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Assay Detail

CHEMBL855303

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

Binding
Displacement of [3H]DAMGO from rat mu opioid receptor
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Mu-type opioid receptor (CHEMBL270)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and evaluation of 3-aminopropionyl substituted fentanyl analogues for opioid activity.
Petrov RR, Vardanyan RS, Lee YS, Ma SW, Davis P, Begay LJ, Lai JY, Porreca F, Hruby VJ.
Bioorg Med Chem Lett (2006) 16 : 4946 -4950
PubMed 16828552 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.54 9.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL214022 1 9.01
CHEMBL385909 1 7.52
CHEMBL214657 1 6.84
CHEMBL212589 1 6.66
CHEMBL214285 1 6.35
CHEMBL386990 1 5.99
CHEMBL385168 AMINOFENTANYL 1 5.68
CHEMBL216492 1 5.57
CHEMBL216239 CARBOXYFENTANYL 1 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL214022 IC50 = 0.97 nM 9.01
CHEMBL385909 IC50 = 29.9 nM 7.52
CHEMBL214657 IC50 = 146.0 nM 6.84
CHEMBL212589 IC50 = 217.0 nM 6.66
CHEMBL214285 IC50 = 451.0 nM 6.35
CHEMBL386990 IC50 = 1030.0 nM 5.99
CHEMBL385168 AMINOFENTANYL IC50 = 2080.0 nM 5.68
CHEMBL216492 IC50 = 2680.0 nM 5.57
CHEMBL216239 CARBOXYFENTANYL IC50 = 5400.0 nM 5.27