL286077 1 5.70
CHEMBL40157 1 5.60
CHEMBL325921 1 5.52
CHEMBL341858 1 -
CHEMBL146972 PHOSPHORYLETHANOLAMINE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL112710 IC50 = 1.0 nM 9.00
CHEMBL112203 IC50 = 3.0 nM 8.52
CHEMBL701 BACLOFEN IC50 = 30.0 nM 7.52
CHEMBL96 GAMMA-AMINOBUTYRIC ACID IC50 = 60.0 nM 7.22
CHEMBL113571 IC50 = 1000.0 nM 6.00
CHEMBL149082 TRAMIPROSATE IC50 = 2000.0 nM 5.70
CHEMBL286077 IC50 = 2000.0 nM 5.70
CHEMBL40157 IC50 = 2500.0 nM 5.60
CHEMBL325921 IC50 = 3000.0 nM 5.52
CHEMBL341858 IC50 > 100000.0 nM -
CHEMBL146972 PHOSPHORYLETHANOLAMINE IC50 > 100000.0 nM -