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Found 393 hits Enz. Inhib. hit(s) with Target = 'Voltage-gated sodium channel subunit alpha Nav1.8' AND taxid = 10116   
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 alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161329
PNG
(US9051270, 114 | US9163042, 1a)
Show SMILES COc1cc(F)ccc1Oc1cc(Cl)c(Cl)cc1C(=O)Nc1cc[nH]c(=O)c1
Show InChI InChI=1S/C19H13Cl2FN2O4/c1-27-17-6-10(22)2-3-15(17)28-16-9-14(21)13(20)8-12(16)19(26)24-11-4-5-23-18(25)7-11/h2-9H,1H3,(H2,23,24,25,26)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9051270 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161329
PNG
(US9051270, 114 | US9163042, 1a)
Show SMILES COc1cc(F)ccc1Oc1cc(Cl)c(Cl)cc1C(=O)Nc1cc[nH]c(=O)c1
Show InChI InChI=1S/C19H13Cl2FN2O4/c1-27-17-6-10(22)2-3-15(17)28-16-9-14(21)13(20)8-12(16)19(26)24-11-4-5-23-18(25)7-11/h2-9H,1H3,(H2,23,24,25,26)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9163042 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM181203
PNG
(US9139529, 46)
Show SMILES COc1cc(F)ccc1Oc1nc2ccccc2nc1C(=O)Nc1cccc(c1)S(C)(=O)=O
Show InChI InChI=1S/C23H18FN3O5S/c1-31-20-12-14(24)10-11-19(20)32-23-21(26-17-8-3-4-9-18(17)27-23)22(28)25-15-6-5-7-16(13-15)33(2,29)30/h3-13H,1-2H3,(H,25,28)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9139529 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161373
PNG
(US9051270, 158)
Show SMILES COc1cc(F)ccc1Oc1cc(ccc1C(=O)Nc1cc[nH]c(=O)c1)C(F)(F)F
Show InChI InChI=1S/C20H14F4N2O4/c1-29-17-9-12(21)3-5-15(17)30-16-8-11(20(22,23)24)2-4-14(16)19(28)26-13-6-7-25-18(27)10-13/h2-10H,1H3,(H2,25,26,27,28)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9051270 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM181223
PNG
(US9139529, 66)
Show SMILES NS(=O)(=O)c1cccc(NC(=O)c2cc3ccccc3nc2Oc2ccc(F)cc2Cl)c1
Show InChI InChI=1S/C22H15ClFN3O4S/c23-18-11-14(24)8-9-20(18)31-22-17(10-13-4-1-2-7-19(13)27-22)21(28)26-15-5-3-6-16(12-15)32(25,29)30/h1-12H,(H,26,28)(H2,25,29,30)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9139529 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161326
PNG
(US9051270, 111 | US9163042, 2a)
Show SMILES COc1cc(F)ccc1Oc1cc(ccc1C(=O)Nc1cc[nH]c(=O)c1)C(F)(F)C(F)(F)F
Show InChI InChI=1S/C21H14F6N2O4/c1-32-17-9-12(22)3-5-15(17)33-16-8-11(20(23,24)21(25,26)27)2-4-14(16)19(31)29-13-6-7-28-18(30)10-13/h2-10H,1H3,(H2,28,29,30,31)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9051270 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161326
PNG
(US9051270, 111 | US9163042, 2a)
Show SMILES COc1cc(F)ccc1Oc1cc(ccc1C(=O)Nc1cc[nH]c(=O)c1)C(F)(F)C(F)(F)F
