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Assay Detail

CHEMBL4369173

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

Binding
Displacement of [3H]-DTG from sigma 2 receptor in rat PC12 cells by radioligand binding assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sigma intracellular receptor 2 (CHEMBL4105864)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 6.07 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4526748 1 6.43
CHEMBL4530091 1 6.05
CHEMBL4534460 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4526748 Ki = 370.0 nM 6.43
CHEMBL4530091 Ki = 900.0 nM 6.05
CHEMBL4534460 Ki = 1910.0 nM 5.72