Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL808204

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

Binding
Binding affinity for Sigma receptor type 1,using [3H](+)-pentazocine as radioligand
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL287)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Thioxanthene-derived analogs as sigma(1) receptor ligands.
Glennon RA, Ismaiel AM, Ablordeppey S, El-Ashmawy M, Fisher JB.
Bioorg Med Chem Lett (2004) 14 : 2217 -2220
PubMed 15081012 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 8.89 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL304079 1 10.15
CHEMBL302087 1 10.05
CHEMBL67808 1 9.89
CHEMBL19355 1 9.77
CHEMBL19544 1 9.60
CHEMBL69256 1 9.32
CHEMBL303263 1 9.18
CHEMBL305218 1 9.10
CHEMBL71155 1 9.05
CHEMBL71883 1 8.96
CHEMBL304283 1 8.89
CHEMBL305461 1 8.85
CHEMBL72045 1 8.72
CHEMBL71773 1 7.92
CHEMBL282567 PROADIFEN 2.0 1 7.77
CHEMBL71616 1 7.70
CHEMBL68905 1 7.54
CHEMBL72061 1 7.54
CHEMBL70352 BENACTYZINE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL304079 Ki = 0.07 nM 10.15
CHEMBL302087 Ki = 0.09 nM 10.05
CHEMBL67808 Ki = 0.13 nM 9.89
CHEMBL19355 Ki = 0.17 nM 9.77
CHEMBL19544 Ki = 0.25 nM 9.60
CHEMBL69256 Ki = 0.48 nM 9.32
CHEMBL303263 Ki = 0.66 nM 9.18
CHEMBL305218 Ki = 0.8 nM 9.10
CHEMBL71155 Ki = 0.89 nM 9.05
CHEMBL71883 Ki = 1.1 nM 8.96
CHEMBL304283 Ki = 1.3 nM 8.89
CHEMBL305461 Ki = 1.4 nM 8.85
CHEMBL72045 Ki = 1.9 nM 8.72
CHEMBL71773 Ki = 12.0 nM 7.92
CHEMBL282567 PROADIFEN Ki = 17.0 nM 7.77
CHEMBL71616 Ki = 20.0 nM 7.70
CHEMBL68905 Ki = 29.0 nM 7.54
CHEMBL72061 Ki = 29.0 nM 7.54
CHEMBL70352 BENACTYZINE Ki > 1000.0 nM -