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Assay Detail

CHEMBL652656

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

Binding
Binding affinity to BZR receptor on bovine cerebral cortex by [3H]flunitrazepam displacement.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

Structure-activity relationships of 1,2,4-triazolo[1,5-a] quinoxalines and their 1-deaza analogues imidazo[1,2-a]quinoxalines at the benzodiazepine receptor.
Catarzi D, Cecchi L, Colotta V, Melani F, Filacchioni G, Martini C, Giusti L, Lucacchini A.
J Med Chem (1994) 37 : 2846 -2850
PubMed 8071933 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.68 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL97569 1 8.54
CHEMBL98678 1 8.27
CHEMBL97372 1 8.05
CHEMBL327853 1 8.01
CHEMBL317545 1 7.88
CHEMBL316824 1 7.84
CHEMBL97286 1 7.80
CHEMBL95396 1 7.80
CHEMBL94830 1 7.76
CHEMBL328437 1 7.66
CHEMBL317815 1 7.53
CHEMBL319058 1 7.48
CHEMBL97349 1 7.37
CHEMBL99026 1 7.25
CHEMBL98509 1 7.17
CHEMBL330399 1 7.15
CHEMBL99178 1 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL97569 Ki = 2.9 nM 8.54
CHEMBL98678 Ki = 5.4 nM 8.27
CHEMBL97372 Ki = 8.9 nM 8.05
CHEMBL327853 Ki = 9.8 nM 8.01
CHEMBL317545 Ki = 13.2 nM 7.88
CHEMBL316824 Ki = 14.5 nM 7.84
CHEMBL97286 Ki = 15.9 nM 7.80
CHEMBL95396 Ki = 15.9 nM 7.80
CHEMBL94830 Ki = 17.4 nM 7.76
CHEMBL328437 Ki = 21.8 nM 7.66
CHEMBL317815 Ki = 29.8 nM 7.53
CHEMBL319058 Ki = 32.8 nM 7.48
CHEMBL97349 Ki = 42.3 nM 7.37
CHEMBL99026 Ki = 56.4 nM 7.25
CHEMBL98509 Ki = 67.5 nM 7.17
CHEMBL330399 Ki = 71.2 nM 7.15
CHEMBL99178 Ki = 87.8 nM 7.06