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PubMed code 28629594

Compile data set for download or QSAR
Found 55 hits of Enzyme Inhibition Constant Data   
Target/Host
(Institution)		LigandTarget/Host
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
Sodium channel protein type 9 subunit alpha


(Homo sapiens (Human))		BDBM231465
PNG
(US9346798, 212)
Show SMILES FC(F)(F)c1ccc(N2CCOc3cc(c(Cl)cc23)S(=O)(=O)Nc2nccs2)c(c1)C#N
Show InChI InChI=1S/C19H12ClF3N4O3S2/c20-13-8-15-16(9-17(13)32(28,29)26-18-25-3-6-31-18)30-5-4-27(15)14-2-1-12(19(21,22)23)7-11(14)10-24/h1-3,6-9H,4-5H2,(H,25,26)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Displacement of (P)-1-(30-chloro-2-fluoro-5,50-dimethoxy-[1,10biphenyl]-4-yl)-N-(isoxazol-3-yl)-2-oxo-1,2-dihydroquinoline-6-sulfonamide[50-methoxy-C...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Homo sapiens (Human))		BDBM231284
PNG
(US9346798, 31)
Show SMILES FC(F)(F)c1ccc(N2CCOc3cc(ccc23)S(=O)(=O)Nc2ncns2)c(c1)C#N
Show InChI InChI=1S/C18H12F3N5O3S2/c19-18(20,21)12-1-3-14(11(7-12)9-22)26-5-6-29-16-8-13(2-4-15(16)26)31(27,28)25-17-23-10-24-30-17/h1-4,7-8,10H,5-6H2,(H,23,24,25)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Displacement of (P)-1-(30-chloro-2-fluoro-5,50-dimethoxy-[1,10biphenyl]-4-yl)-N-(isoxazol-3-yl)-2-oxo-1,2-dihydroquinoline-6-sulfonamide[50-methoxy-C...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Homo sapiens (Human))		BDBM50024250
PNG
(CHEMBL2324000)
Show SMILES Cn1nccc1-c1ccccc1Oc1ccc(cc1C#N)S(=O)(=O)Nc1nccs1
Show InChI InChI=1S/C20H15N5O3S2/c1-25-17(8-9-23-25)16-4-2-3-5-19(16)28-18-7-6-15(12-14(18)13-21)30(26,27)24-20-22-10-11-29-20/h2-12H,1H3,(H,22,24)
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n/an/a 28n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.7

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Homo sapiens (Human))		BDBM154055
PNG
(US9012443, 48)
Show SMILES FC(F)(F)c1ccc(c(c1)C1=CCNCC1)-c1cccc2cc(ccc12)S(=O)(=O)Nc1ccncn1 |t:11|
Show InChI InChI=1S/C26H21F3N4O2S/c27-26(28,29)19-4-6-23(24(15-19)17-8-11-30-12-9-17)22-3-1-2-18-14-20(5-7-21(18)22)36(34,35)33-25-10-13-31-16-32-25/h1-8,10,13-16,30H,9,11-12H2,(H,31,32,33)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Displacement of (P)-1-(30-chloro-2-fluoro-5,50-dimethoxy-[1,10biphenyl]-4-yl)-N-(isoxazol-3-yl)-2-oxo-1,2-dihydroquinoline-6-sulfonamide[50-methoxy-C...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Homo sapiens (Human))		BDBM231468
PNG
(US9346798, 215)
Show SMILES Fc1cc2N(CCOc2cc1S(=O)(=O)Nc1nccs1)c1ccc(cc1C#N)C(F)(F)F
Show InChI InChI=1S/C19H12F4N4O3S2/c20-13-8-15-16(9-17(13)32(28,29)26-18-25-3-6-31-18)30-5-4-27(15)14-2-1-12(19(21,22)23)7-11(14)10-24/h1-3,6-9H,4-5H2,(H,25,26)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Displacement of (P)-1-(30-chloro-2-fluoro-5,50-dimethoxy-[1,10biphenyl]-4-yl)-N-(isoxazol-3-yl)-2-oxo-1,2-dihydroquinoline-6-sulfonamide[50-methoxy-C...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Rattus norvegicus)		BDBM231465
PNG
(US9346798, 212)
Show SMILES FC(F)(F)c1ccc(N2CCOc3cc(c(Cl)cc23)S(=O)(=O)Nc2nccs2)c(c1)C#N
Show InChI InChI=1S/C19H12ClF3N4O3S2/c20-13-8-15-16(9-17(13)32(28,29)26-18-25-3-6-31-18)30-5-4-27(15)14-2-1-12(19(21,22)23)7-11(14)10-24/h1-3,6-9H,4-5H2,(H,25,26)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of rat NaV1.7 by cell based whole cell voltage clamp method

