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Assay Detail

CHEMBL652657

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 cerebral cortical membranes at 10 uM
7
Total Activities
7
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

Benzodiazepine receptor affinity and interaction of some N-(indol-3-ylglyoxylyl)amine derivatives.
Bianucci AM, Da Settimo A, Da Settimo F, Primofiore G, Martini C, Giannaccini G, Lucacchini A.
J Med Chem (1992) 35 : 2214 -2220
PubMed 1319492 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.17 9.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL407 FLUMAZENIL 4.0 1 9.42
CHEMBL11908 1 8.92
CHEMBL12 DIAZEPAM 4.0 1 8.00
CHEMBL307644 1 6.55
CHEMBL71304 1 6.00
CHEMBL71424 1 5.92
CHEMBL304527 1 5.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL407 FLUMAZENIL Ki = 0.38 nM 9.42
CHEMBL11908 Ki = 1.2 nM 8.92
CHEMBL12 DIAZEPAM Ki = 10.0 nM 8.00
CHEMBL307644 Ki = 280.0 nM 6.55
CHEMBL71304 Ki = 1000.0 nM 6.00
CHEMBL71424 Ki = 1200.0 nM 5.92
CHEMBL304527 Ki = 4200.0 nM 5.38