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Assay Detail

CHEMBL5055732

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

Functional
Antinociceptive activity in po dosed FVB hNav1.7 transgenic mouse model of inherited erythromelalgia harboring I848T mutation assessed as reduction in number of nociceptive aconitine injected after compound administration
4
Total Activities
2
Compounds Tested
2
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 Acyl-sulfonamide Na<sub>v</sub>1.7 Inhibitors GDC-0276 and GDC-0310.
Safina BS, McKerrall SJ, Sun S, Chen CA, Chowdhury S, Jia Q, Li J, Zenova AY, Andrez JC, Bankar G, Bergeron P, Chang JH, Chang E, Chen J, Dean R, Decker SM, DiPasquale A, Focken T, Hemeon I, Khakh K, Kim A, Kwan R, Lindgren A, Lin S, Maher J, Mezeyova J, Misner D, Nelkenbrecher K, Pang J, Reese R, Shields SD, Sojo L, Sheng T, Verschoof H, Waldbrook M, Wilson MS, Xie Z, Young C, Zabka TS, Hackos DH, Ortwine DF, White AD, Johnson JP, Robinette CL, Dehnhardt CM, Cohen CJ, Sutherlin DP.
J Med Chem (2021) 64 : 2953 -2966
PubMed 33682420 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 5.87 5.96
fEC50 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5094715 2 5.96
CHEMBL3657855 2 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5094715 EC50 = 1100.0 nM 5.96
CHEMBL3657855 EC50 = 1700.0 nM 5.77
CHEMBL3657855 fEC50 = 0.42 nM -
CHEMBL5094715 fEC50 = 3.5 nM -