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Assay Detail

CHEMBL5030197

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

Functional
Inhibition of electric-field induced mouse vas deferens contraction
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Tissue Vas deferens
Confidence 1 — Organism
Curated By Autocuration

Target

Vas deferens (CHEMBL613599)
Type TISSUE
Organism Mus musculus

Publication

Novel Cyclic Endomorphin Analogues with Multiple Modifications and Oligoarginine Vector Exhibit Potent Antinociception with Reduced Opioid-like Side Effects.
Zhang YZ, Wang MM, Wang SY, Wang XF, Yang WJ, Zhao YN, Han FT, Zhang Y, Gu N, Wang CL.
J Med Chem (2021) 64 : 16801 -16819
PubMed 34781680 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.13 7.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL333357 ENDOMORPHIN 2 1 7.37
CHEMBL5076581 1 7.32
CHEMBL5085104 1 7.31
CHEMBL316446 ENDOMORPHIN-1 1 7.30
CHEMBL5080666 1 7.01
CHEMBL5084034 1 6.97
CHEMBL5080233 1 6.86
CHEMBL5078349 1 6.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL333357 ENDOMORPHIN 2 IC50 = 42.9 nM 7.37
CHEMBL5076581 IC50 = 47.5 nM 7.32
CHEMBL5085104 IC50 = 49.3 nM 7.31
CHEMBL316446 ENDOMORPHIN-1 IC50 = 50.1 nM 7.30
CHEMBL5080666 IC50 = 97.5 nM 7.01
CHEMBL5084034 IC50 = 107.5 nM 6.97
CHEMBL5080233 IC50 = 137.8 nM 6.86
CHEMBL5078349 IC50 = 139.0 nM 6.86