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Assay Detail

CHEMBL911273

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 in rat kidney mitochondrial membranes
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Translocator protein (CHEMBL4552)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation.
Taliani S, Simorini F, Sergianni V, La Motta C, Da Settimo F, Cosimelli B, Abignente E, Greco G, Novellino E, Rossi L, Gremigni V, Spinetti F, Chelli B, Martini C.
J Med Chem (2007) 50 : 404 -407
PubMed 17228885 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.72 9.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53430 1 9.43
CHEMBL54349 ALPIDEM 4.0 1 9.30
CHEMBL481537 PK-11195 1 8.03
CHEMBL374574 1 7.92
CHEMBL384328 1 7.77
CHEMBL286346 RO-54864 1 7.64
CHEMBL386903 1 7.64
CHEMBL425811 1 7.38
CHEMBL265039 1 6.08
CHEMBL220306 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53430 Ki = 0.37 nM 9.43
CHEMBL54349 ALPIDEM Ki = 0.5 nM 9.30
CHEMBL481537 PK-11195 Ki = 9.3 nM 8.03
CHEMBL374574 Ki = 12.0 nM 7.92
CHEMBL384328 Ki = 17.0 nM 7.77
CHEMBL286346 RO-54864 Ki = 23.0 nM 7.64
CHEMBL386903 Ki = 23.0 nM 7.64
CHEMBL425811 Ki = 42.0 nM 7.38
CHEMBL265039 Ki = 835.0 nM 6.08
CHEMBL220306 Ki = 994.0 nM 6.00