Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T76914 | Target Info | |||
| Target Name | Voltage-gated potassium channel Kv1.3 (KCNA3) | ||||
| Synonyms |
Voltage-gated potassium channel subunit Kv1.3; Voltage-gated Kv1.3 K(+) channel; Voltage-gated K(+) channel Kv1.3; Potassium channel Kv1.3; KCNA3; HuKIII; HPCN3; HLK3; HGK5
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| Target Type | Clinical trial Target | ||||
| Gene Name | KCNA3 | ||||
| Biochemical Class | Voltage-gated ion channel | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 20 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
5-methoxypsoralen
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Phase 3 | Compound Info | ||
| Synonyms |
5-MOP
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| Activity |
IC50 = 101000 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 |
1-[3-(N-(1,1-Dioxo-1,2-benzothiazol-3-yl)anilino)propyl]-3-(4-methylpiperazin-1-yl)urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1290278; BDBM50331441
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| 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 |
N'-(1,1-Dioxo-1,2-benzothiazol-3-yl)-N'-phenylpropane-1,3-diamine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1289849; BDBM50331460; N*1*-(1,1-Dioxo-1H-1lambda*6*-benzo[d]isothiazol-3-yl)-N*1*-phenyl-propane-1,3-diamine
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
N-[3-(N-(1,1-Dioxo-1,2-benzothiazol-3-yl)anilino)propyl]-3-imidazol-1-ylpropanamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1289064; BDBM50331440
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
N-[3-(Benzo[b]thiophen-3-yl-phenyl-amino)-propyl]-4-fluoro-benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1289967; BDBM50331457
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| 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-[(1,1-Dioxido-1,2-benzothiazol-3-yl)amino]propyl}-4-fluorobenzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1289297; MLS001124123; SCHEMBL13220678; HMS2988I10; ZINC2835135; BDBM50331444; STL291076; AKOS003211057; MCULE-4526398849; SMR000665752; SR-01000263720; SR-01000263720-1
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
4-Acetyl-N-[3-(N-(1,1-dioxo-1,2-benzothiazol-3-yl)anilino)propyl]piperazine-1-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1290062; BDBM50331439
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|
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
N-[3-(4-Cyano-N-(1,1-dioxo-1,2-benzothiazol-3-yl)anilino)propyl]-4-fluorobenzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1290617; BDBM50331442
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|
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
N-[3-(3-Cyano-N-(1,1-dioxo-1,2-benzothiazol-3-yl)anilino)propyl]-4-fluorobenzamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL1290735; BDBM50331443
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|
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| 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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|
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| Activity |
IC50 ~ 50000 nM
|
[2] | |||
| Compound Name |
4-(N-(1,1-Dioxo-1,2-benzothiazol-3-yl)anilino)butanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1289742; BDBM50331459; 4-[(1,1-Dioxo-1H-1lambda*6*-benzo[d]isothiazol-3-yl)-phenyl-amino]-butyric acid
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
1-(3,3-Diphenylpropyl)piperidin-4-ol
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2205332; SCHEMBL10039407; BDBM50401659
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| Activity |
IC50 = 75000 nM
|
[4] | |||
| Compound Name |
4-(3-Hydroxypiperidin-1-yl)-2,2-diphenylbutanenitrile
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2205331; BDBM50401660
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| Activity |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
4-(4-Methoxypiperidin-1-yl)-2,2-diphenylbutanenitrile
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2205335; BDBM50401656
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| Activity |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
1-(3-Phenylpropyl)piperidin-4-ol
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2205333; SCHEMBL7983946; BDBM50401658; ZINC41233270; AKOS009078151; MCULE-8948439518; Z204702930
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|
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| Activity |
IC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
4-(4-Aminopiperidin-1-yl)-2,2-diphenylbutanenitrile
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2205336; BDBM50401655
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|
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| Activity |
IC50 ~ 100000 nM
|
[4] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 1 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Ethyl 1-(3-cyano-3,3-diphenylpropyl)piperidine-4-carboxylate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2205322; BDBM50401669
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|
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| Activity |
IC50 = 230000 nM
|
[4] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | 4-Phenoxybutoxy-substituted heterocycles--a structure-activity relationship study of blockers of the lymphocyte potassium channel Kv1.3. Eur J Med Chem. 2009 May;44(5):1838-52. | ||||
| 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 | N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs as potent Kv1.3 inhibitors. Part 1. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6983-8. | ||||
| REF 4 | Structure-activity relationship exploration of Kv1.3 blockers based on diphenoxylate. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7106-9. | ||||
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