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Assay Detail

CHEMBL746591

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

Functional
In vitro concentration required to inhibit electrically evoked twitch in isolated mouse vas deferens.
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 1 — Organism
Curated By Intermediate

Target

Mus musculus (CHEMBL375)
Type ORGANISM
Organism Mus musculus

Publication

Dermorphin and deltorphin glycosylated analogues: synthesis and antinociceptive activity after systemic administration.
Negri L, Lattanzi R, Tabacco F, Orrù L, Severini C, Scolaro B, Rocchi R.
J Med Chem (1999) 42 : 400 -404
PubMed 9986710 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.89 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL317956 DELTORPHIN C 1 9.70
CHEMBL429717 1 8.57
CHEMBL405663 1 8.51
CHEMBL408495 1 8.37
CHEMBL134186 1 8.16
CHEMBL261944 1 7.75
CHEMBL278789 DERMORPHIN 1 7.72
CHEMBL130791 1 7.62
CHEMBL2370690 1 7.46
CHEMBL335903 1 7.44
CHEMBL265781 1 7.40
CHEMBL268625 1 7.37
CHEMBL385083 1 7.26
CHEMBL402691 1 7.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL317956 DELTORPHIN C IC50 = 0.2 nM 9.70
CHEMBL429717 IC50 = 2.7 nM 8.57
CHEMBL405663 IC50 = 3.1 nM 8.51
CHEMBL408495 IC50 = 4.3 nM 8.37
CHEMBL134186 IC50 = 6.9 nM 8.16
CHEMBL261944 IC50 = 18.0 nM 7.75
CHEMBL278789 DERMORPHIN IC50 = 19.0 nM 7.72
CHEMBL130791 IC50 = 24.0 nM 7.62
CHEMBL2370690 IC50 = 35.0 nM 7.46
CHEMBL335903 IC50 = 36.0 nM 7.44
CHEMBL265781 IC50 = 40.0 nM 7.40
CHEMBL268625 IC50 = 43.0 nM 7.37
CHEMBL385083 IC50 = 55.0 nM 7.26
CHEMBL402691 IC50 = 65.0 nM 7.19