Show InChI InChI=1S/C21H14F6N2O4/c1-32-17-9-12(22)3-5-15(17)33-16-8-11(20(23,24)21(25,26)27)2-4-14(16)19(31)29-13-6-7-28-18(30)10-13/h2-10H,1H3,(H2,28,29,30,31)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9163042 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM181163
PNG
(US9139529, 6)
Show SMILES NS(=O)(=O)c1cccc(NC(=O)c2nc3ccccc3nc2Oc2ccc(F)cc2Cl)c1
Show InChI InChI=1S/C21H14ClFN4O4S/c22-15-10-12(23)8-9-18(15)31-21-19(26-16-6-1-2-7-17(16)27-21)20(28)25-13-4-3-5-14(11-13)32(24,29)30/h1-11H,(H,25,28)(H2,24,29,30)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9139529 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM186571
PNG
(US9163042, 1)
Show SMILES COc1cc(F)ccc1Oc1cc(Cl)c(Cl)cc1C(=O)Nc1ccn(COP(O)(O)=O)c(=O)c1
Show InChI InChI=1S/C20H16Cl2FN2O8P/c1-31-18-6-11(23)2-3-16(18)33-17-9-15(22)14(21)8-13(17)20(27)24-12-4-5-25(19(26)7-12)10-32-34(28,29)30/h2-9H,10H2,1H3,(H,24,27)(H2,28,29,30)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9163042 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM181161
PNG
(US9139529, 4)
Show SMILES COc1ccc(Oc2nc3ccccc3nc2C(=O)Nc2cccc(c2)S(N)(=O)=O)c(Cl)c1
Show InChI InChI=1S/C22H17ClN4O5S/c1-31-14-9-10-19(16(23)12-14)32-22-20(26-17-7-2-3-8-18(17)27-22)21(28)25-13-5-4-6-15(11-13)33(24,29)30/h2-12H,1H3,(H,25,28)(H2,24,29,30)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9139529 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161369
PNG
(US9051270, 154)
Show SMILES COc1cc(F)ccc1Oc1cc(cc(c1C(=O)Nc1cc[nH]c(=O)c1)C(F)(F)F)C(F)(F)F
Show InChI InChI=1S/C21H13F7N2O4/c1-33-15-8-11(22)2-3-14(15)34-16-7-10(20(23,24)25)6-13(21(26,27)28)18(16)19(32)30-12-4-5-29-17(31)9-12/h2-9H,1H3,(H2,29,30,31,32)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9051270 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM181168
PNG
(US9139529, 11)
Show SMILES COc1cc(Cl)ccc1Oc1nc2ccccc2nc1C(=O)Nc1cccc(c1)S(N)(=O)=O
Show InChI InChI=1S/C22H17ClN4O5S/c1-31-19-11-13(23)9-10-18(19)32-22-20(26-16-7-2-3-8-17(16)27-22)21(28)25-14-5-4-6-15(12-14)33(24,29)30/h2-12H,1H3,(H,25,28)(H2,24,29,30)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9139529 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM160984
PNG
(US9108903, 49)
Show SMILES COc1cc(CO)ccc1Oc1cc(cc(c1C(=O)Nc1ccc(nc1)C(O)=O)C(F)(F)F)C(F)(F)F
Show InChI InChI=1S/C23H16F6N2O6/c1-36-17-6-11(10-32)2-5-16(17)37-18-8-12(22(24,25)26)7-14(23(27,28)29)19(18)20(33)31-13-3-4-15(21(34)35)30-9-13/h2-9,32H,10H2,1H3,(H,31,33)(H,34,35)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9108903 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161328
PNG
(US9051270, 113 | US9163042, 3a)
Show SMILES Fc1ccc(Oc2cc(Cl)c(Cl)cc2C(=O)Nc2cc[nH]c(=O)c2)cc1
