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Assay Detail

CHEMBL2387948

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

Binding
Inhibition of mu opioid receptor in guinea pig ileum/longitudinal muscle with myenteric plexus assessed as inhibition of electrically-stimulated muscle contraction
22
Total Activities
22
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

Effect of anchoring 4-anilidopiperidines to opioid peptides.
Petrov RR, Lee YS, Vardanyan RS, Liu L, Ma SW, Davis P, Lai J, Porreca F, Vanderah TW, Hruby VJ.
Bioorg Med Chem Lett (2013) 23 : 3434 -3437
PubMed 23623418 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.14 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL405618 ANALOG OF DYNORPHIN A 1 8.92
CHEMBL2387215 1 8.42
CHEMBL2387216 1 8.11
CHEMBL200199 BIPHALIN 1 8.06
CHEMBL316446 ENDOMORPHIN-1 1 7.96
CHEMBL2387327 1 7.92
CHEMBL214022 1 7.38
CHEMBL2387211 1 7.31
CHEMBL2387328 1 7.17
CHEMBL2387341 1 7.07
CHEMBL2387339 1 7.01
CHEMBL2387213 1 7.01
CHEMBL2387337 1 6.96
CHEMBL2387214 1 6.92
CHEMBL2387329 1 6.89
CHEMBL2387210 1 6.82
CHEMBL2387330 1 6.32
CHEMBL2387340 1 6.24
CHEMBL2387338 1 6.02
CHEMBL2387212 1 5.72
CHEMBL2387331 1 5.68
CHEMBL20226 DELTORPHIN II 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL405618 ANALOG OF DYNORPHIN A IC50 = 1.2 nM 8.92
CHEMBL2387215 IC50 = 3.8 nM 8.42
CHEMBL2387216 IC50 = 7.7 nM 8.11
CHEMBL200199 BIPHALIN IC50 = 8.8 nM 8.06
CHEMBL316446 ENDOMORPHIN-1 IC50 = 11.0 nM 7.96
CHEMBL2387327 IC50 = 12.0 nM 7.92
CHEMBL214022 IC50 = 42.0 nM 7.38
CHEMBL2387211 IC50 = 49.0 nM 7.31
CHEMBL2387328 IC50 = 67.0 nM 7.17
CHEMBL2387341 IC50 = 86.0 nM 7.07
CHEMBL2387339 IC50 = 97.0 nM 7.01
CHEMBL2387213 IC50 = 98.0 nM 7.01
CHEMBL2387337 IC50 = 110.0 nM 6.96
CHEMBL2387214 IC50 = 120.0 nM 6.92
CHEMBL2387329 IC50 = 130.0 nM 6.89
CHEMBL2387210 IC50 = 150.0 nM 6.82
CHEMBL2387330 IC50 = 480.0 nM 6.32
CHEMBL2387340 IC50 = 580.0 nM 6.24
CHEMBL2387338 IC50 = 950.0 nM 6.02
CHEMBL2387212 IC50 = 1900.0 nM 5.72
CHEMBL2387331 IC50 = 2100.0 nM 5.68
CHEMBL20226 DELTORPHIN II IC50 > 3000.0 nM -