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Mus musculus)		BDBM231468
PNG
(US9346798, 215)
Show SMILES Fc1cc2N(CCOc2cc1S(=O)(=O)Nc1nccs1)c1ccc(cc1C#N)C(F)(F)F
Show InChI InChI=1S/C19H12F4N4O3S2/c20-13-8-15-16(9-17(13)32(28,29)26-18-25-3-6-31-18)30-5-4-27(15)14-2-1-12(19(21,22)23)7-11(14)10-24/h1-3,6-9H,4-5H2,(H,25,26)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of mouse NaV1.7 by whole cell voltage clamp method

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Rattus norvegicus)		BDBM231468
PNG
(US9346798, 215)
Show SMILES Fc1cc2N(CCOc2cc1S(=O)(=O)Nc1nccs1)c1ccc(cc1C#N)C(F)(F)F
Show InChI InChI=1S/C19H12F4N4O3S2/c20-13-8-15-16(9-17(13)32(28,29)26-18-25-3-6-31-18)30-5-4-27(15)14-2-1-12(19(21,22)23)7-11(14)10-24/h1-3,6-9H,4-5H2,(H,25,26)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of rat NaV1.7 by cell based whole cell voltage clamp method

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Homo sapiens (Human))		BDBM231284
PNG
(US9346798, 31)
Show SMILES FC(F)(F)c1ccc(N2CCOc3cc(ccc23)S(=O)(=O)Nc2ncns2)c(c1)C#N
Show InChI InChI=1S/C18H12F3N5O3S2/c19-18(20,21)12-1-3-14(11(7-12)9-22)26-5-6-29-16-8-13(2-4-15(16)26)31(27,28)25-17-23-10-24-30-17/h1-4,7-8,10H,5-6H2,(H,23,24,25)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.7 expressed in HEK293 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Homo sapiens (Human))		BDBM154055
PNG
(US9012443, 48)
Show SMILES FC(F)(F)c1ccc(c(c1)C1=CCNCC1)-c1cccc2cc(ccc12)S(=O)(=O)Nc1ccncn1 |t:11|
Show InChI InChI=1S/C26H21F3N4O2S/c27-26(28,29)19-4-6-23(24(15-19)17-8-11-30-12-9-17)22-3-1-2-18-14-20(5-7-21(18)22)36(34,35)33-25-10-13-31-16-32-25/h1-8,10,13-16,30H,9,11-12H2,(H,31,32,33)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.7 expressed in HEK293 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Mus musculus)		BDBM231465
PNG
(US9346798, 212)
Show SMILES FC(F)(F)c1ccc(N2CCOc3cc(c(Cl)cc23)S(=O)(=O)Nc2nccs2)c(c1)C#N
Show InChI InChI=1S/C19H12ClF3N4O3S2/c20-13-8-15-16(9-17(13)32(28,29)26-18-25-3-6-31-18)30-5-4-27(15)14-2-1-12(19(21,22)23)7-11(14)10-24/h1-3,6-9H,4-5H2,(H,25,26)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of mouse NaV1.7 by whole cell voltage clamp method

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Homo sapiens (Human))		BDBM231435
PNG
(US9346798, 182)
Show SMILES COc1cc(ccc1N1CCOc2cc(ccc12)S(=O)(=O)Nc1nccs1)C(F)(F)F
Show InChI InChI=1S/C19H16F3N3O4S2/c1-28-16-10-12(19(20,21)22)2-4-14(16)25-7-8-29-17-11-13(3-5-15(17)25)31(26,27)24-18-23-6-9-30-18/h2-6,9-11H,7-8H2,1H3,(H,23,24)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.7 expressed in HEK293 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Mus musculus)		BDBM50024250
PNG
(CHEMBL2324000)
Show SMILES Cn1nccc1-c1ccccc1Oc1ccc(cc1C#N)S(=O)(=O)Nc1nccs1
Show InChI InChI=1S/C20H15N5O3S2/c1-25-17(8-9-23-25)16-4-2-3-5-19(16)28-18-7-6-15(12-14(18)13-21)30(26,27)24-20-22-10-11-29-20/h2-12H,1H3,(H,22,24)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of mouse NaV1.7 by whole cell voltage clamp method

