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Assay Detail

CHEMBL651484

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

Binding
Displacement of 3[H]Flunitrazepam from GABA-A central benzodiazepine receptor of bovine brain membranes
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Subcellular Brain membranes
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

1,3-Diarylpyrazolo[4,5-c]- and -[5,4-c]quinolin-4-ones. 4. Synthesis and specific inhibition of benzodiazepine receptor binding.
Palazzino G, Cecchi L, Melani F, Colotta V, Filacchioni G, Martini C, Lucacchini A.
J Med Chem (1987) 30 : 1737 -1742
PubMed 2821257 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.76 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL297126 1 7.16
CHEMBL49558 1 7.05
CHEMBL45788 1 7.00
CHEMBL299156 1 5.96
CHEMBL45871 1 5.94
CHEMBL48374 1 5.82
CHEMBL47336 1 5.52
CHEMBL416648 1 5.52
CHEMBL48989 1 5.51
CHEMBL290037 1 4.68
CHEMBL297272 1 4.52
CHEMBL297153 1 4.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL297126 IC50 = 70.0 nM 7.16
CHEMBL49558 IC50 = 90.0 nM 7.05
CHEMBL45788 IC50 = 100.0 nM 7.00
CHEMBL299156 IC50 = 1100.0 nM 5.96
CHEMBL45871 IC50 = 1160.0 nM 5.94
CHEMBL48374 IC50 = 1500.0 nM 5.82
CHEMBL47336 IC50 = 3000.0 nM 5.52
CHEMBL416648 IC50 = 3000.0 nM 5.52
CHEMBL48989 IC50 = 3100.0 nM 5.51
CHEMBL290037 IC50 = 21000.0 nM 4.68
CHEMBL297272 IC50 = 30000.0 nM 4.52
CHEMBL297153 IC50 = 39000.0 nM 4.41