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Assay Detail

CHEMBL802065

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

Binding
Compound was tested for its binding affinity towards sigma 1 receptor using [3H](+)-pentazocine from guinea pig brain
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL287)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand.
Quaglia W, Giannella M, Piergentili A, Pigini M, Brasili L, Di Toro R, Rossetti L, Spampinato S, Melchiorre C.
J Med Chem (1998) 41 : 1557 -1560
PubMed 9572880 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 8.03 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39900 SPIPETHIANE 1 9.30
CHEMBL38634 1 9.21
CHEMBL41830 1 8.85
CHEMBL54 HALOPERIDOL 4.0 1 8.49
CHEMBL38904 1 7.70
CHEMBL38085 1 7.60
CHEMBL42 CLOZAPINE 4.0 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39900 SPIPETHIANE Ki = 0.5 nM 9.30
CHEMBL38634 Ki = 0.62 nM 9.21
CHEMBL41830 Ki = 1.4 nM 8.85
CHEMBL54 HALOPERIDOL Ki = 3.2 nM 8.49
CHEMBL38904 Ki = 20.0 nM 7.70
CHEMBL38085 Ki = 25.0 nM 7.60
CHEMBL42 CLOZAPINE Ki = 8500.0 nM 5.07