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Homo sapiens (Human))		BDBM231298
PNG
(US9346798, 45)
Show SMILES FC(F)(F)c1ccc(N2CCOc3cc(ccc23)S(=O)(=O)Nc2ccncn2)c(c1)C1=CCNCC1 |t:34|
Show InChI InChI=1S/C24H22F3N5O3S/c25-24(26,27)17-1-3-20(19(13-17)16-5-8-28-9-6-16)32-11-12-35-22-14-18(2-4-21(22)32)36(33,34)31-23-7-10-29-15-30-23/h1-5,7,10,13-15,28H,6,8-9,11-12H2,(H,29,30,31)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.7 expressed in HEK293 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Homo sapiens (Human))		BDBM231468
PNG
(US9346798, 215)
Show SMILES Fc1cc2N(CCOc2cc1S(=O)(=O)Nc1nccs1)c1ccc(cc1C#N)C(F)(F)F
Show InChI InChI=1S/C19H12F4N4O3S2/c20-13-8-15-16(9-17(13)32(28,29)26-18-25-3-6-31-18)30-5-4-27(15)14-2-1-12(19(21,22)23)7-11(14)10-24/h1-3,6-9H,4-5H2,(H,25,26)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.7 expressed in HEK293 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Homo sapiens (Human))		BDBM231302
PNG
(US9346798, 49)
Show SMILES FC(F)(F)c1ccc(N2CCOc3cc(ccc23)S(=O)(=O)Nc2nccs2)c(c1)C#N
Show InChI InChI=1S/C19H13F3N4O3S2/c20-19(21,22)13-1-3-15(12(9-13)11-23)26-6-7-29-17-10-14(2-4-16(17)26)31(27,28)25-18-24-5-8-30-18/h1-5,8-10H,6-7H2,(H,24,25)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.7 expressed in HEK293 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Homo sapiens (Human))		BDBM50024250
PNG
(CHEMBL2324000)
Show SMILES Cn1nccc1-c1ccccc1Oc1ccc(cc1C#N)S(=O)(=O)Nc1nccs1
Show InChI InChI=1S/C20H15N5O3S2/c1-25-17(8-9-23-25)16-4-2-3-5-19(16)28-18-7-6-15(12-14(18)13-21)30(26,27)24-20-22-10-11-29-20/h2-12H,1H3,(H,22,24)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.7 expressed in HEK293 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Homo sapiens (Human))		BDBM231434
PNG
(US9346798, 181)
Show SMILES COc1cc(ccc1N1CCOc2cc(ccc12)S(=O)(=O)Nc1nccs1)C#N
Show InChI InChI=1S/C19H16N4O4S2/c1-26-17-10-13(12-20)2-4-15(17)23-7-8-27-18-11-14(3-5-16(18)23)29(24,25)22-19-21-6-9-28-19/h2-6,9-11H,7-8H2,1H3,(H,21,22)
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n/an/a 250n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.7 expressed in HEK293 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Homo sapiens (Human))		BDBM231403
PNG
(US9346798, 150)
Show SMILES COc1cc(F)ccc1N1CCOc2cc(ccc12)S(=O)(=O)Nc1nccs1
Show InChI InChI=1S/C18H16FN3O4S2/c1-25-16-10-12(19)2-4-14(16)22-7-8-26-17-11-13(3-5-15(17)22)28(23,24)21-18-20-6-9-27-18/h2-6,9-11H,7-8H2,1H3,(H,20,21)
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n/an/a 280n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.7 expressed in HEK293 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 5 subunit alpha


