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Assay Detail

CHEMBL651948

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

Binding
In vitro inhibition of [3H]flunitrazepam binding to GABA-A Benzodiazepine receptor of rat cerebral cortex membranes
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
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

Structural requirements for agonist actions at the benzodiazepine receptor: studies with analogues of 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester.
Hollinshead SP, Trudell ML, Skolnick P, Cook JM.
J Med Chem (1990) 33 : 1062 -1069
PubMed 1968513 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 8.22 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10483 1 9.30
CHEMBL10195 1 9.05
CHEMBL1518572 1 9.00
CHEMBL10534 1 8.64
CHEMBL10597 1 8.05
CHEMBL268262 1 8.00
CHEMBL273464 1 7.66
CHEMBL276377 1 6.03
CHEMBL10701 1 -
CHEMBL10638 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10483 IC50 = 0.5 nM 9.30
CHEMBL10195 IC50 = 0.9 nM 9.05
CHEMBL1518572 IC50 = 1.0 nM 9.00
CHEMBL10534 IC50 = 2.3 nM 8.64
CHEMBL10597 IC50 = 8.9 nM 8.05
CHEMBL268262 IC50 = 10.0 nM 8.00
CHEMBL273464 IC50 = 22.0 nM 7.66
CHEMBL276377 IC50 = 945.0 nM 6.03
CHEMBL10701 IC50 > 5000.0 nM -
CHEMBL10638 IC50 > 5000.0 nM -