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Assay Detail

CHEMBL652443

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

Binding
Displacement [3H]-PK 11195 from rat adrenal peripheral-type benzodiazepine receptor (PBR)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Translocator protein (CHEMBL4552)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis, biological activity, and SARs of pyrrolobenzoxazepine derivatives, a new class of specific "peripheral-type" benzodiazepine receptor ligands.
Campiani G, Nacci V, Fiorini I, De Filippis MP, Garofalo A, Ciani SM, Greco G, Novellino E, Williams DC, Zisterer DM, Woods MJ, Mihai C, Manzoni C, Mennini T.
J Med Chem (1996) 39 : 3435 -3450
PubMed 8784441 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 8.70 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL325169 1 9.00
CHEMBL117444 1 8.96
CHEMBL325649 1 8.72
CHEMBL325025 1 8.72
CHEMBL117589 1 8.60
CHEMBL326772 1 8.55
CHEMBL115470 1 8.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL325169 Ki = 1.0 nM 9.00
CHEMBL117444 Ki = 1.1 nM 8.96
CHEMBL325649 Ki = 1.9 nM 8.72
CHEMBL325025 Ki = 1.9 nM 8.72
CHEMBL117589 Ki = 2.5 nM 8.60
CHEMBL326772 Ki = 2.8 nM 8.55
CHEMBL115470 Ki = 4.8 nM 8.32