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Assay Detail

CHEMBL2155055

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

Binding
Displacement of [3H]-DAMGO from mouse MOR/DOR expressed in HEK293 cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type HEK293
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Opioid receptors; mu and delta (CHEMBL2221343)
Type PROTEIN FAMILY
Organism Mus musculus

Publication

Tuned-Affinity Bivalent Ligands for the Characterization of Opioid Receptor Heteromers.
Harvey JH, Long DH, England PM, Whistler JL.
ACS Med Chem Lett (2012) 3 : 640 -644
PubMed 23585918 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.78 9.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19019 NALTREXONE 4.0 1 9.06
CHEMBL1237164 NALTRINDOLE HYDROCHLORIDE 1 8.46
CHEMBL2151247 1 8.38
CHEMBL963 OXYMORPHONE 4.0 1 8.33
CHEMBL2151327 1 8.21
CHEMBL2151328 1 6.94
CHEMBL2151248 1 6.90
CHEMBL2151246 1 5.92
CHEMBL2151245 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19019 NALTREXONE Ki = 0.871 nM 9.06
CHEMBL1237164 NALTRINDOLE HYDROCHLORIDE Ki = 3.467 nM 8.46
CHEMBL2151247 Ki = 4.169 nM 8.38
CHEMBL963 OXYMORPHONE Ki = 4.677 nM 8.33
CHEMBL2151327 Ki = 6.166 nM 8.21
CHEMBL2151328 Ki = 114.82 nM 6.94
CHEMBL2151248 Ki = 125.89 nM 6.90
CHEMBL2151246 Ki = 1202.26 nM 5.92
CHEMBL2151245 Ki < 1.0 nM -