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Assay Detail

CHEMBL648134

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

Binding
Displacement of [3H]- flunitrazepam from rat GABA-A benzodiazepine receptor
13
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

GABA-A receptor; anion channel (CHEMBL1907607)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Antagonist, partial agonist, and full agonist imidazo[1,5-a]quinoxaline amides and carbamates acting through the GABAA/benzodiazepine receptor.
TenBrink RE, Im WB, Sethy VH, Tang AH, Carter DB.
J Med Chem (1994) 37 : 758 -768
PubMed 8145225 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 8.67 9.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL351822 1 9.24
CHEMBL165458 1 9.16
CHEMBL48418 2 9.15
CHEMBL164243 1 9.12
CHEMBL354385 1 9.11
CHEMBL166874 1 8.85
CHEMBL299133 1 8.82
CHEMBL300633 1 8.72
CHEMBL352974 1 8.40
CHEMBL349876 1 8.18
CHEMBL165194 1 8.17
CHEMBL911 ZOLPIDEM 4.0 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL351822 Ki = 0.58 nM 9.24
CHEMBL165458 Ki = 0.69 nM 9.16
CHEMBL48418 Ki = 0.71 nM 9.15
CHEMBL164243 Ki = 0.76 nM 9.12
CHEMBL354385 Ki = 0.77 nM 9.11
CHEMBL166874 Ki = 1.4 nM 8.85
CHEMBL299133 Ki = 1.5 nM 8.82
CHEMBL300633 Ki = 1.9 nM 8.72
CHEMBL352974 Ki = 4.0 nM 8.40
CHEMBL349876 Ki = 6.6 nM 8.18
CHEMBL165194 Ki = 6.7 nM 8.17
CHEMBL48418 Ki = 6.8 nM 8.17
CHEMBL911 ZOLPIDEM Ki = 25.0 nM 7.60