Assay Detail

CHEMBL4040150

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Binding

Inhibition of dog NaV1.7 expressed in HEK cells assessed as half inactivation potential at -120 mV holding potential by automated patch clamp method

ChEMBL ↗

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Target

Unchecked (CHEMBL612545) ↗

Open DB target context

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Unchecked (CHEMBL612545) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Unchecked

CHEMBL612545

Anchored from Assay target.

Protein identity Unchecked

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	Canis lupus familiaris
Confidence	0 — Uncurated / Unknown
Curated By	Autocuration

Target

Unchecked (CHEMBL612545) ↗

Type

UNCHECKED

Publication

Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of NaV1.7.

Swain NA, Batchelor D, Beaudoin S, Bechle BM, Bradley PA, Brown AD, Brown B, Butcher KJ, Butt RP, Chapman ML, Denton S, Ellis D, Galan SRG, Gaulier SM, Greener BS, de Groot MJ, Glossop MS, Gurrell IK, Hannam J, Johnson MS, Lin Z, Markworth CJ, Marron BE, Millan DS, Nakagawa S, Pike A, Printzenhoff D, Rawson DJ, Ransley SJ, Reister SM, Sasaki K, Storer RI, Stupple PA, West CW.
J Med Chem (2017) 60 : 7029 -7042
PubMed 28682065 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	3	7.09	7.80

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL2325014	PF-05089771	2.0	1	7.80
CHEMBL2324776	PF-05186462	1.0	1	6.88
CHEMBL2324748	PF-05150122	1.0	1	6.58

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL2325014	PF-05089771	IC50	=	16.0	nM	7.80
CHEMBL2324776	PF-05186462	IC50	=	132.0	nM	6.88
CHEMBL2324748	PF-05150122	IC50	=	263.0	nM	6.58