(Homo sapiens (Human))		BDBM231468
PNG
(US9346798, 215)
Show SMILES Fc1cc2N(CCOc2cc1S(=O)(=O)Nc1nccs1)c1ccc(cc1C#N)C(F)(F)F
Show InChI InChI=1S/C19H12F4N4O3S2/c20-13-8-15-16(9-17(13)32(28,29)26-18-25-3-6-31-18)30-5-4-27(15)14-2-1-12(19(21,22)23)7-11(14)10-24/h1-3,6-9H,4-5H2,(H,25,26)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.5 expressed in HEK295 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Homo sapiens (Human))		BDBM231458
PNG
(US9346798, 205)
Show SMILES COc1ccccc1N1CCOc2cc(ccc12)S(=O)(=O)Nc1nccs1
Show InChI InChI=1S/C18H17N3O4S2/c1-24-16-5-3-2-4-14(16)21-9-10-25-17-12-13(6-7-15(17)21)27(22,23)20-18-19-8-11-26-18/h2-8,11-12H,9-10H2,1H3,(H,19,20)
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n/an/a 380n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.7 expressed in HEK293 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Homo sapiens (Human))		BDBM231465
PNG
(US9346798, 212)
Show SMILES FC(F)(F)c1ccc(N2CCOc3cc(c(Cl)cc23)S(=O)(=O)Nc2nccs2)c(c1)C#N
Show InChI InChI=1S/C19H12ClF3N4O3S2/c20-13-8-15-16(9-17(13)32(28,29)26-18-25-3-6-31-18)30-5-4-27(15)14-2-1-12(19(21,22)23)7-11(14)10-24/h1-3,6-9H,4-5H2,(H,25,26)
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n/an/a 390n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.7 expressed in HEK293 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Rattus norvegicus)		BDBM231435
PNG
(US9346798, 182)
Show SMILES COc1cc(ccc1N1CCOc2cc(ccc12)S(=O)(=O)Nc1nccs1)C(F)(F)F
Show InChI InChI=1S/C19H16F3N3O4S2/c1-28-16-10-12(19(20,21)22)2-4-14(16)25-7-8-29-17-11-13(3-5-15(17)25)31(26,27)24-18-23-6-9-30-18/h2-6,9-11H,7-8H2,1H3,(H,23,24)
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n/an/a 390n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of rat NaV1.7 by cell based whole cell voltage clamp method

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Homo sapiens (Human))		BDBM231342
PNG
(US9346798, 89)
Show SMILES FC(F)(F)c1ccc(N2CCOc3cc(ccc23)S(=O)(=O)Nc2ccncn2)c(c1)C#N
Show InChI InChI=1S/C20H14F3N5O3S/c21-20(22,23)14-1-3-16(13(9-14)11-24)28-7-8-31-18-10-15(2-4-17(18)28)32(29,30)27-19-5-6-25-12-26-19/h1-6,9-10,12H,7-8H2,(H,25,26,27)
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n/an/a 460n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.7 expressed in HEK293 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Homo sapiens (Human))		BDBM231469
PNG
(US9346798, 216)
Show SMILES Fc1c2OCCN(c2ccc1S(=O)(=O)Nc1nccs1)c1ccc(cc1C#N)C(F)(F)F
Show InChI InChI=1S/C19H12F4N4O3S2/c20-16-15(32(28,29)26-18-25-5-8-31-18)4-3-14-17(16)30-7-6-27(14)13-2-1-12(19(21,22)23)9-11(13)10-24/h1-5,8-9H,6-7H2,(H,25,26)
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n/an/a 520n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.7 expressed in HEK293 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Rattus norvegicus)		BDBM231471
PNG
(US9346798, 218)
Show SMILES Fc1cc(cc2OCCN(c3ccc(cc3C#N)C(F)(F)F)c12)S(=O)(=O)Nc1nccs1
Show InChI InChI=1S/C19H12F4N4O3S2/c20-14-8-13(32(28,29)26-18-25-3-6-31-18)9-16-17(14)27(4-5-30-16)15-2-1-12(19(21,22)23)7-11(15)10-24/h1-3,6-9H,4-5H2,(H,25,26)
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n/an/a 560n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of rat NaV1.7 by cell based whole cell voltage clamp method

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 5 subunit alpha


(Homo sapiens (Human))		BDBM231465
PNG
(US9346798, 212)
Show SMILES FC(F)(F)c1ccc(N2CCOc3cc(c(Cl)cc23)S(=O)(=O)Nc2nccs2)c(c1)C#N
Show InChI InChI=1S/C19H12ClF3N4O3S2/c20-13-8-15-16(9-17(13)32(28,29)26-18-25-3-6-31-18)30-5-4-27(15)14-2-1-12(19(21,22)23)7-11(14)10-24/h1-3,6-9H,4-5H2,(H,25,26)
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n/an/a 610n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.5 expressed in HEK295 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 5 subunit alpha


