Found 2516 hits Enz. Inhib. hit(s) with Target = 'Sodium channel protein type 8 subunit alpha' Target/Host
(Institution) | Ligand | Target/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 | pH | Temp
°C |
|---|
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM50240277
(CHEMBL4061793)Show SMILES Fc1cc(NCC23CCCN2CCC3)c(Cl)cc1S(=O)(=O)Nc1nccs1 Show InChI InChI=1S/C17H20ClFN4O2S2/c18-12-9-15(27(24,25)22-16-20-5-8-26-16)13(19)10-14(12)21-11-17-3-1-6-23(17)7-2-4-17/h5,8-10,21H,1-4,6-7,11H2,(H,20,22) | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet 
| Purchase
CHEMBL
MCE
PC cid
PC sid
UniChem
Patents
Similars
| Article
PubMed
| n/a | n/a | 0.0600 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Inhibition of human Nav1.6 alpha expressed in HEK293 cells incubated for 5 mins with 6 consecutive train pulses to -10 mV at 0.1 Hz and holding poten... |
Citation and Details
Article DOI: 10.1021/acsmedchemlett.1c00218
BindingDB Entry DOI: 10.7270/Q2C2514T |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM50240278
(CHEMBL4062780)Show SMILES CC1(C)CN2CCC[C@]2(CNc2cc(F)c(cc2Cl)S(=O)(=O)Nc2nccs2)C1 |r| Show InChI InChI=1S/C19H24ClFN4O2S2/c1-18(2)10-19(4-3-6-25(19)12-18)11-23-15-9-14(21)16(8-13(15)20)29(26,27)24-17-22-5-7-28-17/h5,7-9,23H,3-4,6,10-12H2,1-2H3,(H,22,24)/t19-/m1/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 0.0900 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Inhibition of human Nav1.6 alpha expressed in HEK293 cells incubated for 5 mins with 6 consecutive train pulses to -10 mV at 0.1 Hz and holding poten... |
Citation and Details
Article DOI: 10.1021/acsmedchemlett.1c00218
BindingDB Entry DOI: 10.7270/Q2C2514T |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM621932
((S)-N-((R or S)-(3- chloro-4- fluorophenyl)(5- chl...)Show SMILES Fc1ccc(cc1Cl)[C@H](NC(=O)[C@@H]1CNC(=O)N1)c1cc2cc(Cl)ccc2o1 |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 0.200 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
|
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM630994
((S)-N-((R or S)-(3- chloro-4- fluorophenyl)(5- chl...)Show SMILES Fc1ccc(cc1Cl)C(NC(=O)[C@@H]1CNC(=O)N1)c1cc2cc(Cl)ccc2o1 |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 0.200 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
|
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM621933
((S)-N-((R or S)-(3- chloro-4- fluorophenyl)(5- chl...)Show SMILES Fc1ccc(cc1Cl)[C@@H](NC(=O)[C@@H]1CNC(=O)N1)c1cc2cc(Cl)ccc2o1 |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 0.200 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
|
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM630994
((S)-N-((R or S)-(3- chloro-4- fluorophenyl)(5- chl...)Show SMILES Fc1ccc(cc1Cl)C(NC(=O)[C@@H]1CNC(=O)N1)c1cc2cc(Cl)ccc2o1 |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 0.200 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
|
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM621910
((S)-N-((R or S)-(3- chloro-4- fluorophenyl)(5-chlo...)Show SMILES Fc1ccc(cc1Cl)C(NC(=O)[C@@H]1CNC(=O)N1)c1ccc(Cl)c(n1)C(F)(F)F |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 0.400 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
