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Assay Detail

CHEMBL983517

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

Binding
Displacement of [3H]PK11195 from peripheral benzodiazepine receptor in Sprague-Dawley rat cerebral cortex membrane by liquid scintillation counting
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Translocator protein (CHEMBL4552)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

2-Phenyl-imidazo[1,2-a]pyridine compounds containing hydrophilic groups as potent and selective ligands for peripheral benzodiazepine receptors: synthesis, binding affinity and electrophysiological studies.
Denora N, Laquintana V, Pisu MG, Dore R, Murru L, Latrofa A, Trapani G, Sanna E.
J Med Chem (2008) 51 : 6876 -6888
PubMed 18834105 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 8.77 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL520465 1 9.82
CHEMBL485606 1 9.64
CHEMBL485217 1 9.62
CHEMBL521180 1 9.52
CHEMBL509917 1 9.51
CHEMBL484741 1 9.49
CHEMBL485219 1 9.48
CHEMBL519654 1 9.35
CHEMBL521186 1 9.14
CHEMBL483383 1 9.11
CHEMBL483596 1 9.07
CHEMBL484574 1 9.06
CHEMBL520847 1 8.98
CHEMBL485218 1 8.94
CHEMBL481537 PK-11195 1 8.94
CHEMBL484573 1 8.88
CHEMBL521304 1 8.84
CHEMBL484932 1 8.82
CHEMBL483172 1 8.77
CHEMBL220661 1 8.68
CHEMBL484188 1 8.65
CHEMBL520652 1 8.56
CHEMBL485435 1 7.85
CHEMBL485589 1 7.84
CHEMBL484758 1 6.93
CHEMBL520662 1 6.71
CHEMBL484750 1 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL520465 Ki = 0.15 nM 9.82
CHEMBL485606 Ki = 0.23 nM 9.64
CHEMBL485217 Ki = 0.24 nM 9.62
CHEMBL521180 Ki = 0.3 nM 9.52
CHEMBL509917 Ki = 0.31 nM 9.51
CHEMBL484741 Ki = 0.32 nM 9.49
CHEMBL485219 Ki = 0.33 nM 9.48
CHEMBL519654 Ki = 0.45 nM 9.35
CHEMBL521186 Ki = 0.73 nM 9.14
CHEMBL483383 Ki = 0.78 nM 9.11
CHEMBL483596 Ki = 0.86 nM 9.07
CHEMBL484574 Ki = 0.87 nM 9.06
CHEMBL520847 Ki = 1.04 nM 8.98
CHEMBL485218 Ki = 1.16 nM 8.94
CHEMBL481537 PK-11195 Ki = 1.14 nM 8.94
CHEMBL484573 Ki = 1.31 nM 8.88
CHEMBL521304 Ki = 1.44 nM 8.84
CHEMBL484932 Ki = 1.52 nM 8.82
CHEMBL483172 Ki = 1.69 nM 8.77
CHEMBL220661 Ki = 2.07 nM 8.68
CHEMBL484188 Ki = 2.22 nM 8.65
CHEMBL520652 Ki = 2.76 nM 8.56
CHEMBL485435 Ki = 14.2 nM 7.85
CHEMBL485589 Ki = 14.4 nM 7.84
CHEMBL484758 Ki = 117.7 nM 6.93
CHEMBL520662 Ki = 193.1 nM 6.71
CHEMBL484750 Ki = 285.3 nM 6.54