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Assay Detail

CHEMBL2188651

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Functional
Agonist activity at mu opioid receptor in guinea pig ileum
12
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

Variation of the net charge, lipophilicity, and side chain flexibility in Dmt(1)-DALDA: Effect on Opioid Activity and Biodistribution.
Novoa A, Van Dorpe S, Wynendaele E, Spetea M, Bracke N, Stalmans S, Betti C, Chung NN, Lemieux C, Zuegg J, Cooper MA, Tourwé D, De Spiegeleer B, Schiller PW, Ballet S.
J Med Chem (2012) 55 : 9549 -9561
PubMed 23102273 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.54 9.51
IC35 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2181200 1 9.51
CHEMBL2181195 1 9.19
CHEMBL2181199 1 9.05
CHEMBL2181196 1 9.00
CHEMBL2181202 1 8.85
CHEMBL2181193 1 8.84
CHEMBL2181201 1 8.66
CHEMBL2181197 1 8.36
CHEMBL2181198 1 8.08
CHEMBL2181192 1 7.31
CHEMBL2181194 1 7.12
CHEMBL2181191 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2181200 IC50 = 0.31 nM 9.51
CHEMBL2181195 IC50 = 0.65 nM 9.19
CHEMBL2181199 IC50 = 0.89 nM 9.05
CHEMBL2181196 IC50 = 1.01 nM 9.00
CHEMBL2181202 IC50 = 1.41 nM 8.85
CHEMBL2181193 IC50 = 1.45 nM 8.84
CHEMBL2181201 IC50 = 2.2 nM 8.66
CHEMBL2181197 IC50 = 4.35 nM 8.36
CHEMBL2181198 IC50 = 8.3 nM 8.08
CHEMBL2181192 IC50 = 49.0 nM 7.31
CHEMBL2181194 IC50 = 76.0 nM 7.12
CHEMBL2181191 IC35 = 0.78 nM -