|
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM621911
((S)-N-((R or S)-(3- chloro-4- fluorophenyl)(5-chlo...)Show SMILES Fc1ccc(cc1Cl)[C@@H](NC(=O)[C@@H]1CNC(=O)N1)c1ccc(Cl)c(n1)C(F)(F)F |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 0.400 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
|
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM630957
((S)-N-((R or S)-(4- chlorophenyl)(4- fluoro-3-(tri...)Show SMILES Fc1ccc(cc1C(F)(F)F)C(NC(=O)[C@@H]1CNC(=O)N1)c1ccc(Cl)cc1 |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 0.600 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
|
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM621824
((S)-N-((R or S)-(4- chlorophenyl)(4- fluoro-3-(tri...)Show SMILES Fc1ccc(cc1C(F)(F)F)[C@@H](NC(=O)[C@@H]1CNC(=O)N1)c1ccc(Cl)cc1 |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 0.600 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
|
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM621909
((S)-N-(bis(3-chloro-4- fluorophenyl)methyl)- 2-oxo...)Show SMILES Fc1ccc(cc1Cl)C(NC(=O)[C@@H]1CNC(=O)N1)c1ccc(F)c(Cl)c1 |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 0.700 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
|
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM621909
((S)-N-(bis(3-chloro-4- fluorophenyl)methyl)- 2-oxo...)Show SMILES Fc1ccc(cc1Cl)C(NC(=O)[C@@H]1CNC(=O)N1)c1ccc(F)c(Cl)c1 |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 0.700 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
|
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM50118514
(CHEMBL3617063 | US9481677, 38)Show SMILES Nc1nc2cc(ccc2[nH]1)-c1cc(Cl)ccc1Oc1cc(F)c(cc1F)S(=O)(=O)Nc1ncns1 Show InChI InChI=1S/C21H13ClF2N6O3S2/c22-11-2-4-17(12(6-11)10-1-3-15-16(5-10)29-20(25)28-15)33-18-7-14(24)19(8-13(18)23)35(31,32)30-21-26-9-27-34-21/h1-9H,(H3,25,28,29)(H,26,27,30) | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| Purchase
CHEMBL
PC cid
PC sid
UniChem
Patents
Similars
| Article
PubMed
| n/a | n/a | 0.800 | n/a | n/a | n/a | n/a | n/a | n/a |
Xenon Pharmaceuticals, Inc.
Curated by ChEMBL
| Assay Description
Inhibition of full length human Nav1.6 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by... |
ACS Med Chem Lett 7: 277-82 (2016)
Article DOI: 10.1021/acsmedchemlett.5b00447
BindingDB Entry DOI: 10.7270/Q2J1052W |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM161329
(US10087143, Compound 114 | US10738009, Compound 11...)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) | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
Similars
| | n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2TM7G2M |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM374028
((S)-4-((1-benzylpyrrolidin-3-yl)(methyl)amino)-2,6...)Show SMILES CN([C@H]1CCN(Cc2ccccc2)C1)c1cc(F)c(c(F)c1C)S(=O)(=O)Nc1ncns1 |r| Show InChI InChI=1S/C21H23F2N5O2S2/c1-14-18(27(2)16-8-9-28(12-16)11-15-6-4-3-5-7-15)10-17(22)20(19(14)23)32(29,30)26-21-24-13-25-31-21/h3-7,10,13,16H,8-9,11-12H2,1-2H3,(H,24,25,26)/t16-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/a |
Xenon Pharmaceuticals Inc.