Show InChI InChI=1S/C18H11Cl2FN2O3/c19-14-8-13(18(25)23-11-5-6-22-17(24)7-11)16(9-15(14)20)26-12-3-1-10(21)2-4-12/h1-9H,(H2,22,23,24,25)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9051270 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161328
PNG
(US9051270, 113 | US9163042, 3a)
Show SMILES Fc1ccc(Oc2cc(Cl)c(Cl)cc2C(=O)Nc2cc[nH]c(=O)c2)cc1
Show InChI InChI=1S/C18H11Cl2FN2O3/c19-14-8-13(18(25)23-11-5-6-22-17(24)7-11)16(9-15(14)20)26-12-3-1-10(21)2-4-12/h1-9H,(H2,22,23,24,25)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9163042 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM181159
PNG
(US9139529, 2)
Show SMILES COc1cc(F)ccc1Oc1nc2ccccc2nc1C(=O)Nc1cccc(c1)S(N)(=O)=O
Show InChI InChI=1S/C22H17FN4O5S/c1-31-19-11-13(23)9-10-18(19)32-22-20(26-16-7-2-3-8-17(16)27-22)21(28)25-14-5-4-6-15(12-14)33(24,29)30/h2-12H,1H3,(H,25,28)(H2,24,29,30)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9139529 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM181165
PNG
(US9139529, 8)
Show SMILES COc1ccc(Oc2nc3ccccc3nc2C(=O)Nc2cccc(c2)S(N)(=O)=O)c(OC)c1
Show InChI InChI=1S/C23H20N4O6S/c1-31-15-10-11-19(20(13-15)32-2)33-23-21(26-17-8-3-4-9-18(17)27-23)22(28)25-14-6-5-7-16(12-14)34(24,29)30/h3-13H,1-2H3,(H,25,28)(H2,24,29,30)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9139529 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161330
PNG
(US9051270, 115)
Show SMILES COc1ccc(Oc2cc(Cl)c(Cl)cc2C(=O)Nc2cc[nH]c(=O)c2)cc1F
Show InChI InChI=1S/C19H13Cl2FN2O4/c1-27-16-3-2-11(7-15(16)22)28-17-9-14(21)13(20)8-12(17)19(26)24-10-4-5-23-18(25)6-10/h2-9H,1H3,(H2,23,24,25,26)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9051270 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM181171
PNG
(US9139529, 14)
Show SMILES Cc1cc(F)ccc1Oc1nc2ccccc2nc1C(=O)Nc1cccc(c1)S(N)(=O)=O
Show InChI InChI=1S/C22H17FN4O4S/c1-13-11-14(23)9-10-19(13)31-22-20(26-17-7-2-3-8-18(17)27-22)21(28)25-15-5-4-6-16(12-15)32(24,29)30/h2-12H,1H3,(H,25,28)(H2,24,29,30)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9139529 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM181190
PNG
(US9139529, 33)
Show SMILES OC(=O)c1cc(NC(=O)c2nc3ccccc3nc2Oc2ccc(OC(F)(F)F)cc2)ccn1
Show InChI InChI=1S/C22H13F3N4O5/c23-22(24,25)34-14-7-5-13(6-8-14)33-20-18(28-15-3-1-2-4-16(15)29-20)19(30)27-12-9-10-26-17(11-12)21(31)32/h1-11H,(H,31,32)(H,26,27,30)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9139529 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM50329205
PNG
(5-(4-chlorophenyl)-N-((2-(piperidin-1-yl)pyridin-3...)
Show SMILES Clc1ccc(cc1)-c1cncc(c1)C(=O)NCc1cccnc1N1CCCCC1
Show InChI InChI=1S/C23H23ClN4O/c24-21-8-6-17(7-9-21)19-13-20(15-25-14-19)23(29)27-16-18-5-4-10-26-22(18)28-11-2-1-3-12-28/h4-10,13-15H,1-3,11-12,16H2,(H,27,29)
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Abbott Laboratories

