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Assay Detail

CHEMBL678330

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

Binding
Displacement of [3H]Ro-151788 from human GABA-A receptor alpha-1-beta-3-gamma-2 subunits expressed in L(tk-) cells
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

GABA-A receptor; alpha-1/beta-3/gamma-2 (CHEMBL2094121)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.
Collins I, Moyes C, Davey WB, Rowley M, Bromidge FA, Quirk K, Atack JR, McKernan RM, Thompson SA, Wafford K, Dawson GR, Pike A, Sohal B, Tsou NN, Ball RG, Castro JL.
J Med Chem (2002) 45 : 1887 -1900
PubMed 11960500 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 6.19 6.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301195 1 6.20
CHEMBL291335 1 6.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL301195 Ki = 625.0 nM 6.20
CHEMBL291335 Ki = 680.0 nM 6.17