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Assay Detail

CHEMBL871684

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Binding
Binding affinity for rat alpha-1 beta2/3 gamma2 GABA A / BzR receptor
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

A novel selective GABA(A) alpha1 receptor agonist displaying sedative and anxiolytic-like properties in rodents.
Selleri S, Bruni F, Costagli C, Costanzo A, Guerrini G, Ciciani G, Gratteri P, Besnard F, Costa B, Montali M, Martini C, Fohlin J, De Siena G, Aiello PM.
J Med Chem (2005) 48 : 6756 -6760
PubMed 16220991 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.64 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12 DIAZEPAM 4.0 1 7.85
CHEMBL911 ZOLPIDEM 4.0 1 7.57
CHEMBL196305 1 7.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12 DIAZEPAM Ki = 14.0 nM 7.85
CHEMBL911 ZOLPIDEM Ki = 26.7 nM 7.57
CHEMBL196305 Ki = 31.0 nM 7.51