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Assay Detail

CHEMBL753393

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

Binding
Competitive binding displacement analyses was performed from permanently transfected HEK293 cells expressing human Opioid receptor mu 1
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Mu-type opioid receptor (CHEMBL233)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

High-affinity, non-peptide agonists for the ORL1 (orphanin FQ/nociceptin) receptor.
Röver S, Adam G, Cesura AM, Galley G, Jenck F, Monsma FJ, Wichmann J, Dautzenberg FM.
J Med Chem (2000) 43 : 1329 -1338
PubMed 10753470 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.92 8.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27729 1 8.59
CHEMBL26987 1 8.48
CHEMBL283910 1 8.23
CHEMBL281274 1 8.23
CHEMBL283265 1 8.23
CHEMBL283480 1 8.14
CHEMBL418020 1 8.08
CHEMBL27699 1 8.05
CHEMBL447779 1 7.96
CHEMBL26999 1 7.82
CHEMBL283617 1 7.78
CHEMBL285377 1 7.72
CHEMBL28172 1 7.58
CHEMBL280827 1 7.50
CHEMBL26483 1 7.21
CHEMBL27093 1 7.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27729 Ki = 2.6 nM 8.59
CHEMBL26987 Ki = 3.3 nM 8.48
CHEMBL283910 Ki = 5.9 nM 8.23
CHEMBL281274 Ki = 5.9 nM 8.23
CHEMBL283265 Ki = 5.9 nM 8.23
CHEMBL283480 Ki = 7.2 nM 8.14
CHEMBL418020 Ki = 8.4 nM 8.08
CHEMBL27699 Ki = 8.9 nM 8.05
CHEMBL447779 Ki = 10.9 nM 7.96
CHEMBL26999 Ki = 15.1 nM 7.82
CHEMBL283617 Ki = 16.6 nM 7.78
CHEMBL285377 Ki = 19.2 nM 7.72
CHEMBL28172 Ki = 26.0 nM 7.58
CHEMBL280827 Ki = 31.7 nM 7.50
CHEMBL26483 Ki = 61.0 nM 7.21
CHEMBL27093 Ki = 77.0 nM 7.11