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Assay Detail

CHEMBL744887

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

Functional
In vivo antinociceptive activity by tail-pressure test in mice in the presence of dertorphin II as agonist upon intracerebral administration
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mus musculus (CHEMBL375)
Type ORGANISM
Organism Mus musculus

Publication

Development of potent bifunctional endomorphin-2 analogues with mixed mu-/delta-opioid agonist and delta-opioid antagonist properties.
Fujita Y, Tsuda Y, Li T, Motoyama T, Takahashi M, Shimizu Y, Yokoi T, Sasaki Y, Ambo A, Kita A, Jinsmaa Y, Bryant SD, Lazarus LH, Okada Y.
J Med Chem (2004) 47 : 3591 -3599
PubMed 15214786 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 11 6.38 7.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL419591 1 7.18
CHEMBL332196 1 7.05
CHEMBL120091 1 6.94
CHEMBL118942 1 6.70
CHEMBL409907 1 6.52
CHEMBL332371 1 6.33
CHEMBL333350 1 6.14
CHEMBL433643 1 6.12
CHEMBL327036 1 5.93
CHEMBL334147 1 5.88
CHEMBL331255 1 5.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL419591 Kd = 66.07 nM 7.18
CHEMBL332196 Kd = 89.13 nM 7.05
CHEMBL120091 Kd = 114.82 nM 6.94
CHEMBL118942 Kd = 199.53 nM 6.70
CHEMBL409907 Kd = 302.0 nM 6.52
CHEMBL332371 Kd = 467.74 nM 6.33
CHEMBL333350 Kd = 724.44 nM 6.14
CHEMBL433643 Kd = 758.58 nM 6.12
CHEMBL327036 Kd = 1174.9 nM 5.93
CHEMBL334147 Kd = 1318.26 nM 5.88
CHEMBL331255 Kd = 3890.45 nM 5.41