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Assay Detail

CHEMBL1930674

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

Binding
Displacement of [3H]ditolylguanidine from sigma 2 receptor in rat liver membrane after 1.5 hrs by scintillation counting in presence of sigma 1 blocker (+)-pentazocine
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Subcellular Membrane
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Electron-donating para-methoxy converts a benzamide-isoquinoline derivative into a highly Sigma-2 receptor selective ligand.
Hajipour AR, Guo LW, Pal A, Mavlyutov T, Ruoho AE.
Bioorg Med Chem (2011) 19 : 7435 -7440
PubMed 22055714 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.10 7.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1927702 1 7.67
CHEMBL1927694 1 7.57
CHEMBL1927696 1 6.06
CHEMBL1927698 1 5.85
CHEMBL1927697 1 5.40
CHEMBL1927699 1 5.28
CHEMBL1927695 1 4.89
CHEMBL1927700 1 -
CHEMBL1927701 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1927702 Ki = 21.26 nM 7.67
CHEMBL1927694 Ki = 26.78 nM 7.57
CHEMBL1927696 Ki = 866.7 nM 6.06
CHEMBL1927698 Ki = 1400.0 nM 5.85
CHEMBL1927697 Ki = 4000.0 nM 5.40
CHEMBL1927699 Ki = 5290.0 nM 5.28
CHEMBL1927695 Ki = 12930.0 nM 4.89
CHEMBL1927700 Ki = 152000.0 nM -
CHEMBL1927701 Ki > 10000000.0 nM -