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Assay Detail

CHEMBL3379241

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

Binding
Displacement of [3H]-(+)-MK-801 from NMDA receptor PCP binding site in guinea pig brain cortex membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted κ-opioid receptor agonists.
Bourgeois C, Werfel E, Galla F, Lehmkuhl K, Torres-Gómez H, Schepmann D, Kögel B, Christoph T, Straßburger W, Englberger W, Soeberdt M, Hüwel S, Galla HJ, Wünsch B.
J Med Chem (2014) 57 : 6845 -6860
PubMed 25062506 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.98 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL344151 DIZOCILPINE MALEATE -1.0 1 8.54
CHEMBL1165411 DEXOXADROL 2.0 1 7.42
CHEMBL3323509 1 -
CHEMBL3323512 1 -
CHEMBL3323515 1 -
CHEMBL3323516 1 -
CHEMBL3323519 1 -
CHEMBL3323522 1 -
CHEMBL3323527 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL344151 DIZOCILPINE MALEATE Ki = 2.9 nM 8.54
CHEMBL1165411 DEXOXADROL Ki = 38.0 nM 7.42
CHEMBL3323509 Ki - -
CHEMBL3323512 Ki - -
CHEMBL3323515 Ki - -
CHEMBL3323516 Ki - -
CHEMBL3323519 Ki - -
CHEMBL3323522 Ki - -
CHEMBL3323527 Ki - -