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Assay Detail

CHEMBL4148656

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Binding
Binding affinity to sigma-2 receptor (unknown origin)
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sigma intracellular receptor 2 (CHEMBL4105907)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and pharmacological evaluation of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives as sigma-2 receptor ligands.
Sun YT, Wang GF, Yang YQ, Jin F, Wang Y, Xie XY, Mach RH, Huang YS.
Eur J Med Chem (2018) 147 : 227 -237
PubMed 29438891 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 8.46 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL61479 SIRAMESINE 2.0 1 9.92
CHEMBL227126 1 9.59
CHEMBL53325 1 9.47
CHEMBL4169075 1 8.29
CHEMBL60048 1 7.99
CHEMBL1188414 1 7.90
CHEMBL4167498 1 7.50
CHEMBL1215855 1 7.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL61479 SIRAMESINE Ki = 0.12 nM 9.92
CHEMBL227126 Ki = 0.26 nM 9.59
CHEMBL53325 Ki = 0.34 nM 9.47
CHEMBL4169075 Ki = 5.19 nM 8.29
CHEMBL60048 Ki = 10.33 nM 7.99
CHEMBL1188414 Ki = 12.6 nM 7.90
CHEMBL4167498 Ki = 32.0 nM 7.50
CHEMBL1215855 Ki = 90.4 nM 7.04