Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL650876

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

Binding
Inhibition of [3H]-diazepam binding to GABA-A benzodiazepine receptor of rat cerebral cortical membranes
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
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

Synthesis of 7,12-dihydropyrido[3,4-b:5,4-b']diindoles. A novel class of rigid, planar benzodiazepine receptor ligands.
Trudell ML, Basile AS, Shannon HE, Skolnick P, Cook JM.
J Med Chem (1987) 30 : 456 -458
PubMed 3029372 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.33 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301605 1 8.40
CHEMBL79945 1 8.15
CHEMBL141039 1 8.10
CHEMBL439945 1 8.00
CHEMBL311747 1 7.92
CHEMBL310167 1 7.80
CHEMBL78650 1 7.10
CHEMBL302056 1 6.15
CHEMBL343107 1 6.05
CHEMBL312333 1 5.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL301605 IC50 = 4.0 nM 8.40
CHEMBL79945 IC50 = 7.0 nM 8.15
CHEMBL141039 IC50 = 8.0 nM 8.10
CHEMBL439945 IC50 = 10.0 nM 8.00
CHEMBL311747 IC50 = 12.0 nM 7.92
CHEMBL310167 IC50 = 16.0 nM 7.80
CHEMBL78650 IC50 = 80.0 nM 7.10
CHEMBL302056 IC50 = 715.0 nM 6.15
CHEMBL343107 IC50 = 890.0 nM 6.05
CHEMBL312333 IC50 = 2150.0 nM 5.67