US Patent
| Assay Description
Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (Nay's), and... |
US Patent US10815229 (2020)
BindingDB Entry DOI: 10.7270/Q2MS3WTS |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM526223
(4-((2-(azetidin-1-ylmethyl)benzyl)amino)-2,6-diflu...)Show SMILES Cc1c(NCc2ccccc2CN2CCC2)cc(F)c(c1F)S(=O)(=O)Nc1ncns1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2QF8X18 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM526220
(4-((2-(azetidin-1-ylmethyl)benzyl)amino)-3-chloro-...)Show SMILES Fc1cc(NCc2ccccc2CN2CCC2)c(Cl)c(F)c1S(=O)(=O)Nc1ncns1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2QF8X18 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM374028
((S)-4-((1-benzylpyrrolidin-3-yl)(methyl)amino)-2,6...)Show SMILES CN([C@H]1CCN(Cc2ccccc2)C1)c1cc(F)c(c(F)c1C)S(=O)(=O)Nc1ncns1 |r| Show InChI InChI=1S/C21H23F2N5O2S2/c1-14-18(27(2)16-8-9-28(12-16)11-15-6-4-3-5-7-15)10-17(22)20(19(14)23)32(29,30)26-21-24-13-25-31-21/h3-7,10,13,16H,8-9,11-12H2,1-2H3,(H,24,25,26)/t16-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/a |
St. Jude Research Hospital
| Assay Description
Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (Nay's), and... |
J Med Chem 50: 1876-85 (2007)
BindingDB Entry DOI: 10.7270/Q2HM5BRC |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM374028
((S)-4-((1-benzylpyrrolidin-3-yl)(methyl)amino)-2,6...)Show SMILES CN([C@H]1CCN(Cc2ccccc2)C1)c1cc(F)c(c(F)c1C)S(=O)(=O)Nc1ncns1 |r| Show InChI InChI=1S/C21H23F2N5O2S2/c1-14-18(27(2)16-8-9-28(12-16)11-15-6-4-3-5-7-15)10-17(22)20(19(14)23)32(29,30)26-21-24-13-25-31-21/h3-7,10,13,16H,8-9,11-12H2,1-2H3,(H,24,25,26)/t16-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/a |
Xenon Pharmaceuticals Inc.
US Patent
| Assay Description
The following patch voltage clamp electrophysiology studies were performed on representative compounds of the invention using human embryonic kidney ... |
US Patent US10662184 (2020)
BindingDB Entry DOI: 10.7270/Q2MK6GZP |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM374028
((S)-4-((1-benzylpyrrolidin-3-yl)(methyl)amino)-2,6...)Show SMILES CN([C@H]1CCN(Cc2ccccc2)C1)c1cc(F)c(c(F)c1C)S(=O)(=O)Nc1ncns1 |r| Show InChI InChI=1S/C21H23F2N5O2S2/c1-14-18(27(2)16-8-9-28(12-16)11-15-6-4-3-5-7-15)10-17(22)20(19(14)23)32(29,30)26-21-24-13-25-31-21/h3-7,10,13,16H,8-9,11-12H2,1-2H3,(H,24,25,26)/t16-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Sodium currents were measured using the patch clamp technique in the whole-cell configuration using either a PatchXpress automated voltage clamp or m... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2XS5ZK1 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM526223
(4-((2-(azetidin-1-ylmethyl)benzyl)amino)-2,6-diflu...)Show SMILES Cc1c(NCc2ccccc2CN2CCC2)cc(F)c(c1F)S(=O)(=O)Nc1ncns1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
This sodium influx assay employs the use of the cell permeable, sodium sensitive dye ANG2 to quantify sodium ion influx through sodium channels which... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2QF8X18 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM621868
((S)-N-((R or S)-(3- chloro-2,4- difluorophenyl)(5-...)Show SMILES Fc1ccc(C(NC(=O)[C@@H]2CNC(=O)N2)c2cnc(c(Cl)c2)C(F)(F)F)c(F)c1Cl |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 1.10 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
|
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM621868
((S)-N-((R or S)-(3- chloro-2,4- difluorophenyl)(5-...)Show SMILES Fc1ccc(C(NC(=O)[C@@H]2CNC(=O)N2)c2cnc(c(Cl)c2)C(F)(F)F)c(F)c1Cl |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 1.10 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
|
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM621822
((S)-N-((R or S)-(3- choro-4-fluoro- phenyl)(2-(1- ...)Show SMILES Fc1ccc(cc1Cl)[C@H](NC(=O)[C@@H]1CNC(=O)N1)c1csc(n1)C1(CC1)C(F)(F)F |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 1.10 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
|
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM630941
((4S)-N-[((R or S)-5- chloro-6-cyclo- propylpyridin...)Show SMILES Fc1ccc(C(NC(=O)[C@@H]2CNC(=O)N2)c2cnc(C3CC3)c(Cl)c2)c(F)c1Cl |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 1.10 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
|
