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Assay Detail

CHEMBL808183

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

Binding
Inhibition of [3H]DTG binding to sigma receptor in rat hippocampus
9
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL3602)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands.
el Ahmad Y, Laurent E, Maillet P, Talab A, Teste JF, Dokhan R, Tran G, Ollivier R.
J Med Chem (1997) 40 : 952 -960
PubMed 9083484 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.66 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL366388 1 7.52
CHEMBL49 BUSPIRONE 4.0 1 7.32
CHEMBL354210 1 7.05
CHEMBL368061 3 6.89
CHEMBL177031 2 6.70
CHEMBL56 8-OH-DPAT 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL366388 Ki = 30.0 nM 7.52
CHEMBL49 BUSPIRONE Ki = 48.0 nM 7.32
CHEMBL354210 Ki = 90.0 nM 7.05
CHEMBL368061 Ki = 130.0 nM 6.89
CHEMBL368061 Ki = 190.0 nM 6.72
CHEMBL177031 Ki = 200.0 nM 6.70
CHEMBL368061 Ki = 280.0 nM 6.55
CHEMBL177031 Ki = 1250.0 nM 5.90
CHEMBL56 8-OH-DPAT Ki = 5240.0 nM 5.28