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Assay Detail

CHEMBL650287

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
11
Total Activities
11
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 11 7.16 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL330116 1 8.40
CHEMBL318552 1 8.00
CHEMBL329300 1 7.00
CHEMBL317375 1 6.89
CHEMBL330209 1 6.70
CHEMBL432061 1 6.70
CHEMBL318288 1 6.46
CHEMBL329504 1 -
CHEMBL97928 1 -
CHEMBL319071 1 -
CHEMBL327283 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL330116 IC50 = 4.0 nM 8.40
CHEMBL318552 IC50 = 10.0 nM 8.00
CHEMBL329300 IC50 = 100.0 nM 7.00
CHEMBL317375 IC50 = 130.0 nM 6.89
CHEMBL330209 IC50 = 200.0 nM 6.70
CHEMBL432061 IC50 = 200.0 nM 6.70
CHEMBL318288 IC50 = 350.0 nM 6.46
CHEMBL329504 IC50 > 10000.0 nM -
CHEMBL97928 IC50 > 10000.0 nM -
CHEMBL319071 IC50 > 1000.0 nM -
CHEMBL327283 IC50 > 1000.0 nM -