Target Poor or Non Binder(s) Information

Target General Information

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Target ID

T74500

Target Info

Target Name

Voltage-gated potassium channel Kv4.3 (KCND3)

Synonyms

Voltage-gated potassium channel subunit Kv4.3; KCND3

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Target Type

Successful Target

Gene Name

KCND3

Biochemical Class

Voltage-gated ion channel

UniProt ID

Q9UK17

Poor Binders of This Target (in total, 10 binders)

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Compound Name

Solifenacin

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Approved

Compound Info

Synonyms

Vesicare; Vesikur; Solifenacin succinate; Solifenacin succinate [USAN]; YM 905; Solifenacin (INN); Solifenacin [INN:BAN]; Vesicare (TN); YM-53705; YM-67905; YM-905; Quinuclidin-3'-yl-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylatemonosuccinate; [(3R)-1-azabicyclo[2.2.2]octan-3-yl] (1S)-1-phenyl-3,4-dihydro-1H-isoquinoline-2-carboxylate; Butanedioic acid, compd with (1S)-(3R)-1-azabicyclo(2.2.2)oct-3-yl 3,4-dihydro-1-phenyl-2(1H)-isoquinolinecarboxylate (1:1); Butanedioic acid, cmpd. with (1S)-(3R)-1-azabicyclo(2.2.2)oct-3-yl 3,4-dihydro-1-phenyl-2(1H)-isoquinolinecarboxylate (1:1); 1-azabicyclo[2.2.2]oct-8-yl (1S)-1-phenyl-3,4-dihydro-1H-isoquinoline-2-carboxylate; 1-azabicyclo[2.2.2]octan-3-yl (1S)-1-phenyl-3,4-dihydro-1H-isoquinoline-2-carboxylate; 2(1H)-Isoquinolinecarboxylic acid, 3,4-dihydro-1-phenyl-, (3R)-1-azabicyclo(2.2.2)oct-3-yl ester, (1S)-, butanedioate (1:1)

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Activity

IC50 = 50118.72 nM

[1]

Compound Name

Exjade

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Approved

Compound Info

Synonyms

Deferasirox

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Activity

IC50 = 50118.72 nM

[1]

Compound Name

Nebivolol

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Approved

Compound Info

Synonyms

Bystolic; Lobivon; Nebilet; Nebilong; Nebipill; Nebivololum; Nubeta; Nebivololum [Latin]; R 67555; Bystolic (TN); Nebicard-5;Nebilet (TN); Nebilong (TN); Nodon (TN); Nubeta (TN); PI-21858; R-67555; R65,824; Nebicard-5 (TN); Nebivolol (USAN/INN); Nebivolol [USAN:INN:BAN]; Alpha,alpha'-(Iminodimethylene)bis(6-fluoro-2-chromanmethanol); Alpha,alpha'-(Iminobis(methylene))bis(6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol); Alpha,alpha'-(iminobis(methylene))bis(6-fluoro-3,4-dihydro)-2H-1-benzopyran-2-methanol; 1-(6-fluoro-3,4-dihydro-2H-chromen-2-yl)-2-[[2-(6-fluoro-3,4-dihydro-2H-chromen-2-yl)-2-hydroxyethyl]amino]ethanol; 2,2'-iminobis[1-(6-fluoro-3,4-dihydro-2H-chromen-2-yl)ethanol]

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Activity

IC50 = 50118.72 nM

[1]

Compound Name

Paliperidone

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Approved

Compound Info

Synonyms

Xeplion; Invega Sustenna; Paliperidone palmitate; JNS-010; Paliperidone (depot injection, NanoCrystal); Paliperidone (injectable, NanoCrystal), Elan; Paliperidone (depot injection, NanoCrystal), Johnson & Johnson

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Activity

IC50 = 63095.73 nM

[1]

