Target Poor or Non Binder(s) Information

Target General Information

Target ID

T17569

Target Info

Target Name

Voltage-gated potassium channel Kv1.5 (KCNA5)

Synonyms

Voltage-gatedpotassium channel subunit Kv1.5; Voltage-gated potassium channel subunit Kv1.5; Voltage-gated potassium channel HK2; Potassium voltage-gated channel subfamily A member 5; Potassium channel Kv1.5; HPCN1; HK2; 02-Sensitive Potassium Channel Kv1.5

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Target Type

Successful Target

Gene Name

KCNA5

Biochemical Class

Voltage-gated ion channel

UniProt ID

P22460

Poor Binders of This Target (in total, 21 binders)

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Compound Name

Flecainide

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Approved

Compound Info

Synonyms

flecainide; 54143-55-4; Flecaine; Tambocor; Flecainida; Flecainidum; (+-)-Flecainide; Flecainidum [INN-Latin]; Flecainida [INN-Spanish]; N-(piperidin-2-ylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide; Flecainide [INN:BAN]; CCRIS 313; Benzamide, N-(2-piperidinylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)-; C17H20F6N2O3; CHEMBL652; N-(2-Piperidinylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide; CHEBI:75984; DJBNUMBKLMJRSA-UHFFFAOYSA-N; NCGC00015443-06; DSSTox_CID_3054; DSSTox_RID_76854; DSSTox_GSID_23054; (-)-Flecainide; Flecaine; Almarytm (TN); Apocard (TN); Ecrinal (TN); Flecainide (INN); Tambocor (TN); N-(piperidin-2-ylmethyl)-2,5-bis[(2,2,2-trifluoroethyl)oxy]benzamide; Ic Flecainide

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Activity

IC50 = 51000 nM

[1]

Compound Name

N-[3-(N-(6-Fluoro-1,1-dioxo-1,2-benzothiazol-3-yl)anilino)-2,2-dimethylpropyl]-1-benzofuran-2-carboxamide

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Investigative

Compound Info

Synonyms

CHEMBL1290620; BDBM50331511

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Activity

IC50 ~ 50000 nM

[2]

Compound Name

N-[3-(N-(6-Fluoro-1,1-dioxo-1,2-benzothiazol-3-yl)anilino)-2,2-dimethylpropyl]-1-methylpiperidine-4-carboxamide

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Investigative

Compound Info

Synonyms

CHEMBL1290281; BDBM50331509

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Activity

IC50 ~ 50000 nM

[2]

Compound Name

1-[[3-(N-(6-Fluoro-1,1-dioxo-1,2-benzothiazol-3-yl)anilino)-2,2-dimethylpropyl]carbamoyl]cyclopropane-1-carboxylic acid

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Investigative

Compound Info

Synonyms

CHEMBL1289187; BDBM50331508

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Activity

IC50 ~ 50000 nM

[2]

Compound Name

N-[3-(N-(6-Fluoro-1,1-dioxo-1,2-benzothiazol-3-yl)anilino)-2,2-dimethylpropyl]-3-hydroxypyridine-4-carboxamide

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Investigative

Compound Info

Synonyms

CHEMBL1289189; BDBM50331512

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Activity

IC50 ~ 50000 nM

[2]

Compound Name

N-[3-(N-(6-Fluoro-1,1-dioxo-1,2-benzothiazol-3-yl)anilino)-2,2-dimethylpropyl]piperidine-3-carboxamide

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Investigative

Compound Info

Synonyms

CHEMBL1290397; BDBM50331510

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Activity

IC50 ~ 50000 nM

[2]

Compound Name

4-Methoxy-N-(2,4,6-trimethylphenyl)benzenesulfonamide

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Investigative

Compound Info

Synonyms

GSK137647A; GSK 137647; GSK-137647A; N-mesityl-4-methoxybenzenesulfonamide; CHEMBL3311308; MFCD02007969; 4-methoxy-N-(2,4,6-trimethylphenyl)-benzenesulfonamide; CBMicro_012617; Oprea1_349531; Oprea1_545891; SCHEMBL19357604; KS-00000TIW; AOB2991; ZINC184126; BCP17136; EX-A1097; GSK 137647A; SMSF0014079; BDBM50044849; STK899558; AKOS003261220; CB15818; CS-5549; GSK-137647; MCULE-5583867808; N-mesityl-4-methoxy-1-benzenesulfonamide; NCGC00387253-02; NCGC00387253-05; AK240703; AS-16737; HY-19995; BIM-0012523.P001; FFA4 (GPR120) agonist GSK137647A; B7793; EU-0076636; FT-0700296; S0001; ST50719559; GSK137647A, >=98% (HPLC); A14542; AJ-292/14925630; SR-01000478738; J-690285; SR-01000478738-1; [(4-methoxyphenyl)sulfonyl](2,4,6-trimethylphenyl)amine; 4-methoxy-N-(2,4,6-trimethylphenyl)benzene-1-sulfonamide; 4-Methoxy-N-(2,4,6-triMethylphenyl)benzenesulfonaMide, 97%

