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Assay Detail

CHEMBL685496

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

Functional
Inhibition of the electrically induced muscle contractions was determined using the guinea pig ileum
23
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Ileum
Confidence 1 — Organism
Curated By Expert

Target

Cavia porcellus (CHEMBL369)
Type ORGANISM
Organism Cavia porcellus

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
EC50 23 8.02 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL434075 1 9.17
CHEMBL349120 1 9.03
CHEMBL346514 1 8.96
CHEMBL157095 1 8.91
CHEMBL345683 1 8.91
CHEMBL155892 2 8.47
CHEMBL346987 1 8.40
CHEMBL157294 1 8.39
CHEMBL345431 1 8.39
CHEMBL348415 1 8.36
CHEMBL596 FENTANYL 4.0 1 8.35
CHEMBL155797 1 8.31
CHEMBL156230 1 8.25
CHEMBL422877 1 8.22
CHEMBL156440 1 8.18
CHEMBL157660 1 7.94
CHEMBL158205 1 7.75
CHEMBL155748 1 7.39
CHEMBL70 MORPHINE 4.0 1 7.29
CHEMBL156584 1 7.22
CHEMBL25230 1 6.82
CHEMBL348585 1 5.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL434075 EC50 = 0.67 nM 9.17
CHEMBL349120 EC50 = 0.94 nM 9.03
CHEMBL346514 EC50 = 1.1 nM 8.96
CHEMBL345683 EC50 = 1.22 nM 8.91
CHEMBL157095 EC50 = 1.23 nM 8.91
CHEMBL155892 EC50 = 3.4 nM 8.47
CHEMBL346987 EC50 = 4.0 nM 8.40
CHEMBL345431 EC50 = 4.1 nM 8.39
CHEMBL157294 EC50 = 4.1 nM 8.39
CHEMBL348415 EC50 = 4.35 nM 8.36
CHEMBL596 FENTANYL EC50 = 4.5 nM 8.35
CHEMBL155797 EC50 = 4.9 nM 8.31
CHEMBL156230 EC50 = 5.6 nM 8.25
CHEMBL422877 EC50 = 6.07 nM 8.22
CHEMBL156440 EC50 = 6.6 nM 8.18
CHEMBL157660 EC50 = 11.5 nM 7.94
CHEMBL158205 EC50 = 18.0 nM 7.75
CHEMBL155748 EC50 = 41.0 nM 7.39
CHEMBL70 MORPHINE EC50 = 51.0 nM 7.29
CHEMBL156584 EC50 = 59.5 nM 7.22
CHEMBL25230 EC50 = 150.0 nM 6.82
CHEMBL348585 EC50 = 1053.0 nM 5.98
CHEMBL155892 EC50 = 1800.0 nM 5.75