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Assay Detail

CHEMBL682871

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

Binding
Inhibition of [3H]-baclofen binding to Gamma-aminobutyric acid type B receptor of cat cerebellum
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Felis catus
Tissue Cerebellum
Confidence 6 — Multiple protein complex / RNA
Curated By Expert

Target

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

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 14 6.74 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL112203 1 8.62
CHEMBL112710 1 8.18
CHEMBL301742 ARBACLOFEN 3.0 1 7.82
CHEMBL113453 1 7.75
CHEMBL96 GAMMA-AMINOBUTYRIC ACID 1.0 1 7.60
CHEMBL701 BACLOFEN 4.0 1 7.46
CHEMBL113217 1 6.55
CHEMBL113907 1 6.30
CHEMBL111920 1 6.11
CHEMBL111675 1 6.04
CHEMBL325921 1 5.87
CHEMBL302213 1 5.75
CHEMBL324917 1 5.36
CHEMBL112960 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL112203 IC50 = 2.4 nM 8.62
CHEMBL112710 IC50 = 6.6 nM 8.18
CHEMBL301742 ARBACLOFEN IC50 = 15.0 nM 7.82
CHEMBL113453 IC50 = 18.0 nM 7.75
CHEMBL96 GAMMA-AMINOBUTYRIC ACID IC50 = 25.0 nM 7.60
CHEMBL701 BACLOFEN IC50 = 35.0 nM 7.46
CHEMBL113217 IC50 = 280.0 nM 6.55
CHEMBL113907 IC50 = 500.0 nM 6.30
CHEMBL111920 IC50 = 780.0 nM 6.11
CHEMBL111675 IC50 = 920.0 nM 6.04
CHEMBL325921 IC50 = 1350.0 nM 5.87
CHEMBL302213 IC50 = 1770.0 nM 5.75
CHEMBL324917 IC50 = 4410.0 nM 5.36
CHEMBL112960 IC50 = 12800.0 nM 4.89