Assay Detail

CHEMBL5041216

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Toxicity

Inhibition of human Nav1.5 by PatchXpress assay

ChEMBL ↗

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Target

Sodium channel protein type 5 subunit alpha (CHEMBL1980) ↗

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Sodium channel protein type 5 subunit alpha (CHEMBL1980) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Sodium channel protein type 5 subunit alpha

CHEMBL1980

Anchored from Assay target.

Protein identity Sodium channel protein type 5 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	Toxicity
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Sodium channel protein type 5 subunit alpha (CHEMBL1980) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Development of ProTx-II Analogues as Highly Selective Peptide Blockers of Na<sub>v</sub>1.7 for the Treatment of Pain.

Adams GL, Pall PS, Grauer SM, Zhou X, Ballard JE, Vavrek M, Kraus RL, Morissette P, Li N, Colarusso S, Bianchi E, Palani A, Klein R, John CT, Wang D, Tudor M, Nolting AF, Biba M, Nowak T, Makarov AA, Reibarkh M, Buevich AV, Zhong W, Regalado EL, Wang X, Gao Q, Shahripour A, Zhu Y, de Simone D, Frattarelli T, Pasquini NM, Magotti P, Iaccarino R, Li Y, Solly K, Lee KJ, Wang W, Chen F, Zeng H, Wang J, Regan H, Amin RP, Regan CP, Burgey CS, Henze DA, Sun C, Tellers DM.
J Med Chem (2022) 65 : 485 -496
PubMed 34931831 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	3	6.15	6.75

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3318147	—	—	1	6.75
CHEMBL5085021	—	—	1	5.54
CHEMBL5076349	—	—	1	-

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3318147	—	IC50	=	180.0	nM	6.75
CHEMBL5085021	—	IC50	=	2900.0	nM	5.54
CHEMBL5076349	—	IC50	>	15000.0	nM	-