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Assay Detail

CHEMBL683778

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Functional
in vitro inhibition of electrically evoked contractions of GPI (Guinea pig ileum)
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cavia porcellus (CHEMBL369)
Type ORGANISM
Organism Cavia porcellus

Publication

Pseudoproline-containing analogues of morphiceptin and endomorphin-2: evidence for a cis Tyr-Pro amide bond in the bioactive conformation.
Keller M, Boissard C, Patiny L, Chung NN, Lemieux C, Mutter M, Schiller PW.
J Med Chem (2001) 44 : 3896 -3903
PubMed 11689075 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.23 8.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL333357 ENDOMORPHIN 2 1 8.11
CHEMBL2370620 1 6.96
CHEMBL35838 [LEU5]ENKEPHALIN 1 6.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL333357 ENDOMORPHIN 2 IC50 = 7.71 nM 8.11
CHEMBL2370620 IC50 = 109.0 nM 6.96
CHEMBL35838 [LEU5]ENKEPHALIN IC50 = 246.0 nM 6.61