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Assay Detail

CHEMBL1646509

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

Binding
Displacement of [3H]ditolylguanidine from sigma2 receptor in rat liver membrane by scintillation counting
8
Total Activities
8
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

Synthesis, pharmacological activity and structure affinity relationships of spirocyclic σ(1) receptor ligands with a (2-fluoroethyl) residue in 3-position.
Maestrup EG, Wiese C, Schepmann D, Brust P, Wünsch B.
Bioorg Med Chem (2011) 19 : 393 -405
PubMed 21126878 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.66 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1645207 1 7.24
CHEMBL54 HALOPERIDOL 4.0 1 7.11
CHEMBL1645215 1 7.09
CHEMBL1645214 1 6.93
CHEMBL1645209 1 6.38
CHEMBL1645205 1 6.32
CHEMBL1645202 1 6.11
CHEMBL1645212 1 6.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1645207 Ki = 57.0 nM 7.24
CHEMBL54 HALOPERIDOL Ki = 78.0 nM 7.11
CHEMBL1645215 Ki = 82.0 nM 7.09
CHEMBL1645214 Ki = 118.0 nM 6.93
CHEMBL1645209 Ki = 421.0 nM 6.38
CHEMBL1645205 Ki = 481.0 nM 6.32
CHEMBL1645202 Ki = 785.0 nM 6.11
CHEMBL1645212 Ki = 878.0 nM 6.06