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Activity

IC50 ~ 50118.72 nM

[3]

Compound Name

2-[4-[2-(3,4-Dimethylphenoxy)ethyl]piperazin-1-yl]-N-(1,3-thiazol-2-yl)acetamide

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Investigative

Compound Info

Synonyms

CHEMBL3262829; BDBM50016349

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Activity

IC50 = 50240 nM

[4]

Compound Name

(2-Chlorophenyl)-[4-(2-phenoxyethyl)piperazin-1-yl]methanone

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Investigative

Compound Info

Synonyms

CHEMBL3262812; BDBM50016321; AKOS027526453

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Activity

IC50 = 56750 nM

[4]

Compound Name

2-Morpholino-1,1-di(pyridin-3-yl)propan-1-ol

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Investigative

Compound Info

Synonyms

CHEMBL1090795; SCHEMBL1242050; BDBM50315569; 2-morpholin-4-yl-1,1-dipyridin-3-ylpropan-1-ol

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Activity

IC50 ~ 60000 nM

[5]

Compound Name

2-Morpholin-4-yl-2-phenylethanol

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Investigative

Compound Info

Synonyms

CHEMBL1090791; 2-morpholino-2-phenylethanol; 2-Phenyl-2-morpholinoethanol; SCHEMBL11651599; BDBM50315565

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Activity

IC50 ~ 60000 nM

[5]

Compound Name

2-Methyl-1-morpholino-1-phenylpropan-2-ol

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Investigative

Compound Info

Synonyms

CHEMBL1090792; SCHEMBL12508295; BDBM50315566

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Activity

IC50 ~ 60000 nM

[5]

Compound Name

2-[4-[2-(4-Tert-butylphenoxy)ethyl]piperazin-1-yl]-N-(1,3-thiazol-2-yl)acetamide

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Investigative

Compound Info

Synonyms

CHEMBL3262831; BDBM50016359

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Activity

IC50 = 63180 nM

[4]

Compound Name

2-[(4-Butoxyphenyl)sulfonylamino]-3-(1H-indol-3-yl)propanoic acid

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Investigative

Compound Info

Synonyms

CHEMBL2440391; BDBM50493862

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Activity

IC50 = 65420 nM

[6]

Compound Name

2-[4-(2-Naphthalen-2-yloxyethyl)piperazin-1-yl]-N-(1,3-thiazol-2-yl)acetamide

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Investigative

Compound Info

Synonyms

CHEMBL3262839; BDBM50016365

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Activity

IC50 = 68030 nM

[4]

Compound Name

2-[4-[2-(2,6-Dimethylphenoxy)ethyl]piperazin-1-yl]-N-(1,3-thiazol-2-yl)acetamide

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Investigative

Compound Info

Synonyms

CHEMBL3262830; BDBM50016352

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Activity

IC50 = 85930 nM

[4]

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

[7]

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

[7]

Compound Name

Auglurant

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Investigative

Compound Info

Synonyms

VU0424238; N-(5-fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide; CHEMBL2386850; UNII-GRN8X62ZW2; GRN8X62ZW2; SCHEMBL12499337; VU238; EX-A2936; BDBM50257064; MFCD28386341; VU 238; 2-PyridinecarboxaMide, N-(5-fluoro-2-pyridinyl)-6-Methyl-4-(5-pyriMidinyloxy)-; HY-16617; CS-0009173; VU 0424238; YU-0424238; J3.655.475D; 2-PyridinecarboxaMide,N-(5-fluoro-2-pyridinyl)-6-Methyl-4-(5-pyriMidinyloxy)-; N-(5-Fluoro-2-pyridinyl)-6-methyl-4-(5-pyrimidinyloxy)-2-pyridinecarboxamide; N-(5-fluoropyridin-2-yl)-6-methyl-4-pyrimidin-5-yloxypyridine-2-carboxamide

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Activity

IC50 ~ 100000 nM

[8]

Compound Name

Methyl 2-[(4-butoxyphenyl)sulfonylamino]-3-phenylpropanoate

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Investigative

Compound Info

Synonyms

CHEMBL2440390; BDBM50493847

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Activity

IC50 = 109740 nM

[6]

Compound Name

2-[3-[2-[(4-Butoxyphenyl)sulfonylamino]ethyl]indol-1-yl]-N-(4-chlorophenyl)acetamide

