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Assay Detail

CHEMBL985173

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

Binding
Inhibition of rat Nav1.2 channel expressed in Xenopus oocytes by whole cell voltage clamp technique
11
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type Oocyte
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium channel protein type 2 subunit alpha (CHEMBL3399)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure/function characterization of micro-conotoxin KIIIA, an analgesic, nearly irreversible blocker of mammalian neuronal sodium channels.
Zhang MM, Green BR, Catlin P, Fiedler B, Azam L, Chadwick A, Terlau H, McArthur JR, French RJ, Gulyas J, Rivier JE, Smith BJ, Norton RS, Olivera BM, Yoshikami D, Bulaj G.
J Biol Chem (2007) 282 : 30699 -30706
PubMed 17724025 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 10 - -
Kd 1 8.52 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL525818 1 8.52
CHEMBL508113 1 -
CHEMBL525208 1 -
CHEMBL525941 1 -
CHEMBL524475 1 -
CHEMBL505134 1 -
CHEMBL506946 1 -
CHEMBL470273 1 -
CHEMBL503290 1 -
CHEMBL524481 1 -
CHEMBL501301 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL525818 Kd = 3.0 nM 8.52
CHEMBL508113 Activity - -
CHEMBL525208 Activity - -
CHEMBL525941 Activity - -
CHEMBL524475 Activity - -
CHEMBL505134 Activity - -
CHEMBL506946 Activity - -
CHEMBL470273 Activity - -
CHEMBL503290 Activity - -
CHEMBL524481 Activity - -
CHEMBL501301 Activity - -