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Found 1486 hits Enz. Inhib. hit(s) with Target = 'Voltage-gated sodium channel subunit Nav1.5' AND taxid = 9606   
Target
(Institution)
LigandTarget
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM145376
PNG
(US8952169, 155)
Show SMILES Fc1cc(OCC23CC4CC(CC(C4)C2)C3)c(cc1C(=O)NS(=O)(=O)N1CCOCC1)C1CC1
Show InChI InChI=1S/C25H33FN2O5S/c26-22-11-23(33-15-25-12-16-7-17(13-25)9-18(8-16)14-25)20(19-1-2-19)10-21(22)24(29)27-34(30,31)28-3-5-32-6-4-28/h10-11,16-19H,1-9,12-15H2,(H,27,29)
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US Patent
n/an/a 14n/an/an/an/an/an/a



Xenon Pharmaceuticals Inc.; Genentech, Inc.

US Patent


Assay Description
Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and all...


US Patent US8952169 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379448
PNG
(CHEMBL2012259)
Show SMILES Fc1ccccc1Cn1ccc2c(OC3CCN(Cc4cscn4)CC3)ncnc12
Show InChI InChI=1S/C22H22FN5OS/c23-20-4-2-1-3-16(20)11-28-10-7-19-21(28)24-14-25-22(19)29-18-5-8-27(9-6-18)12-17-13-30-15-26-17/h1-4,7,10,13-15,18H,5-6,8-9,11-12H2
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n/an/a 20n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379437
PNG
(CHEMBL2012299)
Show SMILES Fc1cccc(Cn2ccc3c(OC4CCN(Cc5ccccn5)CC4)ncnc23)c1F
Show InChI InChI=1S/C24H23F2N5O/c25-21-6-3-4-17(22(21)26)14-31-13-9-20-23(31)28-16-29-24(20)32-19-7-11-30(12-8-19)15-18-5-1-2-10-27-18/h1-6,9-10,13,16,19H,7-8,11-12,14-15H2
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n/an/a 20n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM145389
PNG
(US8952169, 168)
Show SMILES OCCCNS(=O)(=O)NC(=O)c1cc(C2CC2)c(OCC23CC4CC(CC(C4)C2)C3)cc1F
Show InChI InChI=1S/C24H33FN2O5S/c25-21-10-22(32-14-24-11-15-6-16(12-24)8-17(7-15)13-24)19(18-2-3-18)9-20(21)23(29)27-33(30,31)26-4-1-5-28/h9-10,15-18,26,28H,1-8,11-14H2,(H,27,29)
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n/an/a 22n/an/an/an/an/an/a



Xenon Pharmaceuticals Inc.; Genentech, Inc.

US Patent


Assay Description
Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and all...


US Patent US8952169 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM145369
PNG
(US8952169, 148)
Show SMILES Fc1cc(OCC23CC4CC(CC(C4)C2)C3)c(cc1C(=O)NS(=O)(=O)C1CC1)C1CC1
Show InChI InChI=1S/C24H30FNO4S/c25-21-9-22(30-13-24-10-14-5-15(11-24)7-16(6-14)12-24)19(17-1-2-17)8-20(21)23(27)26-31(28,29)18-3-4-18/h8-9,14-18H,1-7,10-13H2,(H,26,27)
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n/an/a 26n/an/an/an/an/an/a



Xenon Pharmaceuticals Inc.; Genentech, Inc.

US Patent


Assay Description
Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and all...


US Patent US8952169 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM154008
PNG
(US9012443, 1)
Show SMILES Cn1nccc1-c1cc(ccc1-c1cccc2cc(ccc12)S(=O)(=O)Nc1ncns1)C(F)(F)F
Show InChI InChI=1S/C23H16F3N5O2S2/c1-31-21(9-10-28-31)20-12-15(23(24,25)26)5-7-19(20)18-4-2-3-14-11-16(6-8-17(14)18)35(32,33)30-22-27-13-29-34-22/h2-13H,1H3,(H,27,29,30)
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n/an/a 30n/an/an/an/an/an/a



Amgen Inc.

US Patent


Assay Description
293 cells stably transfected with Nav 1.5 were recorded in whole cell voltage clamp mode with the PatchXpress automated electrophysiology system acco...


