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Assay Detail

CHEMBL755352

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

Binding
Inhibition of [3H]- DAMGO binding to Rat brain Opioid receptor mu 1
13
Total Activities
11
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

Probes for narcotic receptor-mediated phenomena. 21. Novel derivatives of 3-(1,2,3,4,5,11-hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol- 6-yl)-phenols with improved delta opioid receptor selectivity.
Bertha CM, Ellis M, Flippen-Anderson JL, Porreca F, Rothman RB, Davis P, Xu H, Becketts K, Rice KC.
J Med Chem (1996) 39 : 2081 -2086
PubMed 8642567 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.28 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL140050 ETORPHINE 2.0 1 9.85
CHEMBL70 MORPHINE 4.0 1 8.71
CHEMBL65348 2 7.62
CHEMBL302454 2 7.54
CHEMBL290301 1 7.53
CHEMBL340032 DADLE 1 7.38
CHEMBL440123 1 7.32
CHEMBL2111530 1 7.18
CHEMBL38791 1 6.86
CHEMBL13470 SNC-80 1 5.61
CHEMBL303113 1 5.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL140050 ETORPHINE IC50 = 0.14 nM 9.85
CHEMBL70 MORPHINE IC50 = 1.94 nM 8.71
CHEMBL65348 IC50 = 24.2 nM 7.62
CHEMBL302454 IC50 = 28.8 nM 7.54
CHEMBL302454 IC50 = 29.4 nM 7.53
CHEMBL290301 IC50 = 29.8 nM 7.53
CHEMBL340032 DADLE IC50 = 41.9 nM 7.38
CHEMBL440123 IC50 = 48.4 nM 7.32
CHEMBL2111530 IC50 = 66.4 nM 7.18
CHEMBL38791 IC50 = 136.8 nM 6.86
CHEMBL65348 IC50 = 474.2 nM 6.32
CHEMBL13470 SNC-80 IC50 = 2467.0 nM 5.61
CHEMBL303113 IC50 = 7267.0 nM 5.14