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Assay Detail

CHEMBL1273611

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

Functional
Agonist activity at human recombinant GABAA alpha-2-beta-3-gamma-2 receptor expressed in Xenopus oocytes at 1 to 10 uM by patch clamp technique
2
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Oocyte
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

GABA-A receptor; alpha-2/beta-3/gamma-2 (CHEMBL2094130)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Design, synthesis, and subtype selectivity of 3,6-disubstituted β-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.
Yin W, Majumder S, Clayton T, Petrou S, VanLinn ML, Namjoshi OA, Ma C, Cromer BA, Roth BL, Platt DM, Cook JM.
Bioorg Med Chem (2010) 18 : 7548 -7564
PubMed 20888240 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 1 - -
Ki 1 6.86 6.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1271047 1 6.86
CHEMBL307783 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1271047 Ki = 137.0 nM 6.86
CHEMBL307783 Activity = 99.0 % -