US Patent US9012443 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379436
PNG
(CHEMBL2012298)
Show SMILES Fc1ccccc1Cn1ccc2c(OC3CCN(Cc4ccccn4)CC3)ncnc12
Show InChI InChI=1S/C24H24FN5O/c25-22-7-2-1-5-18(22)15-30-14-10-21-23(30)27-17-28-24(21)31-20-8-12-29(13-9-20)16-19-6-3-4-11-26-19/h1-7,10-11,14,17,20H,8-9,12-13,15-16H2
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n/an/a 30n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50299980
PNG
((R)-1-(Methylsulfonylamino)-3-[2-(4-methoxyphenyl)...)
Show SMILES COc1ccc(CCN2[C@@H](CN(NS(C)(=O)=O)C2=O)c2ccc(OC)cc2)cc1
Show InChI InChI=1S/C20H25N3O5S/c1-27-17-8-4-15(5-9-17)12-13-22-19(16-6-10-18(28-2)11-7-16)14-23(20(22)24)21-29(3,25)26/h4-11,19,21H,12-14H2,1-3H3/t19-/m0/s1
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n/an/a>30n/an/an/an/an/an/a



Wyeth Research

Curated by ChEMBL


Assay Description
Inhibition of Nav1.5 expressed in CHO cells by patch-clamp technique


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50344821
PNG
(10-hydroxymethyl-5-imino-(2S)-12,13-dioxa-4,6-diaz...)
Show SMILES NC1=N[C@H](O)[C@H]2[C@H]3O[C@]4(O)O[C@@H]([C@@H](O)[C@@]2(N1)[C@@H]4O)[C@]3(O)CO
Show InChI InChI=1S/C11H17N3O8/c12-8-13-6(17)2-4-9(19,1-15)5-3(16)10(2,14-8)7(18)11(20,21-4)22-5/h2-7,15-20H,1H2,(H3,12,13,14)/t2-,3-,4-,5+,6-,7+,9+,10-,11+/m1/s1
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n/an/a>30n/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Inhibition of voltage-gated Na channel 1.5 (unknown origin)


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379441
PNG
(CHEMBL2012180)
Show SMILES Fc1cn(Cc2ccccc2)c2ncnc(OC3CCN(Cc4cscn4)CC3)c12
Show InChI InChI=1S/C22H22FN5OS/c23-19-12-28(10-16-4-2-1-3-5-16)21-20(19)22(25-14-24-21)29-18-6-8-27(9-7-18)11-17-13-30-15-26-17/h1-5,12-15,18H,6-11H2
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n/an/a 30n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379459
PNG
(CHEMBL2012274)
Show SMILES Fc1cccc(F)c1Cn1ccc2c(OC3CCN(Cc4cscn4)CC3)ncnc12
Show InChI InChI=1S/C22H21F2N5OS/c23-19-2-1-3-20(24)18(19)11-29-9-6-17-21(29)25-13-26-22(17)30-16-4-7-28(8-5-16)10-15-12-31-14-27-15/h1-3,6,9,12-14,16H,4-5,7-8,10-11H2
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n/an/a 40n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM47141
PNG
(US8952169, 185 | US8952169, 297)
Show SMILES Fc1cc(OCC2CCCCC2)c(cc1C(=O)NS(=O)(=O)N1CCC1)C1CC1
Show InChI InChI=1S/C20H27FN2O4S/c21-18-12-19(27-13-14-5-2-1-3-6-14)16(15-7-8-15)11-17(18)20(24)22-28(25,26)23-9-4-10-23/h11-12,14-15H,1-10,13H2,(H,22,24)
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n/an/a 40n/an/an/an/an/an/a



Xenon Pharmaceuticals Inc.; Genentech, Inc.

US Patent


Assay Description
Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and all...


