Assay Detail

CHEMBL5049645

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Toxicity

Inhibition of NET (unknown origin)

ChEMBL ↗

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Target

Sodium-dependent noradrenaline transporter (CHEMBL222) ↗

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Sodium-dependent noradrenaline transporter (CHEMBL222) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Sodium-dependent noradrenaline transporter

CHEMBL222

Anchored from Assay target.

Protein identity Sodium-dependent noradrenaline transporter

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-dependent noradrenaline transporter (CHEMBL222) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of (<i>S</i>)-1-((2',6-Bis(difluoromethyl)-[2,4'-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine (BMS-986176/LX-9211): A Highly Selective, CNS Penetrable, and Orally Active Adaptor Protein-2 Associated Kinase 1 Inhibitor in Clinical Trials for the Treatment of Neuropathic Pain.

Luo G, Chen L, Kostich WA, Hamman B, Allen J, Easton A, Bourin C, Gulianello M, Lippy J, Nara S, Maishal TK, Thiyagarajan K, Jalagam P, Pattipati SN, Dandapani K, Dokania M, Vattikundala P, Sharma V, Elavazhagan S, Verma MK, Das ML, Wagh S, Balakrishnan A, Johnson BM, Santone KS, Thalody G, Denton R, Saminathan H, Holenarsipur VK, Kumar A, Rao A, Putlur SP, Sarvasiddhi SK, Shankar G, Louis JV, Ramarao M, Conway CM, Li YW, Pieschl R, Tian Y, Hong Y, Ditta J, Mathur A, Li J, Smith D, Pawluczyk J, Sun D, Yip S, Wu DR, Vetrichelvan M, Gupta A, Wilson A, Gopinathan S, Wason S, Bristow L, Albright CF, Bronson JJ, Macor JE, Dzierba CD.
J Med Chem (2022) 65 : 4457 -4480
PubMed 35257579 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	6.41	6.41

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL5089410	PILAVAPADIN	2.0	1	6.41

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL5089410	PILAVAPADIN	IC50	=	390.0	nM	6.41