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Assay Detail

CHEMBL809857

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

Binding
Inhibition of [3H]-DTG binding to Sigma opioid receptor type 2
ChEMBL ↗
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 3 — Cell-line / Tissue
Curated By Expert

Target

Sigma 2 receptor (CHEMBL613288) ↗
Type UNKNOWN

Publication

An aromatic moiety is not essential for pharmacophore binding to sigma binding sites: Synthesis of N-alkylazacycloheptane derivatives as potent sigma ligands
Yamashita A, Takahashi N, Mochizuki D, Tsujita R, Yamada S, Kawakubo H, Suzuki Y, Watanabe H
Bioorg Med Chem Lett (1997) 7 : 2303 -2306
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.55 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL77812 — — 1 9.64
CHEMBL77817 — — 1 9.60
CHEMBL75555 — — 1 9.55
CHEMBL307839 — — 1 9.48
CHEMBL306318 — — 1 9.25
CHEMBL73633 — — 1 9.15
CHEMBL73818 — — 1 9.11
CHEMBL74499 — — 1 8.96
CHEMBL424606 — — 1 8.50
CHEMBL308816 — — 1 8.45
CHEMBL74803 — — 1 8.17
CHEMBL282433 DITOLYLGUANIDINE — 1 7.78
CHEMBL54 HALOPERIDOL 4.0 1 7.16
CHEMBL101510 — — 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL77812 — Ki = 0.23 nM 9.64
CHEMBL77817 — Ki = 0.25 nM 9.60
CHEMBL75555 — Ki = 0.28 nM 9.55
CHEMBL307839 — Ki = 0.33 nM 9.48
CHEMBL306318 — Ki = 0.56 nM 9.25
CHEMBL73633 — Ki = 0.7 nM 9.15
CHEMBL73818 — Ki = 0.77 nM 9.11
CHEMBL74499 — Ki = 1.1 nM 8.96
CHEMBL424606 — Ki = 3.14 nM 8.50
CHEMBL308816 — Ki = 3.54 nM 8.45
CHEMBL74803 — Ki = 6.79 nM 8.17
CHEMBL282433 DITOLYLGUANIDINE Ki = 16.8 nM 7.78
CHEMBL54 HALOPERIDOL Ki = 69.6 nM 7.16
CHEMBL101510 — Ki = 14200.0 nM 4.85