US Patent US8952169 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379458
PNG
(CHEMBL2012273)
Show SMILES Fc1c(Cn2ccc3c(OC4CCN(Cc5cscn5)CC4)ncnc23)cccc1C(F)(F)F
Show InChI InChI=1S/C23H21F4N5OS/c24-20-15(2-1-3-19(20)23(25,26)27)10-32-9-6-18-21(32)28-13-29-22(18)33-17-4-7-31(8-5-17)11-16-12-34-14-30-16/h1-3,6,9,12-14,17H,4-5,7-8,10-11H2
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n/an/a 40n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379466
PNG
(CHEMBL2012292)
Show SMILES Cc1ccnc(CN2CCC(CC2)Oc2ncnc3n(Cc4ccccc4)ccc23)c1
Show InChI InChI=1S/C25H27N5O/c1-19-7-11-26-21(15-19)17-29-12-8-22(9-13-29)31-25-23-10-14-30(24(23)27-18-28-25)16-20-5-3-2-4-6-20/h2-7,10-11,14-15,18,22H,8-9,12-13,16-17H2,1H3
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n/an/a 40n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379457
PNG
(CHEMBL2012272)
Show SMILES Fc1c(Cl)cccc1Cn1ccc2c(OC3CCN(Cc4cscn4)CC3)ncnc12
Show InChI InChI=1S/C22H21ClFN5OS/c23-19-3-1-2-15(20(19)24)10-29-9-6-18-21(29)25-13-26-22(18)30-17-4-7-28(8-5-17)11-16-12-31-14-27-16/h1-3,6,9,12-14,17H,4-5,7-8,10-11H2
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n/an/a 50n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379440
PNG
(CHEMBL2012179)
Show SMILES Cc1cn(Cc2ccccc2)c2ncnc(OC3CCN(Cc4cscn4)CC3)c12
Show InChI InChI=1S/C23H25N5OS/c1-17-11-28(12-18-5-3-2-4-6-18)22-21(17)23(25-15-24-22)29-20-7-9-27(10-8-20)13-19-14-30-16-26-19/h2-6,11,14-16,20H,7-10,12-13H2,1H3
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n/an/a 50n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM145285
PNG
(US8952169, 64)
Show SMILES Fc1cc(OCC23CC4CC(CC(C4)C2)C3)c(cc1C(=O)NS(=O)(=O)N1CCC1)C1CC1
Show InChI InChI=1S/C24H31FN2O4S/c25-21-10-22(31-14-24-11-15-6-16(12-24)8-17(7-15)13-24)19(18-2-3-18)9-20(21)23(28)26-32(29,30)27-4-1-5-27/h9-10,15-18H,1-8,11-14H2,(H,26,28)
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n/an/a 51.5n/an/an/an/an/an/a



Xenon Pharmaceuticals Inc.; Genentech, Inc.

US Patent


Assay Description
Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and all...


US Patent US8952169 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50173375
PNG
(CHEMBL3810248)
Show SMILES C[Si](C)(C)c1ccc(cc1)-c1ccc2nnc(n2c1)C(F)(F)F
Show InChI InChI=1S/C16H16F3N3Si/c1-23(2,3)13-7-4-11(5-8-13)12-6-9-14-20-21-15(16(17,18)19)22(14)10-12/h4-10H,1-3H3
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n/an/a 59n/an/an/an/an/an/a



Gilead Sciences Inc.

Curated by ChEMBL


Assay Description
Inhibition of Nav 1.5 (unknown origin) assessed as reduction in late channel current


Bioorg Med Chem Lett 26: 3202-6 (2016)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379452
PNG
(CHEMBL2012266)
Show SMILES Cc1cccc(Cn2ccc3c(OC4CCN(Cc5cscn5)CC4)ncnc23)c1
Show InChI InChI=1S/C23H25N5OS/c1-17-3-2-4-18(11-17)12-28-10-7-21-22(28)24-15-25-23(21)29-20-5-8-27(9-6-20)13-19-14-30-16-26-19/h2-4,7,10-11,14-16,20H,5-6,8-9,12-13H2,1H3
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n/an/a 60n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379465
PNG
(CHEMBL2012291)
Show SMILES Cc1ccc(CN2CCC(CC2)Oc2ncnc3n(Cc4ccccc4)ccc23)nc1
Show InChI InChI=1S/C25H27N5O/c1-19-7-8-21(26-15-19)17-29-12-9-22(10-13-29)31-25-23-11-14-30(24(23)27-18-28-25)16-20-5-3-2-4-6-20/h2-8,11,14-15,18,22H,9-10,12-13,16-17H2,1H3
PDB

