Assay Detail

CHEMBL923703

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Binding

Inhibition of recombinant rat Nav1.8 sodium channel assessed as blockade of TTXR current by patch clamp method

ChEMBL ↗

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Target

Sodium channel protein type 10 subunit alpha (CHEMBL4017) ↗

Open DB target context

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Sodium channel protein type 10 subunit alpha (CHEMBL4017) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Sodium channel protein type 10 subunit alpha

CHEMBL4017

Anchored from Assay target.

Protein identity Sodium channel protein type 10 subunit alpha

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

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

Target

Sodium channel protein type 10 subunit alpha (CHEMBL4017) ↗

Type	SINGLE PROTEIN
Organism	Rattus norvegicus

Publication

A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.

Jarvis MF, Honore P, Shieh CC, Chapman M, Joshi S, Zhang XF, Kort M, Carroll W, Marron B, Atkinson R, Thomas J, Liu D, Krambis M, Liu Y, McGaraughty S, Chu K, Roeloffs R, Zhong C, Mikusa JP, Hernandez G, Gauvin D, Wade C, Zhu C, Pai M, Scanio M, Shi L, Drizin I, Gregg R, Matulenko M, Hakeem A, Gross M, Johnson M, Marsh K, Wagoner PK, Sullivan JP, Faltynek CR, Krafte DS.
Proc Natl Acad Sci U S A (2007) 104 : 8520 -8525
PubMed 17483457 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	7.35	7.35

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL250699	—	—	1	7.35

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL250699	—	IC50	=	45.0	nM	7.35