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Assay Detail

CHEMBL653042

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

Binding
Displacement of [3H]diazepam from GABA-A Benzodiazepine receptor of rat forebrain
3
Total Activities
3
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

Synthesis and benzodiazepine binding activity of a series of novel [1,2,4]triazolo[1,5-c]quinazolin-5(6H)-ones.
Francis JE, Cash WD, Barbaz BS, Bernard PS, Lovell RA, Mazzenga GC, Friedmann RC, Hyun JL, Braunwalder AF, Loo PS.
J Med Chem (1991) 34 : 281 -290
PubMed 1846920 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.91 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19732 CGS-8216 1 9.52
CHEMBL13280 FLUNITRAZEPAM 4.0 1 8.82
CHEMBL12 DIAZEPAM 4.0 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19732 CGS-8216 IC50 = 0.3 nM 9.52
CHEMBL13280 FLUNITRAZEPAM IC50 = 1.5 nM 8.82
CHEMBL12 DIAZEPAM IC50 = 4.0 nM 8.40