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Assay Detail

CHEMBL4623862

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

Functional
Analgesic activity in po dosed Slc:ddY mouse model of partial spinal nerve ligation assessed as reduction in thermal hyperalgesia measured at 60 mins by paw thermal stimulator method
5
Total Activities
2
Compounds Tested
4
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mus musculus (CHEMBL375)
Type ORGANISM
Organism Mus musculus

Publication

Discovery of DS-1971a, a Potent, Selective Na<sub>V</sub>1.7 Inhibitor.
Shinozuka T, Kobayashi H, Suzuki S, Tanaka K, Karanjule N, Hayashi N, Tsuda T, Tokumaru E, Inoue M, Ueda K, Kimoto H, Domon Y, Takahashi S, Kubota K, Yokoyama T, Shimizugawa A, Koishi R, Fujiwara C, Asano D, Sakakura T, Takasuna K, Abe Y, Watanabe T, Kitano Y.
J Med Chem (2020) 63 : 10204 -10220
PubMed 32392056 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
ED50 2 - -
Activity 1 - -
EC50 1 7.47 7.47
fEC50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4633566 DS-1971 2.0 4 7.47
CHEMBL2325014 PF-05089771 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4633566 DS-1971 EC50 = 33.6 nM 7.47
CHEMBL2325014 PF-05089771 ED50 = 3.0 mg.kg-1 -
CHEMBL4633566 DS-1971 Activity - -
CHEMBL4633566 DS-1971 ED50 = 0.32 mg.kg-1 -
CHEMBL4633566 DS-1971 fEC50 = 1.1 nM -