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Assay Detail

CHEMBL3858016

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

Binding
Displacement of [3H]-DTG from sigma2 receptor in rat liver membranes after 120 mins by scintillation counting method
26
Total Activities
26
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

Computer-assisted design, synthesis, binding and cytotoxicity assessments of new 1-(4-(aryl(methyl)amino)butyl)-heterocyclic sigma 1 ligands.
Zampieri D, Vio L, Fermeglia M, Pricl S, Wünsch B, Schepmann D, Romano M, Mamolo MG, Laurini E.
Eur J Med Chem (2016) 121 : 712 -726
PubMed 27366902 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 6.71 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3983403 1 7.38
CHEMBL282433 DITOLYLGUANIDINE 1 7.27
CHEMBL54 HALOPERIDOL 4.0 1 7.11
CHEMBL3964384 1 7.05
CHEMBL3966143 1 7.03
CHEMBL3955644 1 6.98
CHEMBL3975617 1 6.96
CHEMBL3984272 1 6.92
CHEMBL3895475 1 6.77
CHEMBL3894565 1 6.76
CHEMBL3983612 1 6.72
CHEMBL3975268 1 6.65
CHEMBL3913418 1 6.62
CHEMBL3913581 1 6.62
CHEMBL3964306 1 6.60
CHEMBL3931495 1 6.60
CHEMBL3966773 1 6.59
CHEMBL3983252 1 6.56
CHEMBL3904413 1 6.50
CHEMBL3946295 1 6.50
CHEMBL3958562 1 6.38
CHEMBL3954990 1 6.22
CHEMBL3547159 1 6.21
CHEMBL3912537 1 5.92
CHEMBL3922582 1 -
CHEMBL3894798 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3983403 Ki = 42.0 nM 7.38
CHEMBL282433 DITOLYLGUANIDINE Ki = 54.0 nM 7.27
CHEMBL54 HALOPERIDOL Ki = 78.0 nM 7.11
CHEMBL3964384 Ki = 89.0 nM 7.05
CHEMBL3966143 Ki = 93.0 nM 7.03
CHEMBL3955644 Ki = 105.0 nM 6.98
CHEMBL3975617 Ki = 110.0 nM 6.96
CHEMBL3984272 Ki = 119.0 nM 6.92
CHEMBL3895475 Ki = 169.0 nM 6.77
CHEMBL3894565 Ki = 173.0 nM 6.76
CHEMBL3983612 Ki = 190.0 nM 6.72
CHEMBL3975268 Ki = 222.0 nM 6.65
CHEMBL3913418 Ki = 239.0 nM 6.62
CHEMBL3913581 Ki = 237.0 nM 6.62
CHEMBL3964306 Ki = 252.0 nM 6.60
CHEMBL3931495 Ki = 252.0 nM 6.60
CHEMBL3966773 Ki = 254.0 nM 6.59
CHEMBL3983252 Ki = 274.0 nM 6.56
CHEMBL3904413 Ki = 315.0 nM 6.50
CHEMBL3946295 Ki = 317.0 nM 6.50
CHEMBL3958562 Ki = 412.0 nM 6.38
CHEMBL3954990 Ki = 603.0 nM 6.22
CHEMBL3547159 Ki = 621.0 nM 6.21
CHEMBL3912537 Ki = 1200.0 nM 5.92
CHEMBL3922582 Ki > 3000.0 nM -
CHEMBL3894798 Ki > 3000.0 nM -