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Assay Detail

CHEMBL654243

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

Binding
Inhibitory concentration against [3H]flunitrazepam binding to Benzodiazepine receptor in bovine brain membranes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Brain membranes
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

Pyrazolo[4,5-c]quinolines. 2. Synthesis and specific inhibition of benzodiazepine receptor binding.
Melani F, Cecchi L, Palazzino G, Filacchioni G, Martini C, Pennacchi E, Lucacchini A.
J Med Chem (1986) 29 : 291 -295
PubMed 3005571 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.53 6.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL330083 1 6.58
CHEMBL91040 1 6.00
CHEMBL313315 1 5.57
CHEMBL101206 1 5.47
CHEMBL101154 1 5.36
CHEMBL317317 1 5.05
CHEMBL419527 1 4.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL330083 IC50 = 260.0 nM 6.58
CHEMBL91040 IC50 = 1000.0 nM 6.00
CHEMBL313315 IC50 = 2700.0 nM 5.57
CHEMBL101206 IC50 = 3400.0 nM 5.47
CHEMBL101154 IC50 = 4400.0 nM 5.36
CHEMBL317317 IC50 = 9000.0 nM 5.05
CHEMBL419527 IC50 = 22000.0 nM 4.66