Curated by ChEMBL


Assay Description
Inhibition of tetrodotoxin-resistant NaV1.8 in rat DRG neuron by electrophysiology


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM181220
PNG
(US9139529, 63)
Show SMILES Cc1cc(F)ccc1Oc1nc2ccccc2cc1C(=O)Nc1cccc(c1)S(N)(=O)=O
Show InChI InChI=1S/C23H18FN3O4S/c1-14-11-16(24)9-10-21(14)31-23-19(12-15-5-2-3-8-20(15)27-23)22(28)26-17-6-4-7-18(13-17)32(25,29)30/h2-13H,1H3,(H,26,28)(H2,25,29,30)
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n/an/a 8n/an/an/an/an/an/a



VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9139529 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM160986
PNG
(US9108903, 51 | US9108903, 76)
Show SMILES COc1cc(F)ccc1Oc1cc(Cl)c(Cl)cc1C(=O)Nc1ccc(nc1)C(O)=O
Show InChI InChI=1S/C20H13Cl2FN2O5/c1-29-18-6-10(23)2-5-16(18)30-17-8-14(22)13(21)7-12(17)19(26)25-11-3-4-15(20(27)28)24-9-11/h2-9H,1H3,(H,25,26)(H,27,28)
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n/an/a 9n/an/an/an/an/an/a



VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9108903 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM50329211
PNG
(5-(4-chlorophenyl)-N-(2-methylbenzyl)nicotinamide ...)
Show SMILES Cc1ccccc1CNC(=O)c1cncc(c1)-c1ccc(Cl)cc1
Show InChI InChI=1S/C20H17ClN2O/c1-14-4-2-3-5-16(14)13-23-20(24)18-10-17(11-22-12-18)15-6-8-19(21)9-7-15/h2-12H,13H2,1H3,(H,23,24)
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n/an/a 9n/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
Inhibition of tetrodotoxin-resistant NaV1.8 in rat DRG neuron by electrophysiology


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161368
PNG
(US9051270, 153)
Show SMILES Cc1cc(F)ccc1Oc1cc(cc(c1C(=O)Nc1cc[nH]c(=O)c1)C(F)(F)F)C(F)(F)F
Show InChI InChI=1S/C21H13F7N2O3/c1-10-6-12(22)2-3-15(10)33-16-8-11(20(23,24)25)7-14(21(26,27)28)18(16)19(32)30-13-4-5-29-17(31)9-13/h2-9H,1H3,(H2,29,30,31,32)
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n/an/a 10n/an/an/an/an/an/a



VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9051270 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM160947
PNG
(US9108903, 12)
Show SMILES COc1cc(F)ccc1Oc1cc(Cl)c(Cl)cc1C(=O)Nc1ccc(cc1)C(O)=O
Show InChI InChI=1S/C21H14Cl2FNO5/c1-29-19-8-12(24)4-7-17(19)30-18-10-16(23)15(22)9-14(18)20(26)25-13-5-2-11(3-6-13)21(27)28/h2-10H,1H3,(H,25,26)(H,27,28)
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n/an/a 11n/an/an/an/an/an/a



VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9108903 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM160953
PNG
(US9108903, 18)
Show SMILES COc1cc(Cl)ccc1Oc1cc(Cl)c(Cl)cc1C(=O)Nc1ccc(cc1)C(O)=O
Show InChI InChI=1S/C21H14Cl3NO5/c1-29-19-8-12(22)4-7-17(19)30-18-10-16(24)15(23)9-14(18)20(26)25-13-5-2-11(3-6-13)21(27)28/h2-10H,1H3,(H,25,26)(H,27,28)
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n/an/a 11n/an/an/an/an/an/a



VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9108903 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM160967
PNG
(US9108903, 32)
Show SMILES Cc1cc(F)ccc1Oc1cc(Cl)c(Cl)cc1C(=O)Nc1ccc(nc1)C(O)=O
Show InChI InChI=1S/C20H13Cl2FN2O4/c1-10-6-11(23)2-5-17(10)29-18-8-15(22)14(21)7-13(18)19(26)25-12-3-4-16(20(27)28)24-9-12/h2-9H,1H3,(H,25,26)(H,27,28)
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n/an/a 11n/an/an/an/an/an/a



VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9108903 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161294
PNG
(US9051270, 79 | US9051270, 82 | US9163042, 5a)
Show SMILES FC(F)(F)Oc1ccc(Oc2cc(ccc2C(=O)Nc2cc[nH]c(=O)c2)C(F)(F)F)cc1
Show InChI InChI=1S/C20H12F6N2O4/c21-19(22,23)11-1-6-15(18(30)28-12-7-8-27-17(29)10-12)16(9-11)31-13-2-4-14(5-3-13)32-20(24,25)26/h1-10H,(H2,27,28,29,30)
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n/an/a 11n/an/an/an/an/an/a



VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9051270 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161245
PNG
(US9051270, 30 | US9163042, 4a)
Show SMILES COc1cc(F)ccc1Oc1ccc(cc1C(=O)Nc1cc[nH]c(=O)c1)C(F)(F)F
Show InChI InChI=1S/C20H14F4N2O4/c1-29-17-9-12(21)3-5-16(17)30-15-4-2-11(20(22,23)24)8-14(15)19(28)26-13-6-7-25-18(27)10-13/h2-10H,1H3,(H2,25,26,27,28)
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n/an/a 11n/an/an/an/an/an/a



VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9051270 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161370
PNG
(US9051270, 155)
Show SMILES Fc1ccc(Oc2cc(cc(c2C(=O)Nc2cc[nH]c(=O)c2)C(F)(F)F)C(F)(F)F)cc1
Show InChI InChI=1S/C20H11F7N2O3/c21-11-1-3-13(4-2-11)32-15-8-10(19(22,23)24)7-14(20(25,26)27)17(15)18(31)29-12-5-6-28-16(30)9-12/h1-9H,(H2,28,29,30,31)
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n/an/a 11n/an/an/an/an/an/a



VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9051270 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161245
PNG
(US9051270, 30 | US9163042, 4a)
Show SMILES COc1cc(F)ccc1Oc1ccc(cc1C(=O)Nc1cc[nH]c(=O)c1)C(F)(F)F
Show InChI InChI=1S/C20H14F4N2O4/c1-29-17-9-12(21)3-5-16(17)30-15-4-2-11(20(22,23)24)8-14(15)19(28)26-13-6-7-25-18(27)10-13/h2-10H,1H3,(H2,25,26,27,28)
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n/an/a 11n/an/an/an/an/an/a



VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9163042 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161294
PNG
(US9051270, 79 | US9051270, 82 | US9163042, 5a)
Show SMILES FC(F)(F)Oc1ccc(Oc2cc(ccc2C(=O)Nc2cc[nH]c(=O)c2)C(F)(F)F)cc1
Show InChI InChI=1S/C20H12F6N2O4/c21-19(22,23)11-1-6-15(18(30)28-12-7-8-27-17(29)10-12)16(9-11)31-13-2-4-14(5-3-13)32-20(24,25)26/h1-10H,(H2,27,28,29,30)
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n/an/a 11n/an/an/an/an/an/a



VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9163042 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM181218
PNG
(US9139529, 61)
Show SMILES COc1cc(F)ccc1Oc1nc2ccccc2cc1C(=O)Nc1cccc(c1)S(N)(=O)=O
Show InChI InChI=1S/C23H18FN3O5S/c1-31-21-12-15(24)9-10-20(21)32-23-18(11-14-5-2-3-8-19(14)27-23)22(28)26-16-6-4-7-17(13-16)33(25,29)30/h2-13H,1H3,(H,26,28)(H2,25,29,30)
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n/an/a 11n/an/an/an/an/an/a



VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9139529 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM181222
PNG
(US9139529, 65)
Show SMILES NS(=O)(=O)c1cccc(NC(=O)c2cc3ccccc3nc2Oc2ccc(F)cc2F)c1
Show InChI InChI=1S/C22H15F2N3O4S/c23-14-8-9-20(18(24)11-14)31-22-17(10-13-4-1-2-7-19(13)27-22)21(28)26-15-5-3-6-16(12-15)32(25,29)30/h1-12H,(H,26,28)(H2,25,29,30)
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n/an/a 11n/an/an/an/an/an/a



VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9139529 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM160976
PNG
(US9108903, 41)
Show SMILES OC(=O)c1ccc(NC(=O)c2cc(Cl)c(Cl)cc2Oc2ccc(F)cc2Cl)cn1
Show InChI InChI=1S/C19H10Cl3FN2O4/c20-12-6-11(18(26)25-10-2-3-15(19(27)28)24-8-10)17(7-13(12)21)29-16-4-1-9(23)5-14(16)22/h1-8H,(H,25,26)(H,27,28)
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n/an/a 12n/an/an/an/an/an/a



VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9108903 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM160986
PNG
(US9108903, 51 | US9108903, 76)
Show SMILES COc1cc(F)ccc1Oc1cc(Cl)c(Cl)cc1C(=O)Nc1ccc(nc1)C(O)=O
Show InChI InChI=1S/C20H13Cl2FN2O5/c1-29-18-6-10(23)2-5-16(18)30-17-8-14(22)13(21)7-12(17)19(26)25-11-3-4-15(20(27)28)24-9-11/h2-9H,1H3,(H,25,26)(H,27,28)
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n/an/a 12n/an/an/an/an/an/a



VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9108903 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161303
PNG
(US9051270, 88 | US9163042, 6a)
Show SMILES Fc1ccc(Oc2cc(ccc2C(=O)Nc2cc[nH]c(=O)c2)C(F)(F)C(F)(F)F)cc1
Show InChI InChI=1S/C20H12F6N2O3/c21-12-2-4-14(5-3-12)31-16-9-11(19(22,23)20(24,25)26)1-6-15(16)18(30)28-13-7-8-27-17(29)10-13/h1-10H,(H2,27,28,29,30)
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n/an/a 12n/an/an/an/an/an/a



VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9051270 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM50330949
PNG
(CHEMBL1277877 | N-(3,5-Dimethylphenyl)-6-(4-ethoxy...)
Show SMILES CCOc1ccc(cc1)-c1cncc(n1)C(=O)Nc1cc(C)cc(C)c1
Show InChI InChI=1S/C21H21N3O2/c1-4-26-18-7-5-16(6-8-18)19-12-22-13-20(24-19)21(25)23-17-10-14(2)9-15(3)11-17/h5-13H,4H2,1-3H3,(H,23,25)
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n/an/a 12n/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
Inhibition of tetrodotoxin-resistant NaV1.8 in rat dorsal root ganglion neurons at holding potential -100 mV by whole-cell patch clamp electrophysiol...


Citation and Details
More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161303
PNG
(US9051270, 88 | US9163042, 6a)
Show SMILES Fc1ccc(Oc2cc(ccc2C(=O)Nc2cc[nH]c(=O)c2)C(F)(F)C(F)(F)F)cc1
Show InChI InChI=1S/C20H12F6N2O3/c21-12-2-4-14(5-3-12)31-16-9-11(19(22,23)20(24,25)26)1-6-15(16)18(30)28-13-7-8-27-17(29)10-13/h1-10H,(H2,27,28,29,30)
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n/an/a 12n/an/an/an/an/an/a



VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9163042 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161285
PNG
(US9051270, 70 | US9163042, 7a)
Show SMILES COc1cc(F)ccc1Oc1ccc(Cl)cc1C(=O)Nc1cc[nH]c(=O)c1
Show InChI InChI=1S/C19H14ClFN2O4/c1-26-17-9-12(21)3-5-16(17)27-15-4-2-11(20)8-14(15)19(25)23-13-6-7-22-18(24)10-13/h2-10H,1H3,(H2,22,23,24,25)
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n/an/a 13n/an/an/an/an/an/a



VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9051270 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161287
PNG
(US9051270, 72 | US9051270, 73 | US9163042, 8a)
Show SMILES FC(F)(F)Oc1ccc(Oc2ccc(cc2C(=O)Nc2cc[nH]c(=O)c2)C(F)(F)F)cc1
Show InChI InChI=1S/C20H12F6N2O4/c21-19(22,23)11-1-6-16(31-13-2-4-14(5-3-13)32-20(24,25)26)15(9-11)18(30)28-12-7-8-27-17(29)10-12/h1-10H,(H2,27,28,29,30)
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n/an/a 13n/an/an/an/an/an/a



VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9051270 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161285
PNG
(US9051270, 70 | US9163042, 7a)
Show SMILES COc1cc(F)ccc1Oc1ccc(Cl)cc1C(=O)Nc1cc[nH]c(=O)c1
Show InChI InChI=1S/C19H14ClFN2O4/c1-26-17-9-12(21)3-5-16(17)27-15-4-2-11(20)8-14(15)19(25)23-13-6-7-22-18(24)10-13/h2-10H,1H3,(H2,22,23,24,25)
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n/an/a 13n/an/an/an/an/an/a



VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9163042 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161287
PNG
(US9051270, 72 | US9051270, 73 | US9163042, 8a)
Show SMILES FC(F)(F)Oc1ccc(Oc2ccc(cc2C(=O)Nc2cc[nH]c(=O)c2)C(F)(F)F)cc1
Show InChI InChI=1S/C20H12F6N2O4/c21-19(22,23)11-1-6-16(31-13-2-4-14(5-3-13)32-20(24,25)26)15(9-11)18(30)28-12-7-8-27-17(29)10-12/h1-10H,(H2,27,28,29,30)
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n/an/a 13n/an/an/an/an/an/a



VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9163042 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM181162
PNG
(US9139529, 5)
Show SMILES NS(=O)(=O)c1cccc(NC(=O)c2nc3ccccc3nc2Oc2ccc(F)cc2F)c1
Show InChI InChI=1S/C21H14F2N4O4S/c22-12-8-9-18(15(23)10-12)31-21-19(26-16-6-1-2-7-17(16)27-21)20(28)25-13-4-3-5-14(11-13)32(24,29)30/h1-11H,(H,25,28)(H2,24,29,30)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9139529 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM181225
PNG
(US9139529, 68)
Show SMILES NS(=O)(=O)c1cccc(NC(=O)c2cc3ccccc3nc2Oc2ccc(OC(F)(F)F)cc2)c1
Show InChI InChI=1S/C23H16F3N3O5S/c24-23(25,26)34-17-10-8-16(9-11-17)33-22-19(12-14-4-1-2-7-20(14)29-22)21(30)28-15-5-3-6-18(13-15)35(27,31)32/h1-13H,(H,28,30)(H2,27,31,32)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9139529 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM160983
PNG
(US9108903, 48)
Show SMILES COc1cc(F)ccc1Oc1cc(cc(c1C(=O)Nc1ccc(nc1)C(O)=O)C(F)(F)F)C(F)(F)F
Show InChI InChI=1S/C22H13F7N2O5/c1-35-16-8-11(23)2-5-15(16)36-17-7-10(21(24,25)26)6-13(22(27,28)29)18(17)19(32)31-12-3-4-14(20(33)34)30-9-12/h2-9H,1H3,(H,31,32)(H,33,34)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9108903 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161225
PNG
(US9051270, 10 | US9163042, 9a)
Show SMILES Cc1cc(F)ccc1Oc1cc(ccc1C(=O)Nc1cc[nH]c(=O)c1)C(F)(F)F
Show InChI InChI=1S/C20H14F4N2O3/c1-11-8-13(21)3-5-16(11)29-17-9-12(20(22,23)24)2-4-15(17)19(28)26-14-6-7-25-18(27)10-14/h2-10H,1H3,(H2,25,26,27,28)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9051270 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161231
PNG
(US9051270, 16)
Show SMILES COc1cc(F)ccc1Oc1cc(Cl)ccc1C(=O)Nc1cc[nH]c(=O)c1
Show InChI InChI=1S/C19H14ClFN2O4/c1-26-17-9-12(21)3-5-15(17)27-16-8-11(20)2-4-14(16)19(25)23-13-6-7-22-18(24)10-13/h2-10H,1H3,(H2,22,23,24,25)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9051270 (2015)

More data for this
Ligand-Target Pair
Voltage-gated sodium channel subunit alpha Nav1.8


(Rattus norvegicus (Rat))
BDBM161225
PNG
(US9051270, 10 | US9163042, 9a)
Show SMILES Cc1cc(F)ccc1Oc1cc(ccc1C(=O)Nc1cc[nH]c(=O)c1)C(F)(F)F
Show InChI InChI=1S/C20H14F4N2O3/c1-11-8-13(21)3-5-16(11)29-17-9-12(20(22,23)24)2-4-15(17)19(28)26-14-6-7-25-18(27)10-14/h2-10H,1H3,(H2,25,26,27,28)
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VERTEX PHARMACEUTICALS INCORPORATED

US Patent


Assay Description
Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons...


US Patent US9163042 (2015)

More data for this
Ligand-Target Pair
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