(Homo sapiens (Human))		BDBM231471
PNG
(US9346798, 218)
Show SMILES Fc1cc(cc2OCCN(c3ccc(cc3C#N)C(F)(F)F)c12)S(=O)(=O)Nc1nccs1
Show InChI InChI=1S/C19H12F4N4O3S2/c20-14-8-13(32(28,29)26-18-25-3-6-31-18)9-16-17(14)27(4-5-30-16)15-2-1-12(19(21,22)23)7-11(15)10-24/h1-3,6-9H,4-5H2,(H,25,26)
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n/an/a 650n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.5 expressed in HEK295 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Rattus norvegicus)		BDBM231434
PNG
(US9346798, 181)
Show SMILES COc1cc(ccc1N1CCOc2cc(ccc12)S(=O)(=O)Nc1nccs1)C#N
Show InChI InChI=1S/C19H16N4O4S2/c1-26-17-10-13(12-20)2-4-15(17)23-7-8-27-18-11-14(3-5-16(18)23)29(24,25)22-19-21-6-9-28-19/h2-6,9-11H,7-8H2,1H3,(H,21,22)
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n/an/a 850n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of rat NaV1.7 by cell based whole cell voltage clamp method

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Rattus norvegicus)		BDBM231403
PNG
(US9346798, 150)
Show SMILES COc1cc(F)ccc1N1CCOc2cc(ccc12)S(=O)(=O)Nc1nccs1
Show InChI InChI=1S/C18H16FN3O4S2/c1-25-16-10-12(19)2-4-14(16)22-7-8-26-17-11-13(3-5-15(17)22)28(23,24)21-18-20-6-9-27-18/h2-6,9-11H,7-8H2,1H3,(H,20,21)
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n/an/a 880n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of rat NaV1.7 by cell based whole cell voltage clamp method

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Rattus norvegicus)		BDBM231302
PNG
(US9346798, 49)
Show SMILES FC(F)(F)c1ccc(N2CCOc3cc(ccc23)S(=O)(=O)Nc2nccs2)c(c1)C#N
Show InChI InChI=1S/C19H13F3N4O3S2/c20-19(21,22)13-1-3-15(12(9-13)11-23)26-6-7-29-17-10-14(2-4-16(17)26)31(27,28)25-18-24-5-8-30-18/h1-5,8-10H,6-7H2,(H,24,25)
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n/an/a 1.10E+3n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of rat NaV1.7 by cell based whole cell voltage clamp method

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 5 subunit alpha


(Homo sapiens (Human))		BDBM231302
PNG
(US9346798, 49)
Show SMILES FC(F)(F)c1ccc(N2CCOc3cc(ccc23)S(=O)(=O)Nc2nccs2)c(c1)C#N
Show InChI InChI=1S/C19H13F3N4O3S2/c20-19(21,22)13-1-3-15(12(9-13)11-23)26-6-7-29-17-10-14(2-4-16(17)26)31(27,28)25-18-24-5-8-30-18/h1-5,8-10H,6-7H2,(H,24,25)
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n/an/a 1.50E+3n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.5 expressed in HEK295 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 5 subunit alpha


(Homo sapiens (Human))		BDBM231298
PNG
(US9346798, 45)
Show SMILES FC(F)(F)c1ccc(N2CCOc3cc(ccc23)S(=O)(=O)Nc2ccncn2)c(c1)C1=CCNCC1 |t:34|
Show InChI InChI=1S/C24H22F3N5O3S/c25-24(26,27)17-1-3-20(19(13-17)16-5-8-28-9-6-16)32-11-12-35-22-14-18(2-4-21(22)32)36(33,34)31-23-7-10-29-15-30-23/h1-5,7,10,13-15,28H,6,8-9,11-12H2,(H,29,30,31)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.5 expressed in HEK295 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Rattus norvegicus)		BDBM231458
PNG
(US9346798, 205)
Show SMILES COc1ccccc1N1CCOc2cc(ccc12)S(=O)(=O)Nc1nccs1
Show InChI InChI=1S/C18H17N3O4S2/c1-24-16-5-3-2-4-14(16)21-9-10-25-17-12-13(6-7-15(17)21)27(22,23)20-18-19-8-11-26-18/h2-8,11-12H,9-10H2,1H3,(H,19,20)
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n/an/a 1.60E+3n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of rat NaV1.7 by cell based whole cell voltage clamp method

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Rattus norvegicus)		BDBM231469
PNG
(US9346798, 216)
Show SMILES Fc1c2OCCN(c2ccc1S(=O)(=O)Nc1nccs1)c1ccc(cc1C#N)C(F)(F)F
Show InChI InChI=1S/C19H12F4N4O3S2/c20-16-15(32(28,29)26-18-25-5-8-31-18)4-3-14-17(16)30-7-6-27(14)13-2-1-12(19(21,22)23)9-11(13)10-24/h1-5,8-9H,6-7H2,(H,25,26)
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n/an/a 1.70E+3n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of rat NaV1.7 by cell based whole cell voltage clamp method