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM621746
(BDBM621803 | US11802122, Example 7A | US2023031252...)Show SMILES Fc1ccc(nc1C(F)(F)F)C(NC(=O)[C@@H]1CNC(=O)N1)c1ccc(OC(F)(F)F)cc1 |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 1.10 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
|
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM190233
(US9174999, Table 1, Compound 1)Show SMILES NC(=O)OC[C@@H]1NC(=N)N2CCC(O)(O)[C@@]22NC(=N)N[C@@H]12 |r| Show InChI InChI=1S/C10H17N7O4/c11-6-15-5-4(3-21-8(13)18)14-7(12)17-2-1-9(19,20)10(5,17)16-6/h4-5,19-20H,1-3H2,(H2,12,14)(H2,13,18)(H3,11,15,16)/t4-,5-,10-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| KEGG
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| n/a | n/a | 1.10 | n/a | n/a | n/a | n/a | n/a | n/a |
SiteOne Therapeutics
Curated by ChEMBL
| Assay Description
Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay |
J Med Chem 62: 8695-8710 (2019)
Article DOI: 10.1021/acs.jmedchem.8b01906
BindingDB Entry DOI: 10.7270/Q2M90CZD |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM630953
((S)-N-((R or S)-(3- choro-4-fluoro- phenyl)(2-(1- ...)Show SMILES Fc1ccc(cc1Cl)C(NC(=O)[C@@H]1CNC(=O)N1)c1csc(n1)C1(CC1)C(F)(F)F |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 1.10 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
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Citation and Details
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More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM621816
((4S)-N-[((R or S)-5- chloro-6-cyclo- propylpyridin...)Show SMILES Fc1ccc([C@@H](NC(=O)[C@@H]2CNC(=O)N2)c2cnc(C3CC3)c(Cl)c2)c(F)c1Cl |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 1.10 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
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Citation and Details
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More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM621746
(BDBM621803 | US11802122, Example 7A | US2023031252...)Show SMILES Fc1ccc(nc1C(F)(F)F)C(NC(=O)[C@@H]1CNC(=O)N1)c1ccc(OC(F)(F)F)cc1 |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 1.10 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
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Citation and Details
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More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM50597018
(CHEMBL5182397)Show SMILES FC(F)(F)c1cc(ccc1Cl)C(NC(=O)[C@@H]1CNC(=O)C1)c1ccc(Cl)cc1 |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| Article
PubMed
| n/a | n/a | 1.20 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
Article DOI: 10.1021/acsmedchemlett.2c00144
BindingDB Entry DOI: 10.7270/Q2SX6J73 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM621869
((S)-N-((R)-3-chloro-4-(trifluoromethoxy)phenyl)(5-...)Show SMILES FC(F)(F)Oc1ccc(nc1)[C@@H](NC(=O)[C@@H]1CNC(=O)N1)c1ccc(OC(F)(F)F)c(Cl)c1 |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 1.30 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
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Citation and Details
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More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM621859
((S)-N-((R)-(3-chloro-2,4-difluorophenyl)(6-(2,2,2-...)Show SMILES Fc1ccc([C@@H](NC(=O)[C@@H]2CNC(=O)N2)c2ccc(OCC(F)(F)F)nc2)c(F)c1Cl |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 1.30 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
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Citation and Details
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More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM631047
((S)—N—((R)-3-chloro-4-(trifluoromethoxy)...)Show SMILES FC(F)(F)Oc1ccc(nc1)C(NC(=O)[C@@H]1CNC(=O)N1)c1ccc(OC(F)(F)F)c(Cl)c1 |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 1.30 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
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Citation and Details
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More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM631027
((S)—N—((R)-(3-chloro-2,4-difluorophenyl)...)Show SMILES Fc1ccc(C(NC(=O)[C@@H]2CNC(=O)N2)c2ccc(OCC(F)(F)F)nc2)c(F)c1Cl |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 1.30 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM621743
