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Assay Detail

CHEMBL650835

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Binding
Inhibitory activity against specific binding of [3H]-CB 34 to peripheral benzodiazepine receptor in rat cortical membranes was evaluated
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Translocator protein (CHEMBL4552)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-activity relationships in carboxamide derivatives based on the targeted delivery of radionuclides and boron atoms by means of peripheral benzodiazepine receptor ligands.
Cappelli A, Pericot Mohr Gl, Gallelli A, Giuliani G, Anzini M, Vomero S, Fresta M, Porcu P, Maciocco E, Concas A, Biggio G, Donati A.
J Med Chem (2003) 46 : 3568 -3571
PubMed 12904061 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.23 9.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL333792 1 9.35
CHEMBL325820 1 8.66
CHEMBL15248 1 8.34
CHEMBL481537 PK-11195 1 8.08
CHEMBL120668 1 8.06
CHEMBL121674 1 8.01
CHEMBL120763 1 7.96
CHEMBL331928 1 7.92
CHEMBL119829 1 7.89
CHEMBL119787 1 7.50
CHEMBL332775 1 7.42
CHEMBL325701 1 7.19
CHEMBL122301 1 5.83
CHEMBL119566 1 5.57
CHEMBL332801 1 5.18
CHEMBL416162 1 4.99
CHEMBL120398 1 4.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL333792 IC50 = 0.45 nM 9.35
CHEMBL325820 IC50 = 2.2 nM 8.66
CHEMBL15248 IC50 = 4.6 nM 8.34
CHEMBL481537 PK-11195 IC50 = 8.4 nM 8.08
CHEMBL120668 IC50 = 8.7 nM 8.06
CHEMBL121674 IC50 = 9.8 nM 8.01
CHEMBL120763 IC50 = 11.0 nM 7.96
CHEMBL331928 IC50 = 12.0 nM 7.92
CHEMBL119829 IC50 = 13.0 nM 7.89
CHEMBL119787 IC50 = 32.0 nM 7.50
CHEMBL332775 IC50 = 38.0 nM 7.42
CHEMBL325701 IC50 = 64.0 nM 7.19
CHEMBL122301 IC50 = 1490.0 nM 5.83
CHEMBL119566 IC50 = 2700.0 nM 5.57
CHEMBL332801 IC50 = 6600.0 nM 5.18
CHEMBL416162 IC50 = 10270.0 nM 4.99
CHEMBL120398 IC50 = 11500.0 nM 4.94