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Assay Detail

CHEMBL2353552

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

Binding
Displacement of [3H]Ro15-1788 from recombinant GABA-A alpha1beta2gamma2 receptor benzodiazepine binding site (unknown origin) after 1 hr
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-2/gamma-2 (CHEMBL2095172)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Synthesis of novel cognition enhancers with pyrazolo[5,1-c][1,2,4]benzotriazine core acting at γ-aminobutyric acid type A (GABA(A)) receptor.
Guerrini G, Ciciani G, Costanzo A, Daniele S, Martini C, Ghelardini C, Di Cesare Mannelli L, Ciattini S.
Bioorg Med Chem (2013) 21 : 2186 -2198
PubMed 23490154 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.50 9.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2348441 1 9.35
CHEMBL2348446 1 7.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2348441 Ki = 0.45 nM 9.35
CHEMBL2348446 Ki = 22.7 nM 7.64