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Assay Detail

CHEMBL3757724

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

Binding
Binding affinity to sigma-1 receptor (unknown origin) by radioligand displacement assay
7
Total Activities
7
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 non-opioid intracellular receptor 1 (CHEMBL287)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Role of the phenolic OH moiety of GluN2B-selective NMDA antagonists with 3-benzazepine scaffold.
Dey S, Schepmann D, Wünsch B.
Bioorg Med Chem Lett (2016) 26 : 889 -893
PubMed 26750254 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.89 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.20
CHEMBL3752701 1 7.51
CHEMBL282433 DITOLYLGUANIDINE 1 7.05
CHEMBL319706 (S)-IFENPRODIL 1 6.90
CHEMBL1289626 1 6.71
CHEMBL3753409 1 6.17
CHEMBL3752293 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 6.3 nM 8.20
CHEMBL3752701 Ki = 31.0 nM 7.51
CHEMBL282433 DITOLYLGUANIDINE Ki = 89.0 nM 7.05
CHEMBL319706 (S)-IFENPRODIL Ki = 125.0 nM 6.90
CHEMBL1289626 Ki = 194.0 nM 6.71
CHEMBL3753409 Ki = 676.0 nM 6.17
CHEMBL3752293 Ki = 2200.0 nM 5.66