Compound Name

Vardenafil

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Approved

Compound Info

Synonyms

VDN; Levitra (TN); VARDENAFIL, LEVITRA; Vardenafil (INN); 1-((3-(3,4-Dihydro-5-methyl-4-oxo-7-propylimidazo(5,1-f)-as-triazin-2-yl)-4-ethoxyphenyl)sulfonyl)-4-ethylpiperazine; 2-(2-Ethoxy-5-(4-ethylpiperazin-1-yl-1-sulfonyl)phenyl)-5-methyl-7-propyl-3H-imidazo(5,1-f)(1,2,4)triazin-4-one; 2-[2-ethoxy-5-(4-ethylpiperazin-1-yl)sulfonylphenyl]-5-methyl-7-propyl-1H-imidazo[5,1-f][1,2,4]triazin-4-one; 2-{2-ETHOXY-5-[(4-ETHYLPIPERAZIN-1-YL)SULFONYL]PHENYL}-5-METHYL-7-PROPYLIMIDAZO[5,1-F][1,2,4]TRIAZIN-4(1H)-ONE; 2-{2-ethoxy-5-[(4-ethylpiperazin-1-yl)sulfonyl]phenyl}-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4-ol

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Activity

IC50 = 79432.82 nM

[1]

Compound Name

Duloxetine

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Approved

Compound Info

Synonyms

Yentreve; LY 248686; Cymbalta (TN); Duloxetine (INN); Duloxetine [INN:BAN]; Yentreve (TN); Duloxetine, (+)-isomer; (3S)-N-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propan-1-amine; (3S)-N-methyl-3-(naphthalen-1-yloxy)-3-(2-thienyl)propan-1-amine; (3S)-N-methyl-3-naphthalen-1-yloxy-3-thiophen-2-ylpropan-1-amine; (S)-Duloxetine; (S)-N-Methyl-gamma-(1-naphthalenyloxy)-2-thiophenepropanamine

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Activity

IC50 = 100000 nM

[1]

Compound Name

Darunavir

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Approved

Compound Info

Synonyms

206361-99-1; TMC114; Prezista; TMC-114; UIC-94017; Darunavirum; TMC 114; Darunavirum [INN-Latin]; UNII-YO603Y8113; AIDS073035; CHEMBL1323; (3R,3AS,6AR)-HEXAHYDROFURO[2,3-B]FURAN-3-YL(1S,2R)-3-[[(4-AMINOPHENYL)SULFONYL](ISOBUTYL)AMINO]-1-BENZYL-2-HYDROXYPROPYLCARBAMATE; CHEBI:367163; Darunavir-d9; YO603Y8113; (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ((2S,3R)-4-(4-amino-N-isobutylphenylsulfonamido)-3-hydroxy-1-phenylbutan-2-yl)carbamate; NCGC00168773-01; (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl; Darunavirum; Darunavir [USAN]; UIC 94017; Prezista(TM); UIC-96017; Darunavir (USAN/INN); Carbamic acid, [(1S,2R)-3-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)propyl]-, (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ester; {(1S,2R)-3-[(4-Amino-benzenesulfonyl)-isobutyl-amino]-1-benzyl-2-hydroxy-propyl}-carbamic acid (3R,3aS,6aR)-(hexahydro-furo[2,3-b]furan-3-yl) ester; [(S)-3-[(4-Amino-benzenesulfonyl)-isobutyl-amino]-2-hydroxy-1-((R)-phenylmethyl)-propyl]-carbamic acid (3R,3aS,6aR)-(hexahydro-furo[2,3-b]furan-3-yl) ester; N-((1S,2R)-3-(((4-Aminophenyl)sulfonyl)(2-methylpropyl)amino)-2-hydroxy-1-benzylpropyl)((1S,2R,5R)-4,6-dioxabicyclo(330)oct-2-yloxy)carboxamide; [(3aS,4R,6aR)-2,3,3a,4,5,6a-hexahydrofuro[2,3-b]furan-4-yl] N-[(2S,3R)-4-[(4-aminophenyl)sulfonyl-(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamate; (3-((4-aminobenzenesulfonyl)isobutylamino)-1-benzyl-2-hydroxypropyl)carbamic acid hexahydrofuro(2,3-b)furan-3-yl ester; (3R,3aS,6aR)-Hexahydrofuro(2,3-b)furan-3-yl N-((1S,2R)-1-benzyl-2-hydroxy-3-(N1-isobutylsulfanilamido)propyl)carbamate; (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl N-((1S,2R)-1-benzyl-2-hydroxy-3-(N(1)-isobutylsulfanilamido)propyl)carbamate; (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3R)-4-{[(4-aminophenyl)sulfonyl](2-methylpropyl)amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate; (3R,3aS,6aR)-tetrahydro-2H-furo[2,3-b]furan-3-yl (2S,3R)-4-(4-amino-N-isobutylphenylsulfonamido)-3-hydroxy-1-phenylbutan-2-ylcarbamate; (3R,3aS,6aR)-tetrahydro-2H-furo[2,3-b]furan-3-yl (2S,3R)-4-(4-amino-N-neopentylphenylsulfonamido)-3-hydroxy-1-phenylbutan-2-ylcarbamate

