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Assay Detail

CHEMBL857686

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

Binding
Inhibition of radioligand [3H]DAMGO binding to rat brain Opioid receptor mu 1 using 100 nM DAMGO
18
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous 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. 23. Synthesis, opioid receptor binding, and bioassay of the highly selective delta agonist (+)-4-[(alpha R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]- N,N-diethylbenzamide (SNC 80) and related novel nonpeptide delta opioid receptor ligands.
Calderon SN, Rice KC, Rothman RB, Porreca F, Flippen-Anderson JL, Kayakiri H, Xu H, Becketts K, Smith LE, Bilsky EJ, Davis P, Horvath R.
J Med Chem (1997) 40 : 695 -704
PubMed 9057856 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.82 8.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL25230 2 8.01
CHEMBL67195 1 6.78
CHEMBL70111 1 6.37
CHEMBL347712 1 5.91
CHEMBL159618 2 5.70
CHEMBL13470 SNC-80 2 5.61
CHEMBL164055 1 5.47
CHEMBL611159 2 5.24
CHEMBL611160 2 5.07
CHEMBL162690 1 -
CHEMBL153648 2 -
CHEMBL2112042 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL25230 IC50 = 9.71 nM 8.01
CHEMBL67195 IC50 = 167.0 nM 6.78
CHEMBL70111 IC50 = 426.0 nM 6.37
CHEMBL347712 IC50 = 1227.0 nM 5.91
CHEMBL159618 IC50 = 1977.0 nM 5.70
CHEMBL25230 IC50 = 2322.0 nM 5.63
CHEMBL13470 SNC-80 IC50 = 2467.0 nM 5.61
CHEMBL164055 IC50 = 3378.0 nM 5.47
CHEMBL611159 IC50 = 5712.0 nM 5.24
CHEMBL611160 IC50 = 8446.0 nM 5.07
CHEMBL611159 IC50 = 9138.0 nM 5.04
CHEMBL13470 SNC-80 IC50 = 9366.0 nM 5.03
CHEMBL159618 IC50 > 10000.0 nM -
CHEMBL2112042 IC50 > 10000.0 nM -
CHEMBL153648 IC50 > 10000.0 nM -
CHEMBL611160 IC50 > 10000.0 nM -
CHEMBL153648 IC50 > 2500.0 nM -
CHEMBL162690 IC50 > 10000.0 nM -