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Assay Detail

CHEMBL4480643

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 cortex membranes measured after 120 mins by scintillation counting analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
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 and receptor binding of thiophene bioisosteres of potent GluN2B ligands with a benzo[7]annulene-scaffold.
Baumeister S, Schepmann D, Wünsch B.
Medchemcomm (2019) 10 : 315 -325
PubMed 30881618 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.69 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4574247 1 7.10
CHEMBL305187 IFENPRODIL 2.0 1 6.90
CHEMBL4287203 1 6.88
CHEMBL4590193 1 6.78
CHEMBL4570472 1 6.33
CHEMBL4513837 1 6.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4574247 Ki = 79.0 nM 7.10
CHEMBL305187 IFENPRODIL Ki = 125.0 nM 6.90
CHEMBL4287203 Ki = 132.0 nM 6.88
CHEMBL4590193 Ki = 167.0 nM 6.78
CHEMBL4570472 Ki = 470.0 nM 6.33
CHEMBL4513837 Ki = 737.0 nM 6.13