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Activity

IC50 = 100000 nM

[1]

Compound Name

PMID28460551-Compound-2

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Patented

Compound Info

Activity

IC50 = 50118.72 nM

[1]

Compound Name

6-[({1-[2-(7-Methoxy-2-oxoquinoxalin-1(2H)-yl)ethyl]piperidin-4-yl}amino)methyl]-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one

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Investigative

Compound Info

Synonyms

CHEMBL2165063; SCHEMBL708423; BDBM50395399

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Activity

IC50 ~ 100000 nM

[2]

Compound Name

6H-Pyrimido[5,4-b][1,4]oxazin-7(8H)-one, 2-[[[trans-4-[(1R)-1-amino-2-(7-fluoro-2-oxo-1(2H)-quinoxalinyl)ethyl]cyclohexyl]amino]methyl]-

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Investigative

Compound Info

Synonyms

CHEMBL3355573; SCHEMBL1375934; SCHEMBL1375938; BDBM50023589; SB19220

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Activity

IC50 ~ 100000 nM

[2]

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Non Binders of This Target (in total, 13 non binders)

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Compound Name

Ambrisentan

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Approved

Compound Info

Synonyms

Letairis; Ambrisentan [INN]; Gilead brand of ambrisentan; BSF 208075; BSF208075; LU 208075; LU208075; BSF-208075; LU-208075; Benzenepropanoic acid, .alpha.-[(4,6-dimethyl-2-pyrimidinyl)oxy]-.beta.-methoxy-.beta.-phe; (+-)-(2S)-2-((4,6-Dimethylpyrimidin-2-yl)oxy)-3-methoxy-3,3-diphenylpropanoic acid; 2-(4,6-dimethylpyrimidin-2-yl)oxy-3-methoxy-3,3-diphenyl-propanoic acid; 2-(4,6-dimethylpyrimidin-2-yl)oxy-3-methoxy-3,3-diphenylpropanoic acid; 2-[(4,6-dimethylpyrimidin-2-yl)oxy]-3-methoxy-3,3-diphenylpropanoic acid

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Activity

IC50 = 251188.64 nM

[1]

Compound Name

Dasatinib

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Approved

Compound Info

Synonyms

Sprycel (TN); BMS 354825; BMS-354825; BMS-354825, Sprycel, BMS354825, Dasatinib; BMS354825; Dasatinib (USAN); Dasatinib [USAN]; Dasatinib anhydrous; Dasatinib, BMS 354825; Dasatinibum; Sprycel; Spyrcel

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Activity

IC50 = 316227.77 nM

[1]

Compound Name

SILODOSIN

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Approved

Compound Info

Synonyms

Silodosin; 160970-54-7; Rapaflo; Urief; Silodyx; Urorec; KMD-3213; Silodosin-d6; UNII-CUZ39LUY82; KMD 3213; KAD 3213; CUZ39LUY82; CHEMBL24778; KAD-3213; (R)-1-(3-hydroxypropyl)-5-(2-((2-(2-(2,2,2-trifluoroethoxy)phenoxy)ethyl)amino)propyl)indoline-7-carboxamide; 1-(3-hydroxypropyl)-5-[(2R)-2-[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethylamino]propyl]-2,3-dihydroindole-7-carboxamide; 160970-64-9; Q-102517; Rapflo

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Activity

IC50 = 316227.77 nM

[1]

