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Assay Detail

CHEMBL1111777

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

Binding
Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane homogenates after 90 mins by liquid scintillation counting
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL4153)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Synthesis and in vitro biological evaluation of carbonyl group-containing inhibitors of vesicular acetylcholine transporter.
Efange SM, Khare AB, von Hohenberg K, Mach RH, Parsons SM, Tu Z.
J Med Chem (2010) 53 : 2825 -2835
PubMed 20218624 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 6.73 8.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1204035 1 8.03
CHEMBL1204032 1 7.80
CHEMBL1204048 1 7.70
CHEMBL20730 VESAMICOL 1 7.59
CHEMBL1204034 1 7.53
CHEMBL1204047 1 7.30
CHEMBL1204049 1 6.93
CHEMBL1204037 1 6.89
CHEMBL1204038 1 6.71
CHEMBL1204030 1 6.55
CHEMBL1204031 1 6.52
CHEMBL1204040 1 6.40
CHEMBL1204045 1 6.32
CHEMBL1204043 1 6.30
CHEMBL1204050 1 6.00
CHEMBL1204046 1 6.00
CHEMBL1204044 1 6.00
CHEMBL1204042 1 6.00
CHEMBL1204041 1 6.00
CHEMBL1204039 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1204035 Ki = 9.39 nM 8.03
CHEMBL1204032 Ki = 15.91 nM 7.80
CHEMBL1204048 Ki = 19.88 nM 7.70
CHEMBL20730 VESAMICOL Ki = 25.8 nM 7.59
CHEMBL1204034 Ki = 29.46 nM 7.53
CHEMBL1204047 Ki = 50.24 nM 7.30
CHEMBL1204049 Ki = 118.12 nM 6.93
CHEMBL1204037 Ki = 128.92 nM 6.89
CHEMBL1204038 Ki = 194.03 nM 6.71
CHEMBL1204030 Ki = 280.8 nM 6.55
CHEMBL1204031 Ki = 302.79 nM 6.52
CHEMBL1204040 Ki = 395.11 nM 6.40
CHEMBL1204045 Ki = 483.24 nM 6.32
CHEMBL1204043 Ki = 497.1 nM 6.30
CHEMBL1204050 Ki = 1000.0 nM 6.00
CHEMBL1204046 Ki = 1000.0 nM 6.00
CHEMBL1204044 Ki = 1000.0 nM 6.00
CHEMBL1204042 Ki = 1000.0 nM 6.00
CHEMBL1204041 Ki = 1000.0 nM 6.00
CHEMBL1204039 Ki = 1000.0 nM 6.00