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Investigative

Compound Info

Synonyms

CHEMBL2440397; BDBM50493876

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Activity

IC50 = 185140 nM

[6]

Click to Show/Hide the Information of All Poor Binders

Non Binders of This Target (in total, 2 non binders)

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Compound Name

Lidocaine

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Approved

Compound Info

Synonyms

Alphacaine; Anestacon; Cappicaine; Cuivasil; Dalcaine; Dentipatch; DermaFlex; Dilocaine; Duncaine; EMBOLEX; Esracaine; Gravocain; Isicaina; Isicaine; Jetocaine; LIDOPEN; LQZ; Lanabiotic; Leostesin; Lidocaina; Lidocainum; Lidocaton; Lidoderm; Lignocaine; Lignocainum; Lingocaine; Maricaine; Octocaine; Remicaine; Rucaina; Solcain; Xilina; Xilocaina; Xllina; Xycaine; Xylestesin; Xylesthesin; Xylocain; Xylocaine; Xylocard; Xylocitin; Xylotox; Zingo; After Burn Double Strength Gel; After Burn Double Strength Spray; After Burn Gel; After Burn Spray; Anestacon Jelly; Cito optadren; Emla Cream; Lidocaine Carbonate; Lidocaine Hydrocarbonate; Lidocaine Monohydrochloride; Norwood Sunburn Spray; Rocephin Kit; Solarcaine aloe extraburn relief cream; Xilocaina [Italian]; Xylocaine Dental Ointment; Xylocaine Endotracheal; Xylocaine Test Dose; Xylocaine Viscous; CDS1_000283; L1026_SIGMA; Xylocaine CO2; Dentipatch (TN); ELA-Max; L-Caine; Lida-Mantle; Lidocaina [INN-Spanish]; Lidocaine (VAN); Lidocainum [INN-Latin]; Lidoject-1; Lidoject-2; Octocaine-100; Octocaine-50; Xylocaine (TN); Xylocaine 5% Spinal; Xylocaine-Mpf; Xylocaine-Mpf with Glucose; Xyloneural (free base); Zilactin-L; Lidocaine [USAN:INN:JAN]; Diethylaminoaceto-2,6-xylidide; Lidocaine (JP15/USP/INN); Alfa-Dietilamino-2,6-dimetilacetanilide; Alfa-Dietilamino-2,6-dimetilacetanilide [Italian]; Alpha-Diethylamino-2,6-dimethylacetanilide; Alpha-Diethylaminoaceto-2,6-xylidide; LIDOCAINE (73-58-6 (MONOHYDROCHLORIDE); Omega-Diethylamino-2,6-dimethylacetanilide; Alpha-(Diethylamino)-2,6-acetoxylidide; N-(2,6-dimethylphenyl)-N(2),N(2)-diethylglycinamide; N-(2,6-dimethylphenyl)-N~2~,N~2~-diethylglycinamide; 2-(Diethylamino)-2',6'-acetoxylidide; 2-(Diethylamino)-N-(2,6-dimethylphenyl)acetamide; 2-Diethylamino-N-(2,6-dimethyl-phenyl)-acetamide; 2-Diethylamino-N-(2,6-dimethylphenyl)acetamide

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Activity

IC50 = 2188000 nM

[1]

Compound Name

1-[(2S)-2-Amino-2-[(1r,4S)-4-[({3-oxo-2H,3H,4H-pyrido[3,2-b][1,4]oxazin-6-yl}methyl)amino]cyclohexyl]ethyl]-7-methoxy-1,2-dihydro-1,5-naphthyridin-2-one

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Investigative

Compound Info

Synonyms

CHEMBL3355575; SCHEMBL1375971; SCHEMBL1375976; BDBM50023582; SB19210

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Activity

IC50 > 333000 nM

[7]

References

Top

REF 1

Synthesis and biological studies of novel 2-aminoalkylethers as potential antiarrhythmic agents for the conversion of atrial fibrillation. J Med Chem. 2007 Jun 14;50(12):2818-41.

REF 2

Substituted N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs as potent Kv1.3 ion channel blockers. Part 2. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6989-92.

REF 3

Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). Bioorg Med Chem Lett. 2014 Jul 15;24(14):3100-3.

REF 4

Discovery of 1-aryloxyethyl piperazine derivatives as Kv1.5 potassium channel inhibitors (part I). Eur J Med Chem. 2014 Jun 23;81:89-94.

REF 5

Discovery of triarylethanolamine inhibitors of the Kv1.5 potassium channel. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2493-6.

REF 6

Design and bio-evaluation of indole derivatives as potent Kv1.5 inhibitors. Bioorg Med Chem. 2013 Nov 1;21(21):6466-76.

REF 7

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.

REF 8

Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation. J Med Chem. 2017 Jun 22;60(12):5072-5085.

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