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Assay Detail

CHEMBL3801685

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 homogenate incubated for 120 mins by solid scintillation counting analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Benzimidazolone bioisosteres of potent GluN2B selective NMDA receptor antagonists.
Lütnant I, Schepmann D, Wünsch B.
Eur J Med Chem (2016) 116 : 136 -146
PubMed 27061977 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.89 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.20
CHEMBL282433 DITOLYLGUANIDINE 1 7.05
CHEMBL319706 (S)-IFENPRODIL 1 6.90
CHEMBL3797704 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 6.3 nM 8.20
CHEMBL282433 DITOLYLGUANIDINE Ki = 89.0 nM 7.05
CHEMBL319706 (S)-IFENPRODIL Ki = 125.0 nM 6.90
CHEMBL3797704 Ki = 4000.0 nM 5.40