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Assay Detail

CHEMBL3738446

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

Binding
Agonist activity at mu opioid receptor in Hartley guniea pig isolated ileum assessed as inhibition of electrically-stimulated muscle contraction
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Ileum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mu-type opioid receptor (CHEMBL4354)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Discovery of Novel Multifunctional Ligands with μ/δ Opioid Agonist/Neurokinin-1 (NK1) Antagonist Activities for the Treatment of Pain.
Giri AK, Apostol CR, Wang Y, Forte BL, Largent-Milnes TM, Davis P, Rankin D, Molnar G, Olson KM, Porreca F, Vanderah TW, Hruby VJ.
J Med Chem (2015) 58 : 8573 -8583
PubMed 26465170 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.96 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4299371 1 7.68
CHEMBL4299423 1 7.38
CHEMBL4299479 1 7.19
CHEMBL4299415 1 7.11
CHEMBL4299390 1 7.09
CHEMBL4299483 1 6.78
CHEMBL4299466 1 6.64
CHEMBL438389 1 6.46
CHEMBL4299476 1 6.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4299371 IC50 = 21.0 nM 7.68
CHEMBL4299423 IC50 = 42.0 nM 7.38
CHEMBL4299479 IC50 = 65.0 nM 7.19
CHEMBL4299415 IC50 = 77.0 nM 7.11
CHEMBL4299390 IC50 = 81.0 nM 7.09
CHEMBL4299483 IC50 = 166.0 nM 6.78
CHEMBL4299466 IC50 = 230.0 nM 6.64
CHEMBL438389 IC50 = 350.0 nM 6.46
CHEMBL4299476 IC50 = 460.0 nM 6.34