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Assay Detail

CHEMBL904138

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

Binding
Displacement of [3H]Ro15-1788 from rat recombinant GABA alpha-3-beta-2-gamma-2 receptor expressed in HEK293 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

GABA A receptor alpha-3/beta-2/gamma-2 (CHEMBL2111343)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Novel 3-iodo-8-ethoxypyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide as promising lead for design of alpha5-inverse agonist useful tools for therapy of mnemonic damage.
Guerrini G, Ciciani G, Cambi G, Bruni F, Selleri S, Besnard F, Montali M, Martini C, Ghelardini C, Galeotti N, Costanzo A.
Bioorg Med Chem (2007) 15 : 2573 -2586
PubMed 17306981 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.53 7.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL229145 1 7.91
CHEMBL12 DIAZEPAM 4.0 1 7.85
CHEMBL229144 1 7.47
CHEMBL388601 1 6.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL229145 Ki = 12.3 nM 7.91
CHEMBL12 DIAZEPAM Ki = 14.0 nM 7.85
CHEMBL229144 Ki = 34.0 nM 7.47
CHEMBL388601 Ki = 133.0 nM 6.88