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Assay Detail

CHEMBL1056547

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

Binding
Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO cells
5
Total Activities
5
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 Intermediate

Target

Kappa-type opioid receptor (CHEMBL237)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) benzamide (ADL5747).
Le Bourdonnec B, Windh RT, Leister LK, Zhou QJ, Ajello CW, Gu M, Chu GH, Tuthill PA, Barker WM, Koblish M, Wiant DD, Graczyk TM, Belanger S, Cassel JA, Feschenko MS, Brogdon BL, Smith SA, Derelanko MJ, Kutz S, Little PJ, DeHaven RN, DeHaven-Hudkins DL, Dolle RE.
J Med Chem (2009) 52 : 5685 -5702
PubMed 19694468 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.12 6.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL562478 1 6.41
CHEMBL550063 1 6.25
CHEMBL551412 1 6.10
CHEMBL551613 1 6.05
CHEMBL551413 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL562478 Ki = 390.0 nM 6.41
CHEMBL550063 Ki = 560.0 nM 6.25
CHEMBL551412 Ki = 800.0 nM 6.10
CHEMBL551613 Ki = 890.0 nM 6.05
CHEMBL551413 Ki = 1600.0 nM 5.80