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Assay Detail

CHEMBL651182

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

Binding
Displacement of [3H]-PK 11195 from peripheral-type benzodiazepine receptor of rat ovary membranes
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Female gonad
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

Translocator protein (CHEMBL4552)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Novel 2-phenylimidazo[1,2-a]pyridine derivatives as potent and selective ligands for peripheral benzodiazepine receptors: synthesis, binding affinity, and in vivo studies.
Trapani G, Franco M, Latrofa A, Ricciardi L, Carotti A, Serra M, Sanna E, Biggio G, Liso G.
J Med Chem (1999) 42 : 3934 -3941
PubMed 10508441 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 7.60 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL450283 1 8.80
CHEMBL481537 PK-11195 1 8.74
CHEMBL321916 1 8.58
CHEMBL432608 ALPDEM 1 8.58
CHEMBL104686 1 8.55
CHEMBL126262 1 8.55
CHEMBL321069 1 8.37
CHEMBL339816 1 8.34
CHEMBL340938 1 8.24
CHEMBL128407 1 8.13
CHEMBL106237 1 8.11
CHEMBL128147 1 8.10
CHEMBL339530 1 8.06
CHEMBL340752 1 7.98
CHEMBL129028 1 7.88
CHEMBL127057 1 7.80
CHEMBL129162 1 7.68
CHEMBL129511 1 7.64
CHEMBL337917 1 7.57
CHEMBL340201 1 7.48
CHEMBL341361 1 7.48
CHEMBL338378 1 7.38
CHEMBL338634 1 7.31
CHEMBL320366 1 7.02
CHEMBL338442 1 6.92
CHEMBL126286 1 6.75
CHEMBL127060 1 6.52
CHEMBL126730 1 6.41
CHEMBL128093 1 6.35
CHEMBL128491 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL450283 IC50 = 1.585 nM 8.80
CHEMBL481537 PK-11195 IC50 = 1.82 nM 8.74
CHEMBL321916 IC50 = 2.63 nM 8.58
CHEMBL432608 ALPDEM IC50 = 2.63 nM 8.58
CHEMBL104686 IC50 = 2.818 nM 8.55
CHEMBL126262 IC50 = 2.818 nM 8.55
CHEMBL321069 IC50 = 4.266 nM 8.37
CHEMBL339816 IC50 = 4.571 nM 8.34
CHEMBL340938 IC50 = 5.754 nM 8.24
CHEMBL128407 IC50 = 7.413 nM 8.13
CHEMBL106237 IC50 = 7.762 nM 8.11
CHEMBL128147 IC50 = 7.943 nM 8.10
CHEMBL339530 IC50 = 8.71 nM 8.06
CHEMBL340752 IC50 = 10.47 nM 7.98
CHEMBL129028 IC50 = 13.18 nM 7.88
CHEMBL127057 IC50 = 15.85 nM 7.80
CHEMBL129162 IC50 = 20.89 nM 7.68
CHEMBL129511 IC50 = 22.91 nM 7.64
CHEMBL337917 IC50 = 26.92 nM 7.57
CHEMBL340201 IC50 = 33.11 nM 7.48
CHEMBL341361 IC50 = 33.11 nM 7.48
CHEMBL338378 IC50 = 41.69 nM 7.38
CHEMBL338634 IC50 = 48.98 nM 7.31
CHEMBL320366 IC50 = 95.5 nM 7.02
CHEMBL338442 IC50 = 120.23 nM 6.92
CHEMBL126286 IC50 = 177.83 nM 6.75
CHEMBL127060 IC50 = 302.0 nM 6.52
CHEMBL126730 IC50 = 389.05 nM 6.41
CHEMBL128093 IC50 = 446.68 nM 6.35
CHEMBL128491 IC50 = 524.81 nM 6.28
CHEMBL129101 IC50 = 1621.81 nM 5.79
CHEMBL338633 IC50 = 1995.26 nM 5.70