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Assay Detail

CHEMBL2339627

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Binding
Antagonist activity at human GABAC rho1 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Gamma-aminobutyric acid receptor subunit rho-1 (CHEMBL3561)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, Synthesis, and Pharmacological Evaluation of Fluorescent and Biotinylated Antagonists of ρ1 GABAC Receptors.
Gavande N, Kim HL, Doddareddy MR, Johnston GA, Chebib M, Hanrahan JR.
ACS Med Chem Lett (2013) 4 : 402 -407
PubMed 24900684 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.01 5.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL446306 1 5.01
CHEMBL2337889 1 -
CHEMBL2337487 1 -
CHEMBL2337486 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL446306 IC50 = 9760.0 nM 5.01
CHEMBL2337889 IC50 = 147920.0 nM -
CHEMBL2337487 IC50 = 103140.0 nM -
CHEMBL2337486 IC50 = 281420.0 nM -