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Assay Detail

CHEMBL4256633

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

Functional
Antinociceptive activity in po dosed FVB hSCN9a Tg inherited erythromelalgia mouse model expressing human NaV1.7 I848T mutant assessed as inhibition of aconitine-induced pain administered 2 hr prior to aconitine challenge measured for 30 mins
4
Total Activities
3
Compounds Tested
2
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

Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNaV1.7 Inhibitors for the Treatment of Pain.
Focken T, Chowdhury S, Zenova A, Grimwood ME, Chabot C, Sheng T, Hemeon I, Decker SM, Wilson M, Bichler P, Jia Q, Sun S, Young C, Lin S, Goodchild SJ, Shuart NG, Chang E, Xie Z, Li B, Khakh K, Bankar G, Waldbrook M, Kwan R, Nelkenbrecher K, Karimi Tari P, Chahal N, Sojo L, Robinette CL, White AD, Chen CA, Zhang Y, Pang J, Chang JH, Hackos DH, Johnson JP, Cohen CJ, Ortwine DF, Sutherlin DP, Dehnhardt CM, Safina BS.
J Med Chem (2018) 61 : 4810 -4831
PubMed 29737846 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 5.40 6.30
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4290579 1 6.30
CHEMBL4279238 2 5.24
CHEMBL4285790 1 4.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4290579 EC50 = 500.0 nM 6.30
CHEMBL4279238 EC50 = 5800.0 nM 5.24
CHEMBL4285790 EC50 = 21200.0 nM 4.67
CHEMBL4279238 Inhibition - % -