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Assay Detail

CHEMBL4629735

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ADMET
Inhibition of human Nav1.7 at resting state expressed in HEK293 cells at -120 mV holding potential by 10 Hz single pulse protocol based manual patch clamp assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium channel protein type 9 subunit alpha (CHEMBL4296)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Potent, Selective, and State-Dependent NaV1.7 Inhibitors with Robust Oral Efficacy in Pain Models: Structure-Activity Relationship and Optimization of Chroman and Indane Aryl Sulfonamides.
Ramdas V, Talwar R, Kanoje V, Loriya RM, Banerjee M, Patil P, Joshi AA, Datrange L, Das AK, Walke DS, Kalhapure V, Khan T, Gote G, Dhayagude U, Deshpande S, Shaikh J, Chaure G, Pal RR, Parkale S, Suravase S, Bhoskar S, Gupta RV, Kalia A, Yeshodharan R, Azhar M, Daler J, Mali V, Sharma G, Kishore A, Vyawahare R, Agarwal G, Pareek H, Budhe S, Nayak A, Warude D, Gupta PK, Joshi P, Joshi S, Darekar S, Pandey D, Wagh A, Nigade PB, Mehta M, Patil V, Modi D, Pawar S, Verma M, Singh M, Das S, Gundu J, Nemmani K, Bock MG, Sharma S, Bakhle D, Kamboj RK, Palle VP.
J Med Chem (2020) 63 : 6107 -6133
PubMed 32368909 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.25 5.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4637917 1 5.64
CHEMBL4637997 1 5.09
CHEMBL4632819 1 5.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4637917 IC50 = 2280.0 nM 5.64
CHEMBL4637997 IC50 = 8100.0 nM 5.09
CHEMBL4632819 IC50 = 9500.0 nM 5.02