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n/an/a 60n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM145268
PNG
(US8952169, 47)
Show SMILES OC1CN(C1)S(=O)(=O)NC(=O)c1cc(C2CC2)c(OCC23CC4CC(CC(C4)C2)C3)cc1F
Show InChI InChI=1S/C24H31FN2O5S/c25-21-7-22(32-13-24-8-14-3-15(9-24)5-16(4-14)10-24)19(17-1-2-17)6-20(21)23(29)26-33(30,31)27-11-18(28)12-27/h6-7,14-18,28H,1-5,8-13H2,(H,26,29)
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n/an/a 60.6n/an/an/an/an/an/a



Xenon Pharmaceuticals Inc.; Genentech, Inc.

US Patent


Assay Description
Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and all...


US Patent US8952169 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379456
PNG
(CHEMBL2012271)
Show SMILES Fc1cccc(Cn2ccc3c(OC4CCN(Cc5cscn5)CC4)ncnc23)c1F
Show InChI InChI=1S/C22H21F2N5OS/c23-19-3-1-2-15(20(19)24)10-29-9-6-18-21(29)25-13-26-22(18)30-17-4-7-28(8-5-17)11-16-12-31-14-27-16/h1-3,6,9,12-14,17H,4-5,7-8,10-11H2
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n/an/a 70n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379462
PNG
(CHEMBL2012285)
Show SMILES Cc1nc(CN2CCC(CC2)Oc2ncnc3n(Cc4ccccc4)ccc23)cs1
Show InChI InChI=1S/C23H25N5OS/c1-17-26-19(15-30-17)14-27-10-7-20(8-11-27)29-23-21-9-12-28(22(21)24-16-25-23)13-18-5-3-2-4-6-18/h2-6,9,12,15-16,20H,7-8,10-11,13-14H2,1H3
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n/an/a 80n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379438
PNG
(CHEMBL2012300)
Show SMILES Fc1c(Cl)cccc1Cn1ccc2c(OC3CCN(Cc4ccccn4)CC3)ncnc12
Show InChI InChI=1S/C24H23ClFN5O/c25-21-6-3-4-17(22(21)26)14-31-13-9-20-23(31)28-16-29-24(20)32-19-7-11-30(12-8-19)15-18-5-1-2-10-27-18/h1-6,9-10,13,16,19H,7-8,11-12,14-15H2
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n/an/a 80n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379442
PNG
(CHEMBL2012181)
Show SMILES Clc1cn(Cc2ccccc2)c2ncnc(OC3CCN(Cc4cscn4)CC3)c12
Show InChI InChI=1S/C22H22ClN5OS/c23-19-12-28(10-16-4-2-1-3-5-16)21-20(19)22(25-14-24-21)29-18-6-8-27(9-7-18)11-17-13-30-15-26-17/h1-5,12-15,18H,6-11H2
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n/an/a 80n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379434
PNG
(CHEMBL2012296)
Show SMILES Fc1cccnc1CN1CCC(CC1)Oc1ncnc2n(Cc3ccccc3)ccc12
Show InChI InChI=1S/C24H24FN5O/c25-21-7-4-11-26-22(21)16-29-12-8-19(9-13-29)31-24-20-10-14-30(23(20)27-17-28-24)15-18-5-2-1-3-6-18/h1-7,10-11,14,17,19H,8-9,12-13,15-16H2
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n/an/a 90n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50051073
PNG
(CHEMBL3318132)
Show SMILES CSCC[C@@H]1NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@H]3CSSC[C@H](NC(=O)[C@@H](NC1=O)C(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c4ccccc14)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC3=O)C(=O)N2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(O)=O
Show InChI InChI=1/C168H250N46O41S8/c1-86(2)66-117-151(239)203-120(70-92-75-183-102-35-15-11-31-97(92)102)154(242)209-126(159(247)193-106(39-19-24-58-170)141(229)188-105(38-18-23-57-169)140(228)189-107(40-20-25-59-171)143(231)200-118(67-87(3)4)152(240)205-123(166(254)255)72-94-77-185-104-37-17-13-33-99(94)104)81-259-261-83-128-163(251)210-127-82-260-258-80-125(207-138(226)100(174)68-90-45-47-95(217)48-46-90)158(246)197-113(49-52-131(175)218)147(235)191-108(41-21-26-60-172)144(232)201-119(69-91-74-182-101-34-14-10-30-96(91)101)153(241)198-116(56-65-257-9)149(237)202-121(71-93-76-184-103-36-16-12-32-98(93)103)156(244)214-137(89(7)216)165(253)212-130(162(250)204-122(73-135(224)225)155(243)206-124(79-215)157(245)196-114(51-54-134(222)223)148(236)192-110(43-28-62-180-167(176)177)142(230)190-109(146(234)208-128)42-22-27-61-173)85-263-262-84-129(161(249)194-111(145(233)199-117)44-29-63-181-168(178)179)211-164(252)136(88(5)6)213-150(238)115(55-64-256-8)187-132(219)78-186-139(227)112(195-160(127)248)50-53-133(220)221/h10-17,30-37,45-48,74-77,86-89,100,105-130,136-137,182-185,215-217H,18-29,38-44,49-73,78-85,169-174H2,1-9H3,(H2,175,218)(H,186,227)(H,187,219)(H,188,229)(H,189,228)(H,190,230)(H,191,235)(H,192,236)(H,193,247)(H,194,249)(H,195,248)(H,196,245)(H,197,246)(H,198,241)(H,199,233)(H,200,231)(H,201,232)(H,202,237)(H,203,239)(H,204,250)(H,205,240)(H,206,243)(H,207,226)(H,208,234)(H,209,242)(H,210,251)(H,211,252)(H,212,253)(H,213,238)(H,214,244)(H,220,221)(H,222,223)(H,224,225)(H,254,255)(H4,176,177,180)(H4,178,179,181)/t89-,100+,105+,106+,107+,108+,109+,110+,111+,112+,113+,114+,115+,116+,117+,118+,119+,120+,121+,122+,123+,124+,125+,126+,127+,128+,129+,130+,136+,137+/s2
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n/an/a 90n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.5 at -140 mV holding potential by whole-cell patch clamp assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM145470
PNG
(US8952169, 249)
Show SMILES Fc1cc(OCC2(CCCC2)C(F)(F)F)c(cc1C(=O)NS(=O)(=O)N1CCC1)C1CC1
Show InChI InChI=1S/C20H24F4N2O4S/c21-16-11-17(30-12-19(20(22,23)24)6-1-2-7-19)14(13-4-5-13)10-15(16)18(27)25-31(28,29)26-8-3-9-26/h10-11,13H,1-9,12H2,(H,25,27)
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n/an/a 90n/an/an/an/an/an/a



