Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL651678

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

Binding
In vitro binding affinity (pIC50) was tested against peripheral benzodiazepine receptor (PBR) in rat.
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Translocator protein (CHEMBL4552)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Mapping the peripheral benzodiazepine receptor binding site by conformationally restrained derivatives of 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3- isoquinolinecarboxamide (PK11195).
Cappelli A, Anzini M, Vomero S, De Benedetti PG, Menziani MC, Giorgi G, Manzoni C.
J Med Chem (1997) 40 : 2910 -2921
PubMed 9288173 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 7.30 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL15248 1 8.68
CHEMBL276756 1 8.68
CHEMBL481537 PK-11195 1 8.66
CHEMBL15003 1 8.54
CHEMBL280482 1 8.51
CHEMBL15254 1 8.47
CHEMBL275410 1 8.19
CHEMBL14956 1 8.06
CHEMBL15237 1 8.05
CHEMBL276341 1 8.01
CHEMBL416713 1 8.00
CHEMBL278011 1 7.95
CHEMBL280035 1 7.89
CHEMBL15714 1 7.34
CHEMBL277586 1 6.77
CHEMBL14920 1 6.64
CHEMBL15584 1 6.57
CHEMBL15315 1 6.32
CHEMBL15630 1 6.31
CHEMBL15239 1 6.26
CHEMBL15316 1 6.21
CHEMBL15255 1 6.10
CHEMBL429386 1 6.09
CHEMBL416162 1 5.92
CHEMBL15473 1 5.92
CHEMBL15709 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL15248 IC50 = 2.089 nM 8.68
CHEMBL276756 IC50 = 2.089 nM 8.68
CHEMBL481537 PK-11195 IC50 = 2.188 nM 8.66
CHEMBL15003 IC50 = 2.884 nM 8.54
CHEMBL280482 IC50 = 3.09 nM 8.51
CHEMBL15254 IC50 = 3.388 nM 8.47
CHEMBL275410 IC50 = 6.457 nM 8.19
CHEMBL14956 IC50 = 8.71 nM 8.06
CHEMBL15237 IC50 = 8.913 nM 8.05
CHEMBL276341 IC50 = 9.772 nM 8.01
CHEMBL416713 IC50 = 10.0 nM 8.00
CHEMBL278011 IC50 = 11.22 nM 7.95
CHEMBL280035 IC50 = 12.88 nM 7.89
CHEMBL15714 IC50 = 45.71 nM 7.34
CHEMBL277586 IC50 = 169.82 nM 6.77
CHEMBL14920 IC50 = 229.09 nM 6.64
CHEMBL15584 IC50 = 269.15 nM 6.57
CHEMBL15315 IC50 = 478.63 nM 6.32
CHEMBL15630 IC50 = 489.78 nM 6.31
CHEMBL15239 IC50 = 549.54 nM 6.26
CHEMBL15316 IC50 = 616.6 nM 6.21
CHEMBL15255 IC50 = 794.33 nM 6.10
CHEMBL429386 IC50 = 812.83 nM 6.09
CHEMBL416162 IC50 = 1202.26 nM 5.92
CHEMBL15473 IC50 = 1202.26 nM 5.92
CHEMBL15709 IC50 = 1698.24 nM 5.77