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Assay Detail

CHEMBL650833

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

Binding
Inhibition of [3H]-Ro- 15-1788 binding to GABA-A benzodiazepine receptor in rat brain membrane
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Computer-aided molecular modeling, synthesis, and biological evaluation of 8-(benzyloxy)-2-phenylpyrazolo[4,3-c]quinoline as a novel benzodiazepine receptor agonist ligand.
Wang CG, Langer T, Kamath PG, Gu ZQ, Skolnick P, Fryer RI.
J Med Chem (1995) 38 : 950 -957
PubMed 7699711 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.54 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10483 1 9.30
CHEMBL3144700 1 9.17
CHEMBL3144823 1 9.13
CHEMBL1518572 1 9.00
CHEMBL3144860 1 8.43
CHEMBL11709 1 8.30
CHEMBL12 DIAZEPAM 4.0 1 7.69
CHEMBL3144703 1 7.28
CHEMBL3144702 1 -
CHEMBL3144699 1 -
CHEMBL3144701 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10483 IC50 = 0.5 nM 9.30
CHEMBL3144700 IC50 = 0.68 nM 9.17
CHEMBL3144823 IC50 = 0.74 nM 9.13
CHEMBL1518572 IC50 = 1.0 nM 9.00
CHEMBL3144860 IC50 = 3.7 nM 8.43
CHEMBL11709 IC50 = 5.0 nM 8.30
CHEMBL12 DIAZEPAM IC50 = 20.6 nM 7.69
CHEMBL3144703 IC50 = 52.3 nM 7.28
CHEMBL3144702 IC50 > 1000000.0 nM -
CHEMBL3144699 IC50 > 1000.0 nM -
CHEMBL3144701 IC50 > 1000.0 nM -