(BDBM621800 | US11802122, Example 5A | US2023031252...)Show SMILES Fc1ccc(C(NC(=O)[C@@H]2CNC(=O)N2)C2CCN(CC2)C2(CC2)C(F)(F)F)c(F)c1Cl |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 1.60 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM621743
(BDBM621800 | US11802122, Example 5A | US2023031252...)Show SMILES Fc1ccc(C(NC(=O)[C@@H]2CNC(=O)N2)C2CCN(CC2)C2(CC2)C(F)(F)F)c(F)c1Cl |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 1.60 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
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Citation and Details
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More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM621873
((S)—N—((R)-(3-chloro-4-(trifluoromethoxy...)Show SMILES FC(F)(F)Oc1ccc(cc1Cl)[C@@H](NC(=O)[C@@H]1CNC(=O)N1)c1cnn(c1)C(F)(F)F |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 1.70 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM631055
((S)—N—((R)-(3-chloro-4-(trifluoromethoxy...)Show SMILES FC(F)(F)Oc1ccc(cc1Cl)C(NC(=O)[C@@H]1CNC(=O)N1)c1cnn(c1)C(F)(F)F |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 1.70 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM458518
(4-((2-((7-azabicyclo[2.2.1]heptan-7-yl)methyl)-6-f...)Show SMILES COc1ccc(F)c(CNc2cc(F)c(c(F)c2)S(=O)(=O)Nc2cscn2)c1CN1C2CCC1CC2 Show InChI InChI=1S/C24H25F3N4O3S2/c1-34-22-7-6-19(25)17(18(22)11-31-15-2-3-16(31)5-4-15)10-28-14-8-20(26)24(21(27)9-14)36(32,33)30-23-12-35-13-29-23/h6-9,12-13,15-16,28,30H,2-5,10-11H2,1H3 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
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| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 2 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
The following patch voltage clamp electrophysiology studies may be performed on representative compounds of the invention using human embryonic kidne... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2BP0603 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM374029
((S)-4-((1-benzylpyrrolidin-3-yl)(methyl)amino)-2,6...)Show SMILES CN([C@H]1CCN(Cc2cccc(C)n2)C1)c1cc(F)c(c(F)c1C)S(=O)(=O)Nc1ncns1 |r| Show InChI InChI=1S/C21H24F2N6O2S2/c1-13-5-4-6-15(26-13)10-29-8-7-16(11-29)28(3)18-9-17(22)20(19(23)14(18)2)33(30,31)27-21-24-12-25-32-21/h4-6,9,12,16H,7-8,10-11H2,1-3H3,(H,24,25,27)/t16-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 2 | n/a | n/a | n/a | n/a | n/a | n/a |
St. Jude Research Hospital
| Assay Description
Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (Nay's), and... |
J Med Chem 50: 1876-85 (2007)
BindingDB Entry DOI: 10.7270/Q2HM5BRC |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM526197
(4-((2-(azetidin-1-ylmethyl)-6-fluorobenzyl)amino)-...)Show SMILES Cc1c(NCc2c(F)cccc2CN2CCC2)cc(F)c(c1F)S(=O)(=O)Nc1cscn1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
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GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 2 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2QF8X18 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM161373
(US10087143, Compound 158 | US10738009, Compound 15...)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) | PDB
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KEGG
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| PC cid
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UniChem
Similars
| | n/a | n/a | 2 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2TM7G2M |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM526227
(5-chloro-2-fluoro-4-(((6-fluoro-1H-indazol-7-yl)me...)Show SMILES Fc1ccc2cn[nH]c2c1CNc1cc(F)c(cc1Cl)S(=O)(=O)Nc1cscn1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
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| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 2 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2QF8X18 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM458321
((R)-3-fluoro-4-methyl-5-((1-(1-phenylethyl)piperid...)Show SMILES C[C@@H](N1CCC(CC1)Oc1cnc(c(F)c1C)S(=O)(=O)Nc1cscn1)c1ccccc1 |r| Show InChI InChI=1S/C22H25FN4O3S2/c1-15-19(12-24-22(21(15)23)32(28,29)26-20-13-31-14-25-20)30-18-8-10-27(11-9-18)16(2)17-6-4-3-5-7-17/h3-7,12-14,16,18,26H,8-11H2,1-2H3/t16-/m1/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 2 | n/a | n/a | n/a | n/a | n/a | n/a |
Xenon Pharmaceuticals Inc.