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Homo sapiens (Human))		BDBM231471
PNG
(US9346798, 218)
Show SMILES Fc1cc(cc2OCCN(c3ccc(cc3C#N)C(F)(F)F)c12)S(=O)(=O)Nc1nccs1
Show InChI InChI=1S/C19H12F4N4O3S2/c20-14-8-13(32(28,29)26-18-25-3-6-31-18)9-16-17(14)27(4-5-30-16)15-2-1-12(19(21,22)23)7-11(15)10-24/h1-3,6-9H,4-5H2,(H,25,26)
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n/an/a 2.00E+3n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.7 expressed in HEK293 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 5 subunit alpha


(Homo sapiens (Human))		BDBM231435
PNG
(US9346798, 182)
Show SMILES COc1cc(ccc1N1CCOc2cc(ccc12)S(=O)(=O)Nc1nccs1)C(F)(F)F
Show InChI InChI=1S/C19H16F3N3O4S2/c1-28-16-10-12(19(20,21)22)2-4-14(16)25-7-8-29-17-11-13(3-5-15(17)25)31(26,27)24-18-23-6-9-30-18/h2-6,9-11H,7-8H2,1H3,(H,23,24)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.5 expressed in HEK295 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 5 subunit alpha


(Homo sapiens (Human))		BDBM231469
PNG
(US9346798, 216)
Show SMILES Fc1c2OCCN(c2ccc1S(=O)(=O)Nc1nccs1)c1ccc(cc1C#N)C(F)(F)F
Show InChI InChI=1S/C19H12F4N4O3S2/c20-16-15(32(28,29)26-18-25-5-8-31-18)4-3-14-17(16)30-7-6-27(14)13-2-1-12(19(21,22)23)9-11(13)10-24/h1-5,8-9H,6-7H2,(H,25,26)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.5 expressed in HEK295 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Homo sapiens (Human))		BDBM231343
PNG
(US9346798, 90)
Show SMILES FC(F)(F)c1ccc(N2CCOc3cc(ccc23)S(=O)(=O)Nc2ncco2)c(c1)C#N
Show InChI InChI=1S/C19H13F3N4O4S/c20-19(21,22)13-1-3-15(12(9-13)11-23)26-6-8-29-17-10-14(2-4-16(17)26)31(27,28)25-18-24-5-7-30-18/h1-5,7,9-10H,6,8H2,(H,24,25)
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n/an/a 2.60E+3n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.7 expressed in HEK293 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Homo sapiens (Human))		BDBM231405
PNG
(US9346798, 152)
Show SMILES FC(F)(F)c1ccc(N2CCOc3cc(ccc23)S(=O)(=O)Nc2cscn2)c(c1)C#N
Show InChI InChI=1S/C19H13F3N4O3S2/c20-19(21,22)13-1-3-15(12(7-13)9-23)26-5-6-29-17-8-14(2-4-16(17)26)31(27,28)25-18-10-30-11-24-18/h1-4,7-8,10-11,25H,5-6H2
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n/an/a 2.80E+3n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.7 expressed in HEK293 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Rattus norvegicus)		BDBM231342
PNG
(US9346798, 89)
Show SMILES FC(F)(F)c1ccc(N2CCOc3cc(ccc23)S(=O)(=O)Nc2ccncn2)c(c1)C#N
Show InChI InChI=1S/C20H14F3N5O3S/c21-20(22,23)14-1-3-16(13(9-14)11-24)28-7-8-31-18-10-15(2-4-17(18)28)32(29,30)27-19-5-6-25-12-26-19/h1-6,9-10,12H,7-8H2,(H,25,26,27)
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n/an/a 3.00E+3n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of rat NaV1.7 by cell based whole cell voltage clamp method

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Rattus norvegicus)		BDBM50024250
PNG
(CHEMBL2324000)
Show SMILES Cn1nccc1-c1ccccc1Oc1ccc(cc1C#N)S(=O)(=O)Nc1nccs1
Show InChI InChI=1S/C20H15N5O3S2/c1-25-17(8-9-23-25)16-4-2-3-5-19(16)28-18-7-6-15(12-14(18)13-21)30(26,27)24-20-22-10-11-29-20/h2-12H,1H3,(H,22,24)
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n/an/a 4.20E+3n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of rat NaV1.7 by cell based whole cell voltage clamp method

