Assay Detail

CHEMBL853069

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

Binding

Displacement of [3H]Ro 15-1788 from recombinant human GABAA alpha3 receptor plus beta-3-gamma-2 expressed in L(tk-) cells

ChEMBL ↗

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Target

GABA-A receptor; alpha-3/beta-3/gamma-2 (CHEMBL2094120) ↗

Open DB target context

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GABA-A receptor; alpha-3/beta-3/gamma-2 (CHEMBL2094120) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target GABA-A receptor; alpha-3/beta-3/gamma-2

CHEMBL2094120

Anchored from Assay target.

Protein identity GABA-A receptor; alpha-3/beta-3/gamma-2

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

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

Target

GABA-A receptor; alpha-3/beta-3/gamma-2 (CHEMBL2094120) ↗

Type	PROTEIN COMPLEX
Organism	Homo sapiens

Publication

Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety.

Russell MG, Carling RW, Street LJ, Hallett DJ, Goodacre S, Mezzogori E, Reader M, Cook SM, Bromidge FA, Newman R, Smith AJ, Wafford KA, Marshall GR, Reynolds DS, Dias R, Ferris P, Stanley J, Lincoln R, Tye SJ, Sheppard WF, Sohal B, Pike A, Dominguez M, Atack JR, Castro JL.
J Med Chem (2006) 49 : 1235 -1238
PubMed 16480260 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	1	8.70	8.70

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL204696	—	—	1	8.70

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL204696	—	Ki	=	2.0	nM	8.70