Compound Name

Rhucin

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Approved

Compound Info

Synonyms

sildenafil; 139755-83-2; VIAGRA; Sildenafil [INN:BAN]; UK-92480; UNII-3M7OB98Y7H; UK-92,480-10; C22H30N6O4S; HSDB 7305; CHEMBL192; UK 92480-10; CHEBI:9139; 3M7OB98Y7H; 1-((3-(4,7-Dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo(4,3-d)pyrimidin-5-yl)-4-ethoxyphenyl)sulfonyl)-4-methylpiperazine; BNRNXUUZRGQAQC-UHFFFAOYSA-N; 5-(2-Ethoxy-5-((4-methylpiperazin-1-yl)sulfonyl)phenyl)-1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one; Sildenafil

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Activity

IC50 = 501187.23 nM

[1]

Compound Name

Alfuzosin

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Approved

Compound Info

Synonyms

Alfusosine; Alfuzosina; Alfuzosine; Alfuzosinum; Alphuzosine; Alfuzosina [Spanish]; Alfuzosine [French]; Alfuzosinum [Latin]; Alfuzosin (INN); Alfuzosin [INN:BAN]; Xatral (TN); N-[3-[(4-amino-6,7-dimethoxyquinazolin-2-yl)-methylamino]propyl]oxolane-2-carboxamide; N-(3-((4-Amino-6,7-dimethoxy-2-quinazolinyl)methylamino)propyl)tetrahydro-2-furancarboxamide; N-{3-[(4-amino-6,7-dimethoxyquinazolin-2-yl)(methyl)amino]propyl}tetrahydrofuran-2-carboxamide

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Activity

IC50 = 1000000 nM

[1]

Compound Name

Eltrombopag

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Approved

Compound Info

Synonyms

Eltrombopag [INN]; SB 497115; SB497115; SB-497115; [1,1'-Biphenyl]-3-carboxylic acid, 3'-[(2Z)-[1-(3,4-dime; Thylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2'-hydroxy-(9CI); (E)-3\'-(2-(1-(3,4-Dimethylphenyl)-3-methyl-5-oxo-1H-pyrazol-4(5H)-ylidene)hydrazinyl)-2\'-hydroxybiphenyl-3-carboxylic acid

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Activity

IC50 = 1584893.19 nM

[1]

Compound Name

Etravirine

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Approved

Compound Info

Synonyms

Intelence; DAPY deriv; Diaminopyrimidine deriv; R 165335; R165335; TMC 125; TMC125; Intelence (TN); Intelence(TM); R-165335; R165335-TMC125; TMC-125; Etravirine (JAN/USAN/INN); TMC-125/R-165335; 4-((6-amino-5-bromo-2-((4-cyanophenyl)amino)-4-pyrimidinyl)oxy)-3,5-dimethyl-benzonitrile; 4-({6-AMINO-5-BROMO-2-[(4-CYANOPHENYL)AMINO]PYRIMIDIN-4-YL}OXY)-3,5-DIMETHYLBENZONITRILE; 4-[6-amino-5-bromo-2-(4-cyanoanilino)pyrimidin-4-yl]oxy-3,5-dimethylbenzonitrile; 65B; ETR

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Activity

IC50 = 3162277.66 nM

[1]

Compound Name

Raltegravir

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Approved

Compound Info

Synonyms

RGV; MK 0518; Isentress(TM); K-0518; MK-0518; Raltegravir (INN); N-(2-(4-(4-fluorobenzylcarbamoyl); N-((4-Fluorophenyl)methyl)-1,6-dihydro-5-hydroxy-1-methyl-2-(1-methyl-1-(((5-methyl-1,3,4-oxadiazol-2-yl)carbonyl)amino)ethyl)-6-oxo-4-pyrimidinecarboxamide; RAL

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Activity

IC50 = 5011872.34 nM

[1]

