Target Poor or Non Binder(s) Information

Target General Information

Target ID

T85272

Target Info

Target Name

Voltage-gated potassium channel Kv1.1 (KCNA1)

Synonyms

Voltagegated potassium channel subunit Kv1.1; Voltagegated potassium channel HBK1; Voltagegated K(+) channel HuKI; Potassium voltagegated channel subfamily A member 1; KCNA1

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Target Type

Literature-reported Target

Gene Name

KCNA1

Biochemical Class

Voltage-gated ion channel

UniProt ID

Q09470

Poor Binders of This Target (in total, 3 binders)

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Compound Name

Dalfampridine

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Approved

Compound Info

Synonyms

Ampyra (TN)

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Activity

IC50 = 89000 nM

[1]

Compound Name

Nifedipine

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Approved

Compound Info

Synonyms

Adalat; Adalate; Adapine; Adapress; Afeditab; Alat; Aldipin; Alfadal; Alonix; Angipec; Anifed; Anpine; Aprical; Bonacid; Calcibloc; Calcigard; Calcilat; Camont; Cardifen; Cardilat; Cardionorm; Chronadalate; Citilat; Coracten; Coral; Cordafen; Cordaflex; Cordalat; Cordicant; Cordilan; Cordipin; Cordipine; Corinfar; Corotrend; Corynphar; Depin; Dignokonstant; Dilafed; Dipinkor; Duranifin; Ecodipi; Ecodipin; Emaberin; Fedcor; Fenamon; Fenigidin; Fenihidin; Fenihidine; Glopir; Hadipin; Hexadilat; Infedipin; Introcar; Kordafen; Korinfar; Macorel; Megalat; Myogard; Nedipin; Nicardia; Nifangin; Nifar; Nifdemin; Nifebene; Nifecard; Nifecor; Nifedepat; Nifediac; Nifedical; Nifedicor; Nifedin; Nifedine; Nifedipino; Nifedipinum; Nifedipres; Nifelan; Nifelat; Nifelate; Nificard; Nifidine; Nifipen; Niphedipine; Orix; Oxcord; Pidilat; Procardia; Sepamit; Tibricol; Vascard; Zenusin; AWD Pharma Brand of Nifedipine; Adalat CC; Adalat CR; Adalat Crono; Adalat FT; Adalat GITS; Adalat LA; Adalat LP; Adalat Oros; Adalat PA; Adalat Retard; Adalat XL; Adalate LP; Adcock Ingram Brand of Nifedipine; Adipine XL; Afeditab CR; Alonix S; Aprical long; Bayer Brand of Nifedipine; Chronadalate LP; Coracten XL; Ecodipin E; Fedcor Retard; Fenamon SR; Fortipine LA; KRKA Brand of Nifedipine; Nifedical XL; Nifedipine Bayer Brand; Nifedipine GTIS; Nifedipine KRKA Brand; Nifedipine Monohydrochloride; Nifedipine Orion Brand; Nifedipine Pfizer Brand; Nifedipine Retard; Nifedirex LP; Nifelat Q; Nifensar XL; Orion Brand of Nifedipine; Pfizer Brand of Nifedipine; Procardia XL; Slofedipine XL; Tensipine MR; Adalat 10; Adalat 20; Adalat 5; Adalat GITS 30; Bay1040; N 7634; N1fedilat; Adalat (TN); Afeditab CR (TN); Alpha-Nifedipine Retard;Apo-Nifed; Bay-1040; KB-1712P; Monohydrochloride, Nifedipine; Nifedical (TN); Nifedipine-GTIS; Nifedipino [INN-Spanish]; Nifedipinum [INN-Latin]; Procardia (TN); Bay-a-1040; Nifedipine (JP15/USP/INN); Nifedipine [USAN:BAN:INN:JAN]

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Activity

IC50 = 96000 nM

[1]

Compound Name

Diltiazem

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Approved

Compound Info

Synonyms

Acalix; Adizem; Aldizem; Anoheal; Cardil; Cardizem; Citizem; Dilacor; Dilcontin; Dilren; Diltia; Diltiazemum; Dilticard; Diltzac; Dilzen; Endrydil; Viazem; Cardizen LA; Incoril AP; Tiazac Tildiem; Tiazac XC; Adizem (TN); Altiazem (TN); Angiozem (TN); Angizem (TN); Angizem CD (TN); Apo-Diltiaz; Cardizem (Hydrochloride); Cardizem (TN); Cartia XT (TN); Dilacor-XR; Dilatam (TN); Dilatem (TN); Dilcardia (TN); Dilcontin SR (TN); Dilt-cd; Dilta-Hexal; Diltelan (TN); Diltiazem (INN); Diltiazem [INN:BAN]; Diltiazemum [INN-Latin]; Diltime (TN); Dilzem (TN); Dyalec (TN); Filazem (TN); Herben (TN); Nu-Diltiaz; Progor (TN); RG 83606 (Hydrochloride); Surazem (TN); Tiamate (TN); Tiazac (TN); Tiazac XC (TN); Tildiem (TN); Vasmulax (TN); Viazem (TN); Zandil (TN); Zemtrial (TN); D-cis-Diltiazem; MK-793 (Malate); [(2S,3S)-5-(2-dimethylaminoethyl)-2-(4-methoxyphenyl)-4-oxo-2,3-dihydro-1,5-benzothiazepin-3-yl] acetate; Acetic acid (2S,3S)-5-(2-dimethylamino-ethyl)-2-(4-methoxy-phenyl)-4-oxo-2,3,4,5-tetrahydro-benzo[b][1,4]thiazepin-3-yl ester; (+)-cis-5-[2-(dimethylamino)ethyl]-2,3-dihydro-3-hydroxy-2-(p-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one acetate ester; (2S,3S)-5-(2-(dimethylamino)ethyl)-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]thiazepin-3-yl acetate; (2S,3S)-5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate; (2S,3S)-5-[2-(dimethylamino)ethyl]-2-[4-(methyloxy)phenyl]-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate; (2S-cis)-3-(acetyloxy)-5-[2-(dimethylamino)ethyl]-2,3-dihydro-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one

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Activity

IC50 = 144000 nM

[1]

Non Binders of This Target (in total, 1 non 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 = 209000 nM

[1]

References

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REF 1

A Rational Design of a Selective Inhibitor for Kv1.1 Channels Prevalent in Demyelinated Nerves That Improves Their Impaired Axonal Conduction. J Med Chem. 2017 Mar 23;60(6):2245-2256.

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