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Assay Detail

CHEMBL964516

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Functional
Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Oocyte
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Gamma-aminobutyric acid type B receptor subunit 1 (CHEMBL2064)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel gamma-aminobutyric acid rho1 receptor antagonists; synthesis, pharmacological activity and structure-activity relationships.
Kumar RJ, Chebib M, Hibbs DE, Kim HL, Johnston GA, Salam NK, Hanrahan JR.
J Med Chem (2008) 51 : 3825 -3840
PubMed 18528996 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 4.62 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL96 GAMMA-AMINOBUTYRIC ACID 1.0 1 5.77
CHEMBL504482 1 4.29
CHEMBL447171 1 4.28
CHEMBL445449 1 4.14
CHEMBL397209 1 -
CHEMBL355921 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL96 GAMMA-AMINOBUTYRIC ACID EC50 = 1700.0 nM 5.77
CHEMBL504482 EC50 = 51000.0 nM 4.29
CHEMBL447171 EC50 = 52200.0 nM 4.28
CHEMBL445449 EC50 = 71900.0 nM 4.14
CHEMBL397209 EC50 = 500000.0 nM -
CHEMBL355921 EC50 - -