Compound Name

VRX496

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Approved

Compound Info

Synonyms

Nelfinavir; nelfinavir; 159989-64-7; Viracept; Nelfinavir [INN:BAN]; AG1343; UNII-HO3OGH5D7I; AG-1343; C32H45N3O4S; NELFINAVIR MESYLATE AG1343; Viracept (TN); HO3OGH5D7I; CHEBI:7496; AG 1343; NLF; 1UN; 2-[2-HYDROXY-3-(3-HYDROXY-2-METHYL-BENZOYLAMINO)-4-PHENYL SULFANYL-BUTYL]-DECAHYDRO-ISOQUINOLINE-3-CARBOXYLIC ACID TERT-BUTYLAMIDE; (3S-(2(2S*,3S*),3alpha,4abeta,8abeta))-N-(1,1-Dimethylethyl)decahydro-2-(2-hydroxy-3-((3-hydroxy-2-methylbenzoyl)amino)-4-(phenylthio)butyl)-3-isoquinolinecarboxamide; NFV; NFV; Nelfinavir Monomethane Sulfonate; AG1346; Nelfinavir (INN); Nelfinavir [BAN:INN]; AG1343 (*Mesylate salt*); Viracept (TM)(*Mesylate salt*); Met-SDF-1beta & Nelfinavir; Met-Stromal Cell-derived Factor-1beta (Human) & Nelfinavir; (3S,4aS,8aS)-N-tert-butyl-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-phenylsulfanylbutyl]-3,4,4a,5,6,7,8,8a-octahydro-1H-isoquinoline-3-carboxamide

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Activity

IC50 = 5011872.34 nM

[1]

Compound Name

Desvenlafaxine

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Approved

Compound Info

Synonyms

Norvenlafaxine; Desvenlafaxine (INN); Desvenlafaxine [INN:BAN]; O-Desmethylvenlafaxine; WY 45,233; O-DESMETHYLVENLAFAXINE (ODV); WY-45,233

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Activity

IC50 = 5011872.34 nM

[1]

Compound Name

Everolimus

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Approved

Compound Info

Synonyms

Afinitor; Afinitor (TN); CERTICAN(R); Certican; Certican (TN); Everolimus (JAN/USAN/INN); Everolimus [USAN]; MTOR kinase inhibitors; NVP-RAD-001; RAD 001; RAD-001; RAD-001C; RAD001; RAD001, SDZ-RAD, Certican, Zortress, Afinitor, Everolimus; SDZ-RAD; Zortress

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Activity

IC50 = 10000000 nM

[1]

Compound Name

Sitagliptin

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Approved

Compound Info

Synonyms

486460-32-6; Januvia; Xelevia; Sitagliptan; MK-0431; UNII-QFP0P1DV7Z; Tesavel; QFP0P1DV7Z; (3R)-3-AMINO-1-[3-(TRIFLUOROMETHYL)-5H,6H,7H,8H-[1,2,4]TRIAZOLO[4,3-A]PYRAZIN-7-YL]-4-(2,4,5-TRIFLUOROPHENYL)BUTAN-1-ONE; (2R)-4-OXO-4-[3-(TRIFLUOROMETHYL)-5,6-DIHYDRO[1,2,4]TRIAZOLO[4,3-A]PYRAZIN-7(8H)-YL]-1-(2,4,5-TRIFLUOROPHENYL)BUTAN-2-AMINE; CHEBI:40237; (R)-3-AMINO-1-(3-(TRIFLUOROMETHYL)-5,6-DIHYDRO-[1,2,4]TRIAZOLO[4,3-A]PYRAZIN-7(8H)-YL)-4-(2,4,5-TRIFLUOROPHENYL)BUTAN-1-ONE; Janumet; Sitagliptin phosphate; Januvia (TN); Sitagliptin (PropINN); Januvia (merck & Co); (3R)-3-Amino-1-[3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,2,4-triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one; (3R)-3-amino-1-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one; (3R)-3-amino-1-[3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one; Sitagliptin/atovastatin

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Activity

IC50 = 100000000 nM

[1]

Compound Name

MCL-1-specific antisense oligonucleotide + nilotinib (AMN107)

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Investigative

Compound Info

Synonyms

641571-10-0; UNII-F41401512X; Nilotinib (AMN-107); CHEMBL255863; CHEBI:52172; C28H22F3N7O; HHZIURLSWUIHRB-UHFFFAOYSA-N; NSC747599

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Activity

IC50 = 3162277.66 nM

[1]

Click to Show/Hide the Information of All Non Binders

References

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REF 1

Prediction of Thorough QT study results using action potential simulations based on ion channel screens. J Pharmacol Toxicol Methods. Nov-Dec 2014;70(3):246-54.

REF 2

Optimization of physicochemical properties and safety profile of novel bacterial topoisomerase type II inhibitors (NBTIs) with activity against Pseudomonas aeruginosa. Bioorg Med Chem. 2014 Oct 1;22(19):5392-409.

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