Xenon Pharmaceuticals Inc.; Genentech, Inc.

US Patent


Assay Description
Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and all...


US Patent US8952169 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379464
PNG
(CHEMBL2012290)
Show SMILES Cc1cccc(CN2CCC(CC2)Oc2ncnc3n(Cc4ccccc4)ccc23)n1
Show InChI InChI=1S/C25H27N5O/c1-19-6-5-9-21(28-19)17-29-13-10-22(11-14-29)31-25-23-12-15-30(24(23)26-18-27-25)16-20-7-3-2-4-8-20/h2-9,12,15,18,22H,10-11,13-14,16-17H2,1H3
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n/an/a 90n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50270707
PNG
(CHEMBL486495 | [5-(4-tert-Butylphenyl)furan-2-yl]-...)
Show SMILES CC(C)(C)c1ccc(cc1)-c1ccc(o1)C(=O)N1CCN(CC1)C1CCCCC1
Show InChI InChI=1S/C25H34N2O2/c1-25(2,3)20-11-9-19(10-12-20)22-13-14-23(29-22)24(28)27-17-15-26(16-18-27)21-7-5-4-6-8-21/h9-14,21H,4-8,15-18H2,1-3H3
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n/an/a 100n/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
Inhibition of human recombinant Nav1.5 channel expressed in HEK293 cells by whole cell voltage clamp technique


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM145270
PNG
(US8952169, 49)
Show SMILES COCCS(=O)(=O)NC(=O)c1cc(C2CC2)c(OCC23CC4CC(CC(C4)C2)C3)cc1F
Show InChI InChI=1S/C24H32FNO5S/c1-30-4-5-32(28,29)26-23(27)20-9-19(18-2-3-18)22(10-21(20)25)31-14-24-11-15-6-16(12-24)8-17(7-15)13-24/h9-10,15-18H,2-8,11-14H2,1H3,(H,26,27)
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n/an/a 101n/an/an/an/an/an/a



Xenon Pharmaceuticals Inc.; Genentech, Inc.

