Assay Detail

CHEMBL5055698

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Binding

Inhibition of full length human Nav1.1 expressed in HEK cells by whole cell voltage clamp analysis

ChEMBL ↗

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Target

Sodium channel protein type 1 subunit alpha (CHEMBL1845) ↗

Open DB target context

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Sodium channel protein type 1 subunit alpha (CHEMBL1845) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Sodium channel protein type 1 subunit alpha

CHEMBL1845

Anchored from Assay target.

Protein identity Sodium channel protein type 1 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	Homo sapiens
Cell Type	HEK
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Sodium channel protein type 1 subunit alpha (CHEMBL1845) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of Acyl-sulfonamide Na<sub>v</sub>1.7 Inhibitors GDC-0276 and GDC-0310.

Safina BS, McKerrall SJ, Sun S, Chen CA, Chowdhury S, Jia Q, Li J, Zenova AY, Andrez JC, Bankar G, Bergeron P, Chang JH, Chang E, Chen J, Dean R, Decker SM, DiPasquale A, Focken T, Hemeon I, Khakh K, Kim A, Kwan R, Lindgren A, Lin S, Maher J, Mezeyova J, Misner D, Nelkenbrecher K, Pang J, Reese R, Shields SD, Sojo L, Sheng T, Verschoof H, Waldbrook M, Wilson MS, Xie Z, Young C, Zabka TS, Hackos DH, Ortwine DF, White AD, Johnson JP, Robinette CL, Dehnhardt CM, Cohen CJ, Sutherlin DP.
J Med Chem (2021) 64 : 2953 -2966
PubMed 33682420 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	7.34	7.97

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3657855	—	—	1	7.97
CHEMBL5094715	—	—	1	6.70

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3657855	—	IC50	=	10.6	nM	7.97
CHEMBL5094715	—	IC50	=	202.0	nM	6.70