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Assay Detail

CHEMBL3097103

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

Binding
Displacement of [3H](+)-pentazocine from sigma1 receptor in rat brain after 120 mins by liquid scintillation counting analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL3602)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Chlorophenylpiperazine analogues as high affinity dopamine transporter ligands.
Motel WC, Healy JR, Viard E, Pouw B, Martin KE, Matsumoto RR, Coop A.
Bioorg Med Chem Lett (2013) 23 : 6920 -6922
PubMed 24211020 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 8.76 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL112125 1 9.92
CHEMBL3093268 1 9.82
CHEMBL3093270 1 9.25
CHEMBL3093269 1 8.73
CHEMBL325262 1 8.31
CHEMBL113621 1 8.19
CHEMBL145867 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL112125 Ki = 0.12 nM 9.92
CHEMBL3093268 Ki = 0.15 nM 9.82
CHEMBL3093270 Ki = 0.56 nM 9.25
CHEMBL3093269 Ki = 1.85 nM 8.73
CHEMBL325262 Ki = 4.93 nM 8.31
CHEMBL113621 Ki = 6.47 nM 8.19
CHEMBL145867 Ki = 82.0 nM 7.09