US Patent


Assay Description
Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and all...


US Patent US8952169 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50173495
PNG
(CHEMBL3809404)
Show SMILES FC(F)(F)Oc1ccc(cc1)-c1ccc2cnc(n2c1)C(F)(F)F
Show InChI InChI=1S/C15H8F6N2O/c16-14(17,18)13-22-7-11-4-1-10(8-23(11)13)9-2-5-12(6-3-9)24-15(19,20)21/h1-8H
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n/an/a 102n/an/an/an/an/an/a



Gilead Sciences Inc.

Curated by ChEMBL


Assay Description
Inhibition of Nav 1.5 (unknown origin) assessed as reduction in late channel current


Bioorg Med Chem Lett 26: 3202-6 (2016)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM145368
PNG
(US8952169, 147)
Show SMILES O[C@H]1CCN(C1)S(=O)(=O)NC(=O)c1cc(C2CC2)c(OCC23CC4CC(CC(C4)C2)C3)cc1F
Show InChI InChI=1/C25H33FN2O5S/c26-22-9-23(33-14-25-10-15-5-16(11-25)7-17(6-15)12-25)20(18-1-2-18)8-21(22)24(30)27-34(31,32)28-4-3-19(29)13-28/h8-9,15-19,29H,1-7,10-14H2,(H,27,30)/t15?,16?,17?,19-,25?/s2
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n/an/a 110n/an/an/an/an/an/a



Xenon Pharmaceuticals Inc.; Genentech, Inc.

US Patent


Assay Description
Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and all...


US Patent US8952169 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379449
PNG
(CHEMBL2012262)
Show SMILES Clc1ccccc1Cn1ccc2c(OC3CCN(Cc4cscn4)CC3)ncnc12
Show InChI InChI=1S/C22H22ClN5OS/c23-20-4-2-1-3-16(20)11-28-10-7-19-21(28)24-14-25-22(19)29-18-5-8-27(9-6-18)12-17-13-30-15-26-17/h1-4,7,10,13-15,18H,5-6,8-9,11-12H2
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n/an/a 110n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379469
PNG
(CHEMBL2012295)
Show SMILES Fc1ccc(CN2CCC(CC2)Oc2ncnc3n(Cc4ccccc4)ccc23)nc1
Show InChI InChI=1S/C24H24FN5O/c25-19-6-7-20(26-14-19)16-29-11-8-21(9-12-29)31-24-22-10-13-30(23(22)27-17-28-24)15-18-4-2-1-3-5-18/h1-7,10,13-14,17,21H,8-9,11-12,15-16H2
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n/an/a 110n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50103584
PNG
(CHEMBL3337595)
Show SMILES COc1ccc-2c(NC3(CCN(CC3)C(=O)c3ccc(OC)c(c3)N3CCCC3)c3cccn-23)c1
Show InChI InChI=1S/C28H32N4O3/c1-34-21-8-9-23-22(19-21)29-28(26-6-5-15-32(23)26)11-16-31(17-12-28)27(33)20-7-10-25(35-2)24(18-20)30-13-3-4-14-30/h5-10,15,18-19,29H,3-4,11-14,16-17H2,1-2H3
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n/an/a 118n/an/an/an/an/an/a



Merck Research Laboratory

Curated by ChEMBL


Assay Description
Inhibition of human Nav1.5 expressed in HEK293 cells after 60 mins by FLIPR assay


