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Assay Detail

CHEMBL896184

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

Binding
Displacement of [3H]DTG from sigma2 receptor in Wistar rat liver membrane in presence of 1 uM [3H]pentazocine
14
Total Activities
14
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

Design and evaluation of naphthol- and carbazole-containing fluorescent sigma ligands as potential probes for receptor binding studies.
Ferorelli S, Abate C, Colabufo NA, Niso M, Inglese C, Berardi F, Perrone R.
J Med Chem (2007) 50 : 4648 -4655
PubMed 17713896 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.04 8.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL538089 1 8.08
CHEMBL535857 1 8.04
CHEMBL535856 1 8.03
CHEMBL535634 1 7.93
CHEMBL536305 1 7.90
CHEMBL541390 1 7.58
CHEMBL282433 DITOLYLGUANIDINE 1 7.51
CHEMBL538091 1 6.93
CHEMBL558572 1 6.38
CHEMBL555969 1 6.28
CHEMBL537696 1 6.22
CHEMBL535410 1 6.19
CHEMBL535636 1 6.17
CHEMBL536759 1 5.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL538089 Ki = 8.27 nM 8.08
CHEMBL535857 Ki = 9.02 nM 8.04
CHEMBL535856 Ki = 9.24 nM 8.03
CHEMBL535634 Ki = 11.8 nM 7.93
CHEMBL536305 Ki = 12.6 nM 7.90
CHEMBL541390 Ki = 26.4 nM 7.58
CHEMBL282433 DITOLYLGUANIDINE Ki = 30.8 nM 7.51
CHEMBL538091 Ki = 117.0 nM 6.93
CHEMBL558572 Ki = 412.0 nM 6.38
CHEMBL555969 Ki = 520.0 nM 6.28
CHEMBL537696 Ki = 600.0 nM 6.22
CHEMBL535410 Ki = 643.0 nM 6.19
CHEMBL535636 Ki = 672.0 nM 6.17
CHEMBL536759 Ki = 4480.0 nM 5.35