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Assay Detail

CHEMBL741590

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

Functional
Inhibition of electrically evoked contractions in mouse vas deferens
16
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Delta-type opioid receptor (CHEMBL3222)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Conformationally restricted deltorphin analogues.
Schiller PW, Weltrowska G, Nguyen TM, Wilkes BC, Chung NN, Lemieux C.
J Med Chem (1992) 35 : 3956 -3961
PubMed 1331451 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 8.05 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL124435 1 10.10
CHEMBL124941 2 9.94
CHEMBL317956 DELTORPHIN C 1 9.83
CHEMBL132164 1 9.33
CHEMBL20775 DELTORPHIN A 2 9.16
CHEMBL8234 ENKEPHALIN 1 7.94
CHEMBL338466 1 7.76
CHEMBL339089 1 7.64
CHEMBL337898 1 7.37
CHEMBL129815 1 7.04
CHEMBL330991 1 6.32
CHEMBL338985 1 6.04
CHEMBL63407 1 5.41
CHEMBL262312 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL124435 IC50 = 0.0803 nM 10.10
CHEMBL124941 IC50 = 0.115 nM 9.94
CHEMBL317956 DELTORPHIN C IC50 = 0.147 nM 9.83
CHEMBL124941 IC50 = 0.163 nM 9.79
CHEMBL132164 IC50 = 0.467 nM 9.33
CHEMBL20775 DELTORPHIN A IC50 = 0.695 nM 9.16
CHEMBL8234 ENKEPHALIN IC50 = 11.4 nM 7.94
CHEMBL338466 IC50 = 17.3 nM 7.76
CHEMBL339089 IC50 = 22.8 nM 7.64
CHEMBL337898 IC50 = 42.7 nM 7.37
CHEMBL129815 IC50 = 90.5 nM 7.04
CHEMBL20775 DELTORPHIN A IC50 = 98.3 nM 7.01
CHEMBL330991 IC50 = 481.0 nM 6.32
CHEMBL338985 IC50 = 919.0 nM 6.04
CHEMBL63407 IC50 = 3880.0 nM 5.41
CHEMBL262312 IC50 > 10000.0 nM -