Bioorg Med Chem Lett 24: 4958-62 (2014)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379454
PNG
(CHEMBL2012268)
Show SMILES FC(F)(F)c1ccccc1Cn1ccc2c(OC3CCN(Cc4cscn4)CC3)ncnc12
Show InChI InChI=1S/C23H22F3N5OS/c24-23(25,26)20-4-2-1-3-16(20)11-31-10-7-19-21(31)27-14-28-22(19)32-18-5-8-30(9-6-18)12-17-13-33-15-29-17/h1-4,7,10,13-15,18H,5-6,8-9,11-12H2
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n/an/a 120n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379431
PNG
(CHEMBL2012178)
Show SMILES Cc1c(C)c2c(OC3CCN(Cc4cscn4)CC3)ncnc2n1Cc1ccccc1
Show InChI InChI=1S/C24H27N5OS/c1-17-18(2)29(12-19-6-4-3-5-7-19)23-22(17)24(26-15-25-23)30-21-8-10-28(11-9-21)13-20-14-31-16-27-20/h3-7,14-16,21H,8-13H2,1-2H3
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n/an/a 120n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50173487
PNG
(CHEMBL3809360)
Show SMILES Cc1cc(OC(F)(F)F)ccc1-c1ccc2nnc(n2c1)C(F)(F)F
Show InChI InChI=1S/C15H9F6N3O/c1-8-6-10(25-15(19,20)21)3-4-11(8)9-2-5-12-22-23-13(14(16,17)18)24(12)7-9/h2-7H,1H3
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n/an/a 123n/an/an/an/an/an/a



Gilead Sciences Inc.

Curated by ChEMBL


Assay Description
Inhibition of Nav 1.5 (unknown origin) assessed as reduction in late channel current


Bioorg Med Chem Lett 26: 3202-6 (2016)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM145481
PNG
(US8952169, 262)
Show SMILES Fc1cc(OCC23CC4CC(C2)C(F)(F)C(C4)C3)c(cc1C(=O)NS(=O)(=O)C1CC1)C1CC1
Show InChI InChI=1/C24H28F3NO4S/c25-20-8-21(32-12-23-9-13-5-15(10-23)24(26,27)16(6-13)11-23)18(14-1-2-14)7-19(20)22(29)28-33(30,31)17-3-4-17/h7-8,13-17H,1-6,9-12H2,(H,28,29)
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n/an/a 130n/an/an/an/an/an/a



Xenon Pharmaceuticals Inc.; Genentech, Inc.

US Patent


Assay Description
Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and all...


US Patent US8952169 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM145412
PNG
(US8952169, 191)
Show SMILES Fc1cc(OCC2C3CC4CC(C3)CC2C4)c(cc1C(=O)NS(=O)(=O)N1CCC1)C1CC1
Show InChI InChI=1S/C24H31FN2O4S/c25-22-12-23(31-13-21-17-7-14-6-15(9-17)10-18(21)8-14)19(16-2-3-16)11-20(22)24(28)26-32(29,30)27-4-1-5-27/h11-12,14-18,21H,1-10,13H2,(H,26,28)
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n/an/a 130n/an/an/an/an/an/a



Xenon Pharmaceuticals Inc.; Genentech, Inc.

US Patent


Assay Description
Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and all...


US Patent US8952169 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379447
PNG
(CHEMBL2012250)
Show SMILES CC1(C)C(=O)N(Cc2ccccc2)c2ncnc(OC3CCN(Cc4cscn4)CC3)c12
Show InChI InChI=1S/C24H27N5O2S/c1-24(2)20-21(29(23(24)30)12-17-6-4-3-5-7-17)25-15-26-22(20)31-19-8-10-28(11-9-19)13-18-14-32-16-27-18/h3-7,14-16,19H,8-13H2,1-2H3
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n/an/a 130n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM145407
PNG
(US8952169, 186)
Show SMILES COCCS(=O)(=O)NC(=O)c1cc(C2CC2)c(OCC2CCCCC2)cc1F
Show InChI InChI=1S/C20H28FNO5S/c1-26-9-10-28(24,25)22-20(23)17-11-16(15-7-8-15)19(12-18(17)21)27-13-14-5-3-2-4-6-14/h11-12,14-15H,2-10,13H2,1H3,(H,22,23)
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n/an/a 140n/an/an/an/an/an/a



Xenon Pharmaceuticals Inc.; Genentech, Inc.

US Patent


Assay Description
Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and all...


