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Assay Detail

CHEMBL4124267

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

Functional
Agonist activity at mu-opioid receptor in guinea pig ileum assessed as inhibition of electrically induced contractions
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Chemical space screening around Phe3 in opioid peptides: Modulating µ versus δ agonism by Suzuki-Miyaura cross-couplings.
Willemse T, Eiselt E, Hollanders K, Schepens W, van Vlijmen HWT, Chung NN, Blais V, Holleran B, Longpré JM, Schiller PW, Maes BUW, Sarret P, Gendron L, Ballet S.
Bioorg Med Chem Lett (2018) 28 : 2320 -2323
PubMed 29853330 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 8.48 9.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4126102 1 9.41
CHEMBL4128530 1 9.19
CHEMBL4126322 1 9.15
CHEMBL4127547 1 9.10
CHEMBL4127485 1 9.04
CHEMBL4129901 1 8.93
CHEMBL4128945 1 8.90
CHEMBL4129753 1 8.90
CHEMBL4126249 1 8.85
CHEMBL4126050 1 8.82
CHEMBL4129689 1 8.81
CHEMBL4126470 1 8.80
CHEMBL4129679 1 8.65
CHEMBL4127702 1 8.62
CHEMBL4127080 1 8.46
CHEMBL4129548 1 7.62
CHEMBL38874 DAMGO 1 7.55
CHEMBL4128313 1 7.52
CHEMBL4127226 1 7.21
CHEMBL26575 DELTORPHIN 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4126102 IC50 = 0.389 nM 9.41
CHEMBL4128530 IC50 = 0.641 nM 9.19
CHEMBL4126322 IC50 = 0.701 nM 9.15
CHEMBL4127547 IC50 = 0.801 nM 9.10
CHEMBL4127485 IC50 = 0.901 nM 9.04
CHEMBL4129901 IC50 = 1.18 nM 8.93
CHEMBL4128945 IC50 = 1.26 nM 8.90
CHEMBL4129753 IC50 = 1.27 nM 8.90
CHEMBL4126249 IC50 = 1.43 nM 8.85
CHEMBL4126050 IC50 = 1.5 nM 8.82
CHEMBL4129689 IC50 = 1.54 nM 8.81
CHEMBL4126470 IC50 = 1.6 nM 8.80
CHEMBL4129679 IC50 = 2.26 nM 8.65
CHEMBL4127702 IC50 = 2.39 nM 8.62
CHEMBL4127080 IC50 = 3.47 nM 8.46
CHEMBL4129548 IC50 = 24.1 nM 7.62
CHEMBL38874 DAMGO IC50 = 28.3 nM 7.55
CHEMBL4128313 IC50 = 30.4 nM 7.52
CHEMBL4127226 IC50 = 61.7 nM 7.21
CHEMBL26575 DELTORPHIN IC50 = 854.0 nM 6.07