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Mus musculus)		BDBM154055
PNG
(US9012443, 48)
Show SMILES FC(F)(F)c1ccc(c(c1)C1=CCNCC1)-c1cccc2cc(ccc12)S(=O)(=O)Nc1ccncn1 |t:11|
Show InChI InChI=1S/C26H21F3N4O2S/c27-26(28,29)19-4-6-23(24(15-19)17-8-11-30-12-9-17)22-3-1-2-18-14-20(5-7-21(18)22)36(34,35)33-25-10-13-31-16-32-25/h1-8,10,13-16,30H,9,11-12H2,(H,31,32,33)
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n/an/a 4.30E+3n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of mouse NaV1.7 by whole cell voltage clamp method

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 5 subunit alpha


(Homo sapiens (Human))		BDBM231342
PNG
(US9346798, 89)
Show SMILES FC(F)(F)c1ccc(N2CCOc3cc(ccc23)S(=O)(=O)Nc2ccncn2)c(c1)C#N
Show InChI InChI=1S/C20H14F3N5O3S/c21-20(22,23)14-1-3-16(13(9-14)11-24)28-7-8-31-18-10-15(2-4-17(18)28)32(29,30)27-19-5-6-25-12-26-19/h1-6,9-10,12H,7-8H2,(H,25,26,27)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.5 expressed in HEK295 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Homo sapiens (Human))		BDBM231344
PNG
(US9346798, 91)
Show SMILES FC(F)(F)c1ccc(N2CCOc3cc(ccc23)S(=O)(=O)Nc2ccno2)c(c1)C#N
Show InChI InChI=1S/C19H13F3N4O4S/c20-19(21,22)13-1-3-15(12(9-13)11-23)26-7-8-29-17-10-14(2-4-16(17)26)31(27,28)25-18-5-6-24-30-18/h1-6,9-10,25H,7-8H2
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.7 expressed in HEK293 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 5 subunit alpha


(Homo sapiens (Human))		BDBM50024250
PNG
(CHEMBL2324000)
Show SMILES Cn1nccc1-c1ccccc1Oc1ccc(cc1C#N)S(=O)(=O)Nc1nccs1
Show InChI InChI=1S/C20H15N5O3S2/c1-25-17(8-9-23-25)16-4-2-3-5-19(16)28-18-7-6-15(12-14(18)13-21)30(26,27)24-20-22-10-11-29-20/h2-12H,1H3,(H,22,24)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.5

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 5 subunit alpha


(Homo sapiens (Human))		BDBM231434
PNG
(US9346798, 181)
Show SMILES COc1cc(ccc1N1CCOc2cc(ccc12)S(=O)(=O)Nc1nccs1)C#N
Show InChI InChI=1S/C19H16N4O4S2/c1-26-17-10-13(12-20)2-4-15(17)23-7-8-27-18-11-14(3-5-16(18)23)29(24,25)22-19-21-6-9-28-19/h2-6,9-11H,7-8H2,1H3,(H,21,22)
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n/an/a 1.40E+4n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.5 expressed in HEK295 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 5 subunit alpha


(Homo sapiens (Human))		BDBM231403
PNG
(US9346798, 150)
Show SMILES COc1cc(F)ccc1N1CCOc2cc(ccc12)S(=O)(=O)Nc1nccs1
Show InChI InChI=1S/C18H16FN3O4S2/c1-25-16-10-12(19)2-4-14(16)22-7-8-26-17-11-13(3-5-15(17)22)28(23,24)21-18-20-6-9-27-18/h2-6,9-11H,7-8H2,1H3,(H,20,21)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.5 expressed in HEK295 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 10 subunit alpha


(Rattus norvegicus (Rat))		BDBM231468
PNG
(US9346798, 215)
Show SMILES Fc1cc2N(CCOc2cc1S(=O)(=O)Nc1nccs1)c1ccc(cc1C#N)C(F)(F)F
Show InChI InChI=1S/C19H12F4N4O3S2/c20-13-8-15-16(9-17(13)32(28,29)26-18-25-3-6-31-18)30-5-4-27(15)14-2-1-12(19(21,22)23)7-11(14)10-24/h1-3,6-9H,4-5H2,(H,25,26)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of NaV1.8 in rat DRG neurons assessed as reduction in tetrodotoxin-sensitive sodium channel currents at holding potential of -140 mV by ma...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Rattus norvegicus)		BDBM231298
PNG
(US9346798, 45)
Show SMILES FC(F)(F)c1ccc(N2CCOc3cc(ccc23)S(=O)(=O)Nc2ccncn2)c(c1)C1=CCNCC1 |t:34|
Show InChI InChI=1S/C24H22F3N5O3S/c25-24(26,27)17-1-3-20(19(13-17)16-5-8-28-9-6-16)32-11-12-35-22-14-18(2-4-21(22)32)36(33,34)31-23-7-10-29-15-30-23/h1-5,7,10,13-15,28H,6,8-9,11-12H2,(H,29,30,31)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of rat NaV1.7 by cell based whole cell voltage clamp method

