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Assay Detail

CHEMBL805746

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

Binding
Binding affinity towards sigma 2 receptor site in rat liver membranes using [3H]DTG as radioligand in presence of (+)-pentazocine.
ChEMBL ↗
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Subcellular Membrane
Confidence 3 — Cell-line / Tissue
Curated By Expert

Target

Sigma 2 receptor (CHEMBL613288) ↗
Type UNKNOWN

Publication

Synthesis and quantitative structure-activity relationships of N-(1-benzylpiperidin-4-yl)phenylacetamides and related analogues as potent and selective sigma1 receptor ligands.
Huang Y, Hammond PS, Whirrett BR, Kuhner RJ, Wu L, Childers SR, Mach RH.
J Med Chem (1998) 41 : 2361 -2370
PubMed 9632369 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 45 6.98 7.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL77286 — — 1 7.84
CHEMBL77405 — — 1 7.82
CHEMBL77285 — — 1 7.62
CHEMBL262760 — — 1 7.61
CHEMBL54 HALOPERIDOL 4.0 1 7.54
CHEMBL1036 HYDROXYHALOPERIDOL — 1 7.54
CHEMBL76864 — — 1 7.43
CHEMBL312254 — — 1 7.43
CHEMBL77953 — — 1 7.42
CHEMBL77773 — — 1 7.27
CHEMBL308818 — — 1 7.27
CHEMBL306955 — — 1 7.21
CHEMBL310499 — — 1 7.16
CHEMBL77352 — — 1 7.15
CHEMBL311622 — — 1 7.10
CHEMBL413057 — — 1 7.09
CHEMBL76802 — — 1 7.09
CHEMBL75816 — — 1 7.08
CHEMBL431775 — — 1 7.06
CHEMBL307253 — — 1 6.98
CHEMBL76547 — — 1 6.89
CHEMBL77289 — — 1 6.89
CHEMBL306768 — — 1 6.82
CHEMBL76564 — — 1 6.76
CHEMBL78059 — — 1 6.68
CHEMBL77120 — — 1 6.64
CHEMBL76895 — — 1 6.62
CHEMBL74665 — — 1 6.61
CHEMBL80397 — — 1 6.54
CHEMBL312692 — — 1 6.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL77286 — Ki = 14.6 nM 7.84
CHEMBL77405 — Ki = 15.2 nM 7.82
CHEMBL77285 — Ki = 23.9 nM 7.62
CHEMBL262760 — Ki = 24.5 nM 7.61
CHEMBL54 HALOPERIDOL Ki = 28.5 nM 7.54
CHEMBL1036 HYDROXYHALOPERIDOL Ki = 28.6 nM 7.54
CHEMBL76864 — Ki = 36.9 nM 7.43
CHEMBL312254 — Ki = 37.3 nM 7.43
CHEMBL77953 — Ki = 37.8 nM 7.42
CHEMBL77773 — Ki = 53.4 nM 7.27
CHEMBL308818 — Ki = 53.5 nM 7.27
CHEMBL306955 — Ki = 61.9 nM 7.21
CHEMBL310499 — Ki = 69.2 nM 7.16
CHEMBL77352 — Ki = 70.8 nM 7.15
CHEMBL311622 — Ki = 79.2 nM 7.10
CHEMBL413057 — Ki = 80.7 nM 7.09
CHEMBL76802 — Ki = 80.5 nM 7.09
CHEMBL75816 — Ki = 83.3 nM 7.08
CHEMBL431775 — Ki = 86.6 nM 7.06
CHEMBL307253 — Ki = 105.4 nM 6.98
CHEMBL76547 — Ki = 130.0 nM 6.89
CHEMBL77289 — Ki = 129.3 nM 6.89
CHEMBL306768 — Ki = 153.0 nM 6.82
CHEMBL76564 — Ki = 174.0 nM 6.76
CHEMBL78059 — Ki = 207.0 nM 6.68
CHEMBL77120 — Ki = 227.0 nM 6.64
CHEMBL76895 — Ki = 240.0 nM 6.62
CHEMBL74665 — Ki = 243.0 nM 6.61
CHEMBL80397 — Ki = 290.0 nM 6.54
CHEMBL312692 — Ki = 326.0 nM 6.49
CHEMBL311579 — Ki = 343.0 nM 6.46
CHEMBL308304 — Ki = 483.0 nM 6.32
CHEMBL305728 — Ki = 493.0 nM 6.31
CHEMBL311451 — Ki = 535.0 nM 6.27
CHEMBL76806 — Ki = 667.0 nM 6.18
CHEMBL75810 — Ki = 757.0 nM 6.12
CHEMBL312576 — Ki > 1000.0 nM -
CHEMBL76528 — Ki > 1000.0 nM -
CHEMBL80395 — Ki > 1000.0 nM -
CHEMBL309228 — Ki > 1000.0 nM -
CHEMBL75864 — Ki > 1000.0 nM -
CHEMBL419656 — Ki > 1000.0 nM -
CHEMBL312631 — Ki > 1000.0 nM -
CHEMBL308097 — Ki > 1000.0 nM -
CHEMBL80326 — Ki > 1000.0 nM -