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Assay Detail

CHEMBL3390300

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

Binding
Displacement of [3H](+)-pentazocine from sigma1 receptor in guinea pig brain membranes after 180 mins by scintillation counting method
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL4153)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Synthesis, GluN2B affinity and selectivity of benzo[7]annulen-7-amines.
Gawaskar S, Schepmann D, Bonifazi A, Wünsch B.
Bioorg Med Chem (2014) 22 : 6638 -6646
PubMed 25458498 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.31 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3357790 1 8.24
CHEMBL54 HALOPERIDOL 4.0 1 8.20
CHEMBL3357791 1 7.85
CHEMBL3357792 1 7.70
CHEMBL3357786 1 7.66
CHEMBL3357788 1 7.66
CHEMBL3357784 1 7.57
CHEMBL282433 DITOLYLGUANIDINE 1 7.05
CHEMBL3357785 1 6.97
CHEMBL305187 IFENPRODIL 2.0 1 6.90
CHEMBL3357783 1 6.88
CHEMBL296601 1 6.82
CHEMBL1289403 1 6.74
CHEMBL3357789 1 6.74
CHEMBL3357787 1 6.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3357790 Ki = 5.7 nM 8.24
CHEMBL54 HALOPERIDOL Ki = 6.3 nM 8.20
CHEMBL3357791 Ki = 14.0 nM 7.85
CHEMBL3357792 Ki = 20.0 nM 7.70
CHEMBL3357786 Ki = 22.0 nM 7.66
CHEMBL3357788 Ki = 22.0 nM 7.66
CHEMBL3357784 Ki = 27.0 nM 7.57
CHEMBL282433 DITOLYLGUANIDINE Ki = 89.0 nM 7.05
CHEMBL3357785 Ki = 107.0 nM 6.97
CHEMBL305187 IFENPRODIL Ki = 125.0 nM 6.90
CHEMBL3357783 Ki = 132.0 nM 6.88
CHEMBL296601 Ki = 150.0 nM 6.82
CHEMBL1289403 Ki = 182.0 nM 6.74
CHEMBL3357789 Ki = 182.0 nM 6.74
CHEMBL3357787 Ki = 216.0 nM 6.67