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Assay Detail

CHEMBL650820

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 bovine cortical membranes
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

GABA-A receptor; anion channel (CHEMBL2094107)
Type PROTEIN COMPLEX GROUP
Organism Bos taurus

Publication

Synthesis, structure-activity relationships, and molecular modeling studies of N-(indol-3-ylglyoxylyl)benzylamine derivatives acting at the benzodiazepine receptor.
Da Settimo A, Primofiore G, Da Settimo F, Marini AM, Novellino E, Greco G, Martini C, Giannaccini G, Lucacchini A.
J Med Chem (1996) 39 : 5083 -5091
PubMed 8978839 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.52 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL146633 1 7.92
CHEMBL146761 1 7.19
CHEMBL145881 1 6.24
CHEMBL357164 1 6.09
CHEMBL356061 1 5.90
CHEMBL146389 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL146633 Ki = 12.0 nM 7.92
CHEMBL146761 Ki = 65.0 nM 7.19
CHEMBL145881 Ki = 570.0 nM 6.24
CHEMBL357164 Ki = 820.0 nM 6.09
CHEMBL356061 Ki = 1260.0 nM 5.90
CHEMBL146389 Ki = 1800.0 nM 5.75