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Assay Detail

CHEMBL1225825

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

Binding
Inhibition of human Nav 1.7 channel by electrophysiology
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium channel protein type 9 subunit alpha (CHEMBL4296)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Substituted biaryl pyrazoles as sodium channel blockers.
Tyagarajan S, Chakravarty PK, Zhou B, Taylor B, Fisher MH, Wyvratt MJ, Lyons K, Klatt T, Li X, Kumar S, Williams B, Felix J, Priest BT, Brochu RM, Warren V, Smith M, Garcia M, Kaczorowski GJ, Martin WJ, Abbadie C, McGowan E, Jochnowitz N, Parsons WH.
Bioorg Med Chem Lett (2010) 20 : 5480 -5483
PubMed 20709545 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 9.10 10.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1224266 1 10.74
CHEMBL1224265 1 9.96
CHEMBL1224198 1 7.89
CHEMBL1224197 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1224266 Ki = 0.018 nM 10.74
CHEMBL1224265 Ki = 0.111 nM 9.96
CHEMBL1224198 Ki = 13.0 nM 7.89
CHEMBL1224197 Ki = 15.0 nM 7.82