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Assay Detail

CHEMBL756649

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

Binding
Inhibition of [3H]DAMGO binding to mu opioid receptor of rat brain membranes
23
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

3-(alphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N-alkyl-N-arylbenzamides: potent, non-peptidic agonists of both the micro and delta opioid receptors.
Bishop MJ, Garrido DM, Boswell GE, Collins MA, Harris PA, McNutt RW, O'Neill SJ, Wei K, Chang KJ.
J Med Chem (2003) 46 : 623 -633
PubMed 12570383 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 8.58 9.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL155892 2 9.34
CHEMBL70 MORPHINE 4.0 1 9.00
CHEMBL156584 1 8.97
CHEMBL434075 1 8.83
CHEMBL596 FENTANYL 4.0 1 8.82
CHEMBL345683 1 8.81
CHEMBL157294 1 8.80
CHEMBL158205 1 8.74
CHEMBL422877 1 8.67
CHEMBL156440 1 8.66
CHEMBL346514 1 8.63
CHEMBL157095 1 8.62
CHEMBL157660 1 8.59
CHEMBL156230 1 8.56
CHEMBL345431 1 8.56
CHEMBL348415 1 8.49
CHEMBL349120 1 8.47
CHEMBL155797 1 8.46
CHEMBL348585 1 8.15
CHEMBL346987 1 8.15
CHEMBL155748 1 8.05
CHEMBL25230 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL155892 Ki = 0.46 nM 9.34
CHEMBL70 MORPHINE Ki = 1.0 nM 9.00
CHEMBL156584 Ki = 1.06 nM 8.97
CHEMBL434075 Ki = 1.49 nM 8.83
CHEMBL596 FENTANYL Ki = 1.5 nM 8.82
CHEMBL345683 Ki = 1.55 nM 8.81
CHEMBL157294 Ki = 1.58 nM 8.80
CHEMBL158205 Ki = 1.82 nM 8.74
CHEMBL422877 Ki = 2.16 nM 8.67
CHEMBL156440 Ki = 2.19 nM 8.66
CHEMBL346514 Ki = 2.35 nM 8.63
CHEMBL157095 Ki = 2.37 nM 8.62
CHEMBL157660 Ki = 2.55 nM 8.59
CHEMBL156230 Ki = 2.74 nM 8.56
CHEMBL345431 Ki = 2.78 nM 8.56
CHEMBL348415 Ki = 3.2 nM 8.49
CHEMBL349120 Ki = 3.39 nM 8.47
CHEMBL155797 Ki = 3.46 nM 8.46
CHEMBL348585 Ki = 7.06 nM 8.15
CHEMBL346987 Ki = 7.08 nM 8.15
CHEMBL155892 Ki = 7.56 nM 8.12
CHEMBL155748 Ki = 8.88 nM 8.05
CHEMBL25230 Ki = 15.0 nM 7.82