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Assay Detail

CHEMBL4048899

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

Binding
Displacement of [3H](+)-pentazocine from sigma1 receptor in Hartley guinea pig brain cortex after 120 mins by scintillation counting method
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D4 Receptor.
Del Bello F, Bonifazi A, Giorgioni G, Cifani C, Micioni Di Bonaventura MV, Petrelli R, Piergentili A, Fontana S, Mammoli V, Yano H, Matucci R, Vistoli G, Quaglia W.
J Med Chem (2018) 61 : 3712 -3725
PubMed 29589445 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.57 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3354065 1 8.14
CHEMBL4072818 1 8.00
CHEMBL4085780 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3354065 Ki = 7.244 nM 8.14
CHEMBL4072818 Ki = 10.0 nM 8.00
CHEMBL4085780 Ki = 269.15 nM 6.57