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

CHEMBL3225558

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

Binding
Displacement of [3H]-pentazocine from human recombinant sigma-1 receptor expressed in CHO cells after 180 mins by beta counting analysis
20
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of novel selective Sigma-1 ligands as cognitive enhancers
Valade A, Cross SB, Brown C, Detrait E, Ene D, Gillard M, Guyaux M, Lamberty Y, Maguire M, Namdev N, Provins L, Schwartz E, Vermeiren C
Medchemcomm (2011) 2 : 655 -660
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.01 8.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL408867 [11C]SA4503 1 8.50
CHEMBL3218986 1 8.00
CHEMBL3218985 1 7.80
CHEMBL3218989 1 7.60
CHEMBL3218987 1 7.60
CHEMBL3218982 1 7.20
CHEMBL3218981 1 7.20
CHEMBL3218992 1 7.10
CHEMBL3218994 1 7.10
CHEMBL3218993 1 7.00
CHEMBL3218980 1 6.90
CHEMBL98883 1 6.80
CHEMBL3218979 3 6.80
CHEMBL3218991 1 6.70
CHEMBL3218984 1 6.40
CHEMBL3218988 1 6.20
CHEMBL3218983 1 5.90
CHEMBL3218990 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL408867 [11C]SA4503 Ki = 3.162 nM 8.50
CHEMBL3218986 Ki = 10.0 nM 8.00
CHEMBL3218985 Ki = 15.85 nM 7.80
CHEMBL3218989 Ki = 25.12 nM 7.60
CHEMBL3218987 Ki = 25.12 nM 7.60
CHEMBL3218982 Ki = 63.1 nM 7.20
CHEMBL3218981 Ki = 63.1 nM 7.20
CHEMBL3218994 Ki = 79.43 nM 7.10
CHEMBL3218992 Ki = 79.43 nM 7.10
CHEMBL3218993 Ki = 100.0 nM 7.00
CHEMBL3218980 Ki = 125.89 nM 6.90
CHEMBL98883 Ki = 158.49 nM 6.80
CHEMBL3218979 Ki = 158.49 nM 6.80
CHEMBL3218979 Ki = 158.49 nM 6.80
CHEMBL3218979 Ki = 199.53 nM 6.70
CHEMBL3218991 Ki = 199.53 nM 6.70
CHEMBL3218984 Ki = 398.11 nM 6.40
CHEMBL3218988 Ki = 630.96 nM 6.20
CHEMBL3218983 Ki = 1258.93 nM 5.90
CHEMBL3218990 Ki = 1258.93 nM 5.90