US Patent
| Assay Description
This sodium influx assay employs the use of the cell permeable, sodium sensitive dye ANG2 to quantify sodium ion influx through sodium channels which... |
US Patent US10752623 (2020)
BindingDB Entry DOI: 10.7270/Q26H4MGW |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM374029
((S)-4-((1-benzylpyrrolidin-3-yl)(methyl)amino)-2,6...)Show SMILES CN([C@H]1CCN(Cc2cccc(C)n2)C1)c1cc(F)c(c(F)c1C)S(=O)(=O)Nc1ncns1 |r| Show InChI InChI=1S/C21H24F2N6O2S2/c1-13-5-4-6-15(26-13)10-29-8-7-16(11-29)28(3)18-9-17(22)20(19(23)14(18)2)33(30,31)27-21-24-12-25-32-21/h4-6,9,12,16H,7-8,10-11H2,1-3H3,(H,24,25,27)/t16-/m0/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 2 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description
Sodium currents were measured using the patch clamp technique in the whole-cell configuration using either a PatchXpress automated voltage clamp or m... |
Citation and Details
BindingDB Entry DOI: 10.7270/Q2XS5ZK1 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM458308
((R)-3-fluoro-N-(6-fluoropyridin-2-yl)-4-methyl-5-(...)Show SMILES C[C@@H](N1CCC(CC1)N(C)c1cnc(c(F)c1C)S(=O)(=O)Nc1cccc(F)n1)c1ccccc1 |r| Show InChI InChI=1S/C25H29F2N5O2S/c1-17-21(16-28-25(24(17)27)35(33,34)30-23-11-7-10-22(26)29-23)31(3)20-12-14-32(15-13-20)18(2)19-8-5-4-6-9-19/h4-11,16,18,20H,12-15H2,1-3H3,(H,29,30)/t18-/m1/s1 | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 2 | n/a | n/a | n/a | n/a | n/a | n/a |
Xenon Pharmaceuticals Inc.
US Patent
| Assay Description
This sodium influx assay employs the use of the cell permeable, sodium sensitive dye ANG2 to quantify sodium ion influx through sodium channels which... |
US Patent US10752623 (2020)
BindingDB Entry DOI: 10.7270/Q26H4MGW |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM458518
(4-((2-((7-azabicyclo[2.2.1]heptan-7-yl)methyl)-6-f...)Show SMILES COc1ccc(F)c(CNc2cc(F)c(c(F)c2)S(=O)(=O)Nc2cscn2)c1CN1C2CCC1CC2 Show InChI InChI=1S/C24H25F3N4O3S2/c1-34-22-7-6-19(25)17(18(22)11-31-15-2-3-16(31)5-4-15)10-28-14-8-20(26)24(21(27)9-14)36(32,33)30-23-12-35-13-29-23/h6-9,12-13,15-16,28,30H,2-5,10-11H2,1H3 | PDB
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KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| US Patent
| n/a | n/a | 2 | n/a | n/a | n/a | n/a | n/a | n/a |
Xenon Pharmaceuticals Inc.
US Patent
| Assay Description
In general, Trex HEK293 cells were stably transfected with an inducible expression vector containing the full-length cDNA coding for the desired huma... |
US Patent US10745392 (2020)
BindingDB Entry DOI: 10.7270/Q2NK3J21 |
More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM630925
((S)—N—((R)-(3-chlorophenyl)(4-(trifluoro...)Show SMILES FC(F)(F)Oc1ccc(cc1)C(NC(=O)[C@@H]1CNC(=O)N1)c1cccc(Cl)c1 |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
DrugBank
GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 2 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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More data for this
Ligand-Target Pair | |
Sodium channel protein type 8 subunit alpha
(Homo sapiens (Human)) | BDBM630925
((S)—N—((R)-(3-chlorophenyl)(4-(trifluoro...)Show SMILES FC(F)(F)Oc1ccc(cc1)C(NC(=O)[C@@H]1CNC(=O)N1)c1cccc(Cl)c1 |r| | PDB
Reactome pathway
KEGG
UniProtKB/SwissProt
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GoogleScholar
AffyNet
| PC cid
PC sid
UniChem
| | n/a | n/a | 2 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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More data for this
Ligand-Target Pair | |
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