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Assay Detail

CHEMBL4046487

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Binding
Inhibition of human Nav1.5 inactivated state form expressed in HEK293 cells at -60 mV holding potential by by automated patch clamp electrophysiology assay
ChEMBL ↗
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
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

Discovery of non-zwitterionic aryl sulfonamides as Nav1.7 inhibitors with efficacy in preclinical behavioral models and translational measures of nociceptive neuron activation.
Wu YJ, Guernon J, McClure A, Luo G, Rajamani R, Ng A, Easton A, Newton A, Bourin C, Parker D, Mosure K, Barnaby O, Soars MG, Knox RJ, Matchett M, Pieschl R, Herrington J, Chen P, Sivarao DV, Bristow LJ, Meanwell NA, Bronson J, Olson R, Thompson LA, Dzierba C.
Bioorg Med Chem (2017) 25 : 5490 -5505
PubMed 28818462 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 6.57 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4061793 — — 1 8.66
CHEMBL4075332 — — 1 7.43
CHEMBL4094490 — — 1 7.30
CHEMBL4102624 — — 1 7.28
CHEMBL4087220 — — 1 7.13
CHEMBL4072883 — — 1 7.12
CHEMBL4102233 — — 1 7.11
CHEMBL4100176 — — 1 7.03
CHEMBL4104727 — — 1 6.97
CHEMBL4064762 — — 1 6.92
CHEMBL4102647 — — 1 6.90
CHEMBL4073353 — — 1 6.88
CHEMBL4073324 — — 1 6.82
CHEMBL4094879 — — 1 6.82
CHEMBL4064295 — — 1 6.81
CHEMBL4092435 — — 1 6.81
CHEMBL4074392 — — 1 6.79
CHEMBL4071736 — — 1 6.77
CHEMBL4101414 — — 1 6.73
CHEMBL4100208 — — 1 6.72
CHEMBL4076229 — — 1 6.66
CHEMBL4083744 — — 1 6.62
CHEMBL4092463 — — 1 6.62
CHEMBL4082252 — — 1 6.58
CHEMBL4061129 — — 1 6.58
CHEMBL4084685 — — 1 6.55
CHEMBL4092025 — — 1 6.48
CHEMBL4062009 — — 1 6.47
CHEMBL4098747 — — 1 6.46
CHEMBL4068484 — — 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4061793 — IC50 = 2.2 nM 8.66
CHEMBL4075332 — IC50 = 37.0 nM 7.43
CHEMBL4094490 — IC50 = 50.0 nM 7.30
CHEMBL4102624 — IC50 = 52.0 nM 7.28
CHEMBL4087220 — IC50 = 74.0 nM 7.13
CHEMBL4072883 — IC50 = 76.0 nM 7.12
CHEMBL4102233 — IC50 = 77.0 nM 7.11
CHEMBL4100176 — IC50 = 94.0 nM 7.03
CHEMBL4104727 — IC50 = 108.0 nM 6.97
CHEMBL4064762 — IC50 = 120.0 nM 6.92
CHEMBL4102647 — IC50 = 127.0 nM 6.90
CHEMBL4073353 — IC50 = 133.0 nM 6.88
CHEMBL4073324 — IC50 = 150.0 nM 6.82
CHEMBL4094879 — IC50 = 151.0 nM 6.82
CHEMBL4092435 — IC50 = 156.0 nM 6.81
CHEMBL4064295 — IC50 = 156.0 nM 6.81
CHEMBL4074392 — IC50 = 162.0 nM 6.79
CHEMBL4071736 — IC50 = 169.0 nM 6.77
CHEMBL4101414 — IC50 = 188.0 nM 6.73
CHEMBL4100208 — IC50 = 189.0 nM 6.72
CHEMBL4076229 — IC50 = 221.0 nM 6.66
CHEMBL4092463 — IC50 = 237.0 nM 6.62
CHEMBL4083744 — IC50 = 242.0 nM 6.62
CHEMBL4082252 — IC50 = 266.0 nM 6.58
CHEMBL4061129 — IC50 = 260.0 nM 6.58
CHEMBL4084685 — IC50 = 281.0 nM 6.55
CHEMBL4092025 — IC50 = 328.0 nM 6.48
CHEMBL4062009 — IC50 = 336.0 nM 6.47
CHEMBL4098747 — IC50 = 348.0 nM 6.46
CHEMBL4068484 — IC50 = 380.0 nM 6.42
CHEMBL4095822 — IC50 = 407.0 nM 6.39
CHEMBL4084268 — IC50 = 415.0 nM 6.38
CHEMBL4064737 — IC50 = 444.0 nM 6.35
CHEMBL4071860 — IC50 = 614.0 nM 6.21
CHEMBL4084713 — IC50 = 706.0 nM 6.15
CHEMBL4099769 — IC50 = 796.0 nM 6.10
CHEMBL4065798 — IC50 = 874.0 nM 6.06
CHEMBL4089301 — IC50 = 916.0 nM 6.04
CHEMBL4069801 — IC50 = 931.0 nM 6.03
CHEMBL4073933 — IC50 = 1300.0 nM 5.89
CHEMBL4097000 — IC50 = 1400.0 nM 5.85
CHEMBL4086750 — IC50 = 1500.0 nM 5.82
CHEMBL4080500 — IC50 = 3400.0 nM 5.47
CHEMBL4071739 — IC50 = 6400.0 nM 5.19
CHEMBL4065325 — IC50 = 6500.0 nM 5.19