US Patent US8952169 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379451
PNG
(CHEMBL2012265)
Show SMILES Cc1ccccc1Cn1ccc2c(OC3CCN(Cc4cscn4)CC3)ncnc12
Show InChI InChI=1S/C23H25N5OS/c1-17-4-2-3-5-18(17)12-28-11-8-21-22(28)24-15-25-23(21)29-20-6-9-27(10-7-20)13-19-14-30-16-26-19/h2-5,8,11,14-16,20H,6-7,9-10,12-13H2,1H3
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n/an/a 140n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM145390
PNG
(US8952169, 169)
Show SMILES COC1CN(C1)S(=O)(=O)NC(=O)c1cc(C2CC2)c(OCC23CC4CC(CC(C4)C2)C3)cc1F
Show InChI InChI=1S/C25H33FN2O5S/c1-32-19-12-28(13-19)34(30,31)27-24(29)21-7-20(18-2-3-18)23(8-22(21)26)33-14-25-9-15-4-16(10-25)6-17(5-15)11-25/h7-8,15-19H,2-6,9-14H2,1H3,(H,27,29)
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n/an/a 144n/an/an/an/an/an/a



Xenon Pharmaceuticals Inc.; Genentech, Inc.

US Patent


Assay Description
Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and all...


US Patent US8952169 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379467
PNG
(CHEMBL2012293)
Show SMILES Cc1cccnc1CN1CCC(CC1)Oc1ncnc2n(Cc3ccccc3)ccc12
Show InChI InChI=1S/C25H27N5O/c1-19-6-5-12-26-23(19)17-29-13-9-21(10-14-29)31-25-22-11-15-30(24(22)27-18-28-25)16-20-7-3-2-4-8-20/h2-8,11-12,15,18,21H,9-10,13-14,16-17H2,1H3
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n/an/a 150n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM145281
PNG
(US8952169, 60)
Show SMILES CS(=O)(=O)NC(=O)c1cc(C2CC2)c(OCC23CC4CC(CC(C4)C2)C3)cc1F
Show InChI InChI=1S/C22H28FNO4S/c1-29(26,27)24-21(25)18-7-17(16-2-3-16)20(8-19(18)23)28-12-22-9-13-4-14(10-22)6-15(5-13)11-22/h7-8,13-16H,2-6,9-12H2,1H3,(H,24,25)
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n/an/a 159n/an/an/an/an/an/a



Xenon Pharmaceuticals Inc.; Genentech, Inc.

US Patent


Assay Description
Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and all...


US Patent US8952169 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM50379463
PNG
(CHEMBL2012287)
Show SMILES C(N1CCC(CC1)Oc1ncnc2n(Cc3ccccc3)ccc12)c1ccccn1
Show InChI InChI=1S/C24H25N5O/c1-2-6-19(7-3-1)16-29-15-11-22-23(29)26-18-27-24(22)30-21-9-13-28(14-10-21)17-20-8-4-5-12-25-20/h1-8,11-12,15,18,21H,9-10,13-14,16-17H2
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n/an/a 160n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human NaV1.5 channel by patchXpress assay


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM145641
PNG
(US8952169, 446)
Show SMILES Fc1cc(OCC2(CCCCC2)C(F)(F)F)c(cc1C(=O)NS(=O)(=O)C1CC1)C1CC1
Show InChI InChI=1S/C21H25F4NO4S/c22-17-11-18(30-12-20(21(23,24)25)8-2-1-3-9-20)15(13-4-5-13)10-16(17)19(27)26-31(28,29)14-6-7-14/h10-11,13-14H,1-9,12H2,(H,26,27)
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n/an/a 160n/an/an/an/an/an/a



Xenon Pharmaceuticals Inc.; Genentech, Inc.

US Patent


Assay Description
Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and all...


US Patent US8952169 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit Nav1.5


(Homo sapiens (Human))
BDBM145485
PNG
(US8952169, 269)
Show SMILES Fc1cc(OCC23CC2CCCC3)c(cc1C(=O)NS(=O)(=O)N1CCC1)C1CC1
Show InChI InChI=1/C21H27FN2O4S/c22-18-11-19(28-13-21-7-2-1-4-15(21)12-21)16(14-5-6-14)10-17(18)20(25)23-29(26,27)24-8-3-9-24/h10-11,14-15H,1-9,12-13H2,(H,23,25)
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n/an/a 160n/an/an/an/an/an/a



Xenon Pharmaceuticals Inc.; Genentech, Inc.

US Patent


Assay Description
Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and all...


US Patent US8952169 (2015)

More data for this
Ligand-Target Pair
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