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Assay Detail

CHEMBL1638616

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

Binding
Binding affinity to human alpha5beta3gamma2 GABA receptor expressed in Xenopus laevis oocytes
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

GABA-A receptor; alpha-5/beta-3/gamma-2 (CHEMBL2094122)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Developing dual functional allosteric modulators of GABA(A) receptors.
Liu XF, Chang HF, Schmiesing RJ, Wesolowski SS, Knappenberger KS, Arriza JL, Chapdelaine MJ.
Bioorg Med Chem (2010) 18 : 8374 -8382
PubMed 20980155 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 6.97 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL17468 1 8.52
CHEMBL12 DIAZEPAM 4.0 1 7.35
CHEMBL1631466 1 6.69
CHEMBL1631467 1 6.34
CHEMBL1631468 1 5.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL17468 EC50 = 3.0 nM 8.52
CHEMBL12 DIAZEPAM EC50 = 45.0 nM 7.35
CHEMBL1631466 EC50 = 206.0 nM 6.69
CHEMBL1631467 EC50 = 455.0 nM 6.34
CHEMBL1631468 EC50 = 1130.0 nM 5.95