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Assay Detail

CHEMBL3239229

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

Binding
Displacement of [3H]-DTG from sigma-2 receptor in human RT4 cell membranes after 120 mins by scintillation counting analysis in presence of (+)-pentazocine
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type RT-4
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis, pharmacological evaluation, and σ1 receptor interaction analysis of hydroxyethyl substituted piperazines.
Weber F, Brune S, Korpis K, Bednarski PJ, Laurini E, Dal Col V, Pricl S, Schepmann D, Wünsch B.
J Med Chem (2014) 57 : 2884 -2894
PubMed 24617836 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 7.26 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3233530 1 7.80
CHEMBL282433 DITOLYLGUANIDINE 1 7.70
CHEMBL3233532 1 7.51
CHEMBL3233531 1 7.43
CHEMBL3104857 1 7.41
CHEMBL3104856 1 7.37
CHEMBL3233528 1 6.78
CHEMBL54 HALOPERIDOL 4.0 1 6.70
CHEMBL3233529 1 6.60
CHEMBL3233525 1 -
CHEMBL3233537 1 -
CHEMBL3233536 1 -
CHEMBL3233535 1 -
CHEMBL3233534 1 -
CHEMBL3233533 1 -
CHEMBL3233526 1 -
CHEMBL3233524 1 -
CHEMBL3233527 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3233530 Ki = 16.0 nM 7.80
CHEMBL282433 DITOLYLGUANIDINE Ki = 20.0 nM 7.70
CHEMBL3233532 Ki = 31.0 nM 7.51
CHEMBL3233531 Ki = 37.0 nM 7.43
CHEMBL3104857 Ki = 39.0 nM 7.41
CHEMBL3104856 Ki = 43.0 nM 7.37
CHEMBL3233528 Ki = 168.0 nM 6.78
CHEMBL54 HALOPERIDOL Ki = 200.0 nM 6.70
CHEMBL3233529 Ki = 251.0 nM 6.60
CHEMBL3233525 Ki - -
CHEMBL3233537 Ki - -
CHEMBL3233536 Ki - -
CHEMBL3233535 Ki - -
CHEMBL3233534 Ki - -
CHEMBL3233533 Ki - -
CHEMBL3233526 Ki - -
CHEMBL3233524 Ki - -
CHEMBL3233527 Ki - -