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Assay Detail

CHEMBL687345

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

Functional
In vitro inhibition of electrically evoked contractions of GPI (Guinea pig ileum)
8
Total Activities
8
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 8 6.75 7.65

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL338198 1 7.65
CHEMBL339725 1 7.38
CHEMBL126611 1 7.13
CHEMBL126794 1 6.61
CHEMBL339724 1 6.52
CHEMBL129323 1 6.33
CHEMBL338572 1 6.30
CHEMBL338113 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL338198 IC50 = 22.2 nM 7.65
CHEMBL339725 IC50 = 41.7 nM 7.38
CHEMBL126611 IC50 = 74.5 nM 7.13
CHEMBL126794 IC50 = 246.0 nM 6.61
CHEMBL339724 IC50 = 305.0 nM 6.52
CHEMBL129323 IC50 = 470.0 nM 6.33
CHEMBL338572 IC50 = 502.0 nM 6.30
CHEMBL338113 IC50 = 860.0 nM 6.07