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 5 subunit alpha


(Homo sapiens (Human))		BDBM154055
PNG
(US9012443, 48)
Show SMILES FC(F)(F)c1ccc(c(c1)C1=CCNCC1)-c1cccc2cc(ccc12)S(=O)(=O)Nc1ccncn1 |t:11|
Show InChI InChI=1S/C26H21F3N4O2S/c27-26(28,29)19-4-6-23(24(15-19)17-8-11-30-12-9-17)22-3-1-2-18-14-20(5-7-21(18)22)36(34,35)33-25-10-13-31-16-32-25/h1-8,10,13-16,30H,9,11-12H2,(H,31,32,33)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.5 expressed in HEK295 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 5 subunit alpha


(Homo sapiens (Human))		BDBM231458
PNG
(US9346798, 205)
Show SMILES COc1ccccc1N1CCOc2cc(ccc12)S(=O)(=O)Nc1nccs1
Show InChI InChI=1S/C18H17N3O4S2/c1-24-16-5-3-2-4-14(16)21-9-10-25-17-12-13(6-7-15(17)21)27(22,23)20-18-19-8-11-26-18/h2-8,11-12H,9-10H2,1H3,(H,19,20)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.5 expressed in HEK295 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 9 subunit alpha


(Rattus norvegicus)		BDBM154055
PNG
(US9012443, 48)
Show SMILES FC(F)(F)c1ccc(c(c1)C1=CCNCC1)-c1cccc2cc(ccc12)S(=O)(=O)Nc1ccncn1 |t:11|
Show InChI InChI=1S/C26H21F3N4O2S/c27-26(28,29)19-4-6-23(24(15-19)17-8-11-30-12-9-17)22-3-1-2-18-14-20(5-7-21(18)22)36(34,35)33-25-10-13-31-16-32-25/h1-8,10,13-16,30H,9,11-12H2,(H,31,32,33)
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Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of rat NaV1.7 by cell based whole cell voltage clamp method

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 5 subunit alpha


(Homo sapiens (Human))		BDBM50024250
PNG
(CHEMBL2324000)
Show SMILES Cn1nccc1-c1ccccc1Oc1ccc(cc1C#N)S(=O)(=O)Nc1nccs1
Show InChI InChI=1S/C20H15N5O3S2/c1-25-17(8-9-23-25)16-4-2-3-5-19(16)28-18-7-6-15(12-14(18)13-21)30(26,27)24-20-22-10-11-29-20/h2-12H,1H3,(H,22,24)
PDB

KEGG

UniProtKB/SwissProt

B.MOAD
DrugBank
antibodypedia
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CHEMBL
MCE
PC cid
PC sid
UniChem

Similars
Article
PubMed
n/an/a>3.00E+4n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of human NaV1.5 expressed in HEK295 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp metho...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
Sodium channel protein type 10 subunit alpha


(Mus musculus)		BDBM231468
PNG
(US9346798, 215)
Show SMILES Fc1cc2N(CCOc2cc1S(=O)(=O)Nc1nccs1)c1ccc(cc1C#N)C(F)(F)F
Show InChI InChI=1S/C19H12F4N4O3S2/c20-13-8-15-16(9-17(13)32(28,29)26-18-25-3-6-31-18)30-5-4-27(15)14-2-1-12(19(21,22)23)7-11(14)10-24/h1-3,6-9H,4-5H2,(H,25,26)
PDB

KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
PC cid
PC sid
UniChem
Article
PubMed
n/an/a 5.30E+4n/an/an/an/an/an/a



Department of Medicinal Chemistry, Amgen Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: daniel.la@sagerx.com.

Curated by ChEMBL


Assay Description
Inhibition of NaV1.8 in C57BL/6 mouse DRG neurons assessed as reduction in tetrodotoxin-sensitive sodium channel currents at holding potential of -14...

Bioorg Med Chem Lett 27: 3477-3485 (2017)


Article DOI: 10.1016/j.bmcl.2017.05.070
BindingDB Entry DOI: 10.7270/Q2H134H4
More data for this
Ligand-Target Pair
* indicates data uncertainty>20%