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Assay Detail

CHEMBL673588

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

Binding
In vitro binding affinity at Dopamine receptor D2 in rat striatum by [3H]spiroperidol displacement.
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

4-(tetralin-1-yl)- and 4-(naphthalen-1-yl)alkyl derivatives of 1-cyclohexylpiperazine as sigma receptor ligands with agonist sigma2 activity.
Berardi F, Ferorelli S, Abate C, Colabufo NA, Contino M, Perrone R, Tortorella V.
J Med Chem (2004) 47 : 2308 -2317
PubMed 15084129 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.77 6.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL75444 1 6.32
CHEMBL53325 1 6.22
CHEMBL309064 1 5.94
CHEMBL74858 1 5.79
CHEMBL306365 1 5.61
CHEMBL74811 1 5.46
CHEMBL77220 1 5.43
CHEMBL75878 1 5.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL75444 Ki = 479.0 nM 6.32
CHEMBL53325 Ki = 604.0 nM 6.22
CHEMBL309064 Ki = 1160.0 nM 5.94
CHEMBL74858 Ki = 1620.0 nM 5.79
CHEMBL306365 Ki = 2450.0 nM 5.61
CHEMBL74811 Ki = 3480.0 nM 5.46
CHEMBL77220 Ki = 3670.0 nM 5.43
CHEMBL75878 Ki = 4260.0 nM 5.37