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Assay Detail

CHEMBL4369175

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

Binding
Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig by radioligand binding assay
3
Total Activities
3
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

Structure activity relationship of 2-arylalkynyl-adenine derivatives as human A<sub>3</sub> adenosine receptor antagonists.
Yu J, Mannes P, Jung YH, Ciancetta A, Bitant A, Lieberman DI, Khaznadar S, Auchampach JA, Gao ZG, Jacobson KA.
Medchemcomm (2018) 9 : 1920 -1932
PubMed 30568760 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 5.87 5.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4593728 1 5.94
CHEMBL4526748 1 5.86
CHEMBL4534460 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4593728 Ki = 1160.0 nM 5.94
CHEMBL4526748 Ki = 1390.0 nM 5.86
CHEMBL4534460 Ki = 1520.0 nM 5.82