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Assay Detail

CHEMBL1685123

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 membrane
11
Total Activities
11
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

Effect of structural modification in the amine portion of substituted aminobutyl-benzamides as ligands for binding σ1 and σ2 receptors.
Fan KH, Lever JR, Lever SZ.
Bioorg Med Chem (2011) 19 : 1852 -1859
PubMed 21376604 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 6.26 9.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 9.08
CHEMBL408867 [11C]SA4503 1 8.36
CHEMBL1682086 1 6.23
CHEMBL391153 1 6.06
CHEMBL291439 1 6.05
CHEMBL1682080 1 5.84
CHEMBL1682083 1 5.68
CHEMBL1682084 1 5.59
CHEMBL1682085 1 5.35
CHEMBL1682082 1 5.34
CHEMBL1682081 1 5.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 0.83 nM 9.08
CHEMBL408867 [11C]SA4503 Ki = 4.34 nM 8.36
CHEMBL1682086 Ki = 583.0 nM 6.23
CHEMBL391153 Ki = 880.0 nM 6.06
CHEMBL291439 Ki = 881.0 nM 6.05
CHEMBL1682080 Ki = 1442.0 nM 5.84
CHEMBL1682083 Ki = 2068.0 nM 5.68
CHEMBL1682084 Ki = 2564.0 nM 5.59
CHEMBL1682085 Ki = 4499.0 nM 5.35
CHEMBL1682082 Ki = 4521.0 nM 5.34
CHEMBL1682081 Ki = 5073.0 nM 5.29