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Assay Detail

CHEMBL747874

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Binding
Evaluated for inhibition of [3H]DAMGO binding from mu receptor in rat brain membranes
9
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Probes for narcotic receptor mediated phenomena. 19. Synthesis of (+)-4-[(alpha R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3- methoxybenzyl]-N,N-diethylbenzamide (SNC 80): a highly selective, nonpeptide delta opioid receptor agonist.
Calderon SN, Rothman RB, Porreca F, Flippen-Anderson JL, McNutt RW, Xu H, Smith LE, Bilsky EJ, Davis P, Rice KC.
J Med Chem (1994) 37 : 2125 -2128
PubMed 8035418 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.12 8.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL25230 1 8.01
CHEMBL303855 1 7.33
CHEMBL69052 1 6.78
CHEMBL70111 1 6.37
CHEMBL67195 1 5.63
CHEMBL611159 1 5.61
CHEMBL13470 SNC-80 2 5.24
CHEMBL67378 1 5.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL25230 IC50 = 9.71 nM 8.01
CHEMBL303855 IC50 = 46.3 nM 7.33
CHEMBL69052 IC50 = 167.0 nM 6.78
CHEMBL70111 IC50 = 426.0 nM 6.37
CHEMBL67195 IC50 = 2322.0 nM 5.63
CHEMBL611159 IC50 = 2467.0 nM 5.61
CHEMBL13470 SNC-80 IC50 = 5712.0 nM 5.24
CHEMBL67378 IC50 = 9138.0 nM 5.04
CHEMBL13470 SNC-80 IC50 = 9366.0 nM 5.03