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Assay Detail

CHEMBL679644

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

Binding
Inhibition of [3H]baclofen binding to rat gamma-aminobutyric acid type B receptor.
18
Total Activities
17
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

3-Thienyl- and 3-furylaminobutyric acids. Synthesis and binding GABAB receptor studies.
Berthelot P, Vaccher C, Flouquet N, Debaert M, Luyckx M, Brunet C.
J Med Chem (1991) 34 : 2557 -2560
PubMed 1652022 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.66 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL96 GAMMA-AMINOBUTYRIC ACID 1.0 1 7.40
CHEMBL701 BACLOFEN 4.0 2 6.75
CHEMBL87482 4-AMINO-3- (5-CHLOROTHIEN-2-YL)BUTANOIC ACID 1 6.21
CHEMBL83245 1 6.10
CHEMBL301492 1 5.88
CHEMBL86144 1 5.87
CHEMBL314177 1 5.73
CHEMBL315476 1 5.01
CHEMBL315789 1 4.70
CHEMBL87856 1 4.68
CHEMBL315950 1 4.41
CHEMBL85948 1 4.34
CHEMBL83011 1 -
CHEMBL85880 1 -
CHEMBL53073 1 -
CHEMBL315440 1 -
CHEMBL313323 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL96 GAMMA-AMINOBUTYRIC ACID IC50 = 40.0 nM 7.40
CHEMBL701 BACLOFEN IC50 = 180.0 nM 6.75
CHEMBL701 BACLOFEN IC50 = 330.0 nM 6.48
CHEMBL87482 4-AMINO-3- (5-CHLOROTHIEN-2-YL)BUTANOIC ACID IC50 = 610.0 nM 6.21
CHEMBL83245 IC50 = 800.0 nM 6.10
CHEMBL301492 IC50 = 1330.0 nM 5.88
CHEMBL86144 IC50 = 1340.0 nM 5.87
CHEMBL314177 IC50 = 1860.0 nM 5.73
CHEMBL315476 IC50 = 9720.0 nM 5.01
CHEMBL315789 IC50 = 20000.0 nM 4.70
CHEMBL87856 IC50 = 20900.0 nM 4.68
CHEMBL315950 IC50 = 39100.0 nM 4.41
CHEMBL85948 IC50 = 45300.0 nM 4.34
CHEMBL83011 IC50 > 100000.0 nM -
CHEMBL85880 IC50 > 100000.0 nM -
CHEMBL53073 IC50 > 100000.0 nM -
CHEMBL315440 IC50 > 100000.0 nM -
CHEMBL313323 IC50 = 124000.0 nM -