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Assay Detail

CHEMBL2183136

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

Binding
Displacement of [3H]DAMGO from MOR in guinea pig brain membrane
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mu-type opioid receptor (CHEMBL4354)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Fumaroylamino-4,5-epoxymorphinans and related opioids with irreversible μ opioid receptor antagonist effects.
Moynihan HA, Derrick I, Broadbear JH, Greedy BM, Aceto MD, Harris LS, Purington LC, Thomas MP, Woods JH, Traynor JR, Husbands SM, Lewis JW.
J Med Chem (2012) 55 : 9868 -9874
PubMed 23043264 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 9.17 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2179258 1 9.70
CHEMBL2179264 1 9.62
CHEMBL473136 1 9.40
CHEMBL2179263 1 9.15
CHEMBL2179259 1 9.15
CHEMBL2179262 1 9.05
CHEMBL2179261 1 9.05
CHEMBL511142 BUPRENORPHINE 4.0 1 8.89
CHEMBL2179260 1 8.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2179258 Ki = 0.2 nM 9.70
CHEMBL2179264 Ki = 0.24 nM 9.62
CHEMBL473136 Ki = 0.4 nM 9.40
CHEMBL2179263 Ki = 0.7 nM 9.15
CHEMBL2179259 Ki = 0.7 nM 9.15
CHEMBL2179262 Ki = 0.9 nM 9.05
CHEMBL2179261 Ki = 0.9 nM 9.05
CHEMBL511142 BUPRENORPHINE Ki = 1.3 nM 8.89
CHEMBL2179260 Ki = 2.8 nM 8.55