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Assay Detail

CHEMBL650799

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

Binding
Inhibition of [3H]PK11195 binding to Peripheral type benzodiazepine receptor (PBR) in rat cortex homogenate by 50%
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Translocator protein (CHEMBL4552)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis of new molecular probes for investigation of steroid biosynthesis induced by selective interaction with peripheral type benzodiazepine receptors (PBR).
Campiani G, Ramunno A, Fiorini I, Nacci V, Morelli E, Novellino E, Goegan M, Mennini T, Sullivan S, Zisterer DM, Williams CD.
J Med Chem (2002) 45 : 4276 -4281
PubMed 12213069 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 8.87 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135514 1 9.96
CHEMBL135391 1 9.74
CHEMBL136036 1 9.64
CHEMBL136926 1 9.36
CHEMBL335300 1 9.25
CHEMBL133144 1 9.17
CHEMBL335085 1 9.16
CHEMBL341455 1 9.11
CHEMBL135801 1 9.04
CHEMBL134282 1 9.04
CHEMBL134781 1 8.92
CHEMBL135428 1 8.90
CHEMBL135327 1 8.75
CHEMBL445583 1 8.66
CHEMBL336774 1 8.65
CHEMBL135484 1 8.60
CHEMBL336903 1 8.24
CHEMBL132915 1 8.22
CHEMBL135807 1 8.14
CHEMBL135663 1 7.94
CHEMBL137600 1 7.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135514 Ki = 0.11 nM 9.96
CHEMBL135391 Ki = 0.18 nM 9.74
CHEMBL136036 Ki = 0.23 nM 9.64
CHEMBL136926 Ki = 0.44 nM 9.36
CHEMBL335300 Ki = 0.56 nM 9.25
CHEMBL133144 Ki = 0.68 nM 9.17
CHEMBL335085 Ki = 0.69 nM 9.16
CHEMBL341455 Ki = 0.78 nM 9.11
CHEMBL135801 Ki = 0.91 nM 9.04
CHEMBL134282 Ki = 0.92 nM 9.04
CHEMBL134781 Ki = 1.2 nM 8.92
CHEMBL135428 Ki = 1.26 nM 8.90
CHEMBL135327 Ki = 1.77 nM 8.75
CHEMBL445583 Ki = 2.21 nM 8.66
CHEMBL336774 Ki = 2.26 nM 8.65
CHEMBL135484 Ki = 2.5 nM 8.60
CHEMBL336903 Ki = 5.7 nM 8.24
CHEMBL132915 Ki = 6.03 nM 8.22
CHEMBL135807 Ki = 7.2 nM 8.14
CHEMBL135663 Ki = 11.5 nM 7.94
CHEMBL137600 Ki = 13.5 nM 7.87