Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T24982 | Target Info | |||
| Target Name | Ileal sodium/bile acid cotransporter (SLC10A2) | ||||
| Synonyms |
Solute carrier family 10 member 2; Sodium/taurocholate cotransporting polypeptide, ileal; SLC10A2; Na(+)dependent ileal bile acid transporter; Ileal sodiumdependent bile acid transporter; Ileal Na(+)/bile acid cotransporter; ISBT; IBAT; Apical sodiumdependent bile acid transporter; ASBT
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| Target Type | Successful Target | ||||
| Gene Name | SLC10A2 | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 7 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Ursodeoxycholic acid
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Approved | Compound Info | ||
| Synonyms |
Actigall; Antigall; Arsacol; Delursan; Destolit; Deursil; Litursol; Lyeton; Peptarom; Solutrat; UDCA; UDCS; UrSO; Urosiol; Ursacol; Ursobilin; Ursochol; Ursodamor; Ursodeoxycholate; Ursodiol; Ursofalk; Ursolvan; Ursosan; Acide ursodesoxycholique; Acido ursodeossicolico; Acido ursodeossicolico [Italian]; Acido ursodeoxicolico; Acidum ursodeoxycholicum; Deoxyursocholic Acid; Sodium Ursodeoxycholate; Ursacholic Acid; Urso DS; Urso Forte; Ursodeoxy cholic acid; Ursodesoxycholicacid; Ursodexycholic Acid; Ursodiol [USAN]; IU5; U0030; Urso 250; Acide ursodesoxycholique [INN-French]; Acido ursodeoxicolico [INN-Spanish]; Acidum ursodeoxycholicum [INN-Latin]; Actigall (TN); Cholit-ursan; Deursil (TN); Dom-ursodiol c; ISO-URSODEOXYCHOLIC ACID; PHL-ursodiol c; PMS-ursodiol c; U-9000; Urso (TN); Urso Forte (TN); Ursodiol (USP); Ursosan (TN); Ursodeoxycholic acid (JP15/INN); Ursodeoxycholic acid, UDCA, Ursosan, Ursofalk, Urso Forte, Udiliv, Ursodiol; Cholan-24-oic acid, 3,7-dihydroxy-, (3-alpha,5-beta,7-beta)-(9CI); (3alpha,5beta,7beta)-3,7-dihydroxycholan-24-oic acid; (3alpha,5beta,7beta,8xi)-3,7-dihydroxycholan-24-oic acid; (4R)-4-[(3R,5S,7S,8R,9S,10S,13R,14S,17R)-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoic acid; 17-beta-(1-Methyl-3-carboxypropyl)etiocholane-3-alpha,7-beta-diol; 3 alpha,7 beta-Dihydroxy-5 beta-cholan-24-oic Acid; 3,7-Dihydroxycholan-24-oic acid; 3-alpha,7-beta-Dihydroxy-5-beta-cholanoic acid; 3-alpha,7-beta-Dihydroxycholanic acid; 3-alpha,7-beta-Dioxycholanic acid; 3alpha,7beta-Dihydroxy-5beta-cholan-24-oic acid; 3alpha,7beta-Dihydroxy-5beta-cholanic acid; 5beta-Cholan-24-oic acid-3alpha,7beta-diol; 5beta-Cholanic Acid-3alpha,7beta-diol; 7-beta-Hydroxylithocholic acid; 7beta-Hydroxylithocholic acid
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| Activity |
Ki = 75000 nM
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[1] | |||
| Compound Name |
bromsulphthalein
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Investigative | Compound Info | ||
| Synonyms |
sulfobromophthalein; BSP
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| Activity |
Ki = 144000 nM
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[1] | |||
| Compound Name |
(4R,5R)-7-Amino-3,3-dimethyl-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL196520; BDBM50172635
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| Activity |
IC50 ~ 50000 nM
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[2] | |||
| Compound Name |
2-[[(4R)-4-[(2S,18R)-2,18-Dimethyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4(8),5-dien-17-yl]pentanoyl]amino]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL185179; BDBM50157078
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| Activity |
IC50 = 60000 nM
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[3] | |||
| Compound Name |
2,3,4,5-Tetrahydro-3,3-dibutyl-4alpha-hydroxy-5alpha-(4-methoxyphenyl)-7-(dimethylamino)-1-benzothiepin 1,1-dioxide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL18219; SCHEMBL14904728; BDBM50140283
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| Activity |
IC50 ~ 63000 nM
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[4] | |||
| Compound Name |
4-[[(4S)-4-Carboxy-4-[[(4R)-4-[(3R,5R,7R,8R,9S,10S,13R,14S,17R)-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]butanoyl]amino]benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1170256; BDBM50322494
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| Activity |
Ki = 108000 nM
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[5] | |||
| Compound Name |
3-[[[(4S)-4-Carboxy-4-[[(4R)-4-[(3R,5R,7R,8R,9S,10S,13R,14S,17R)-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]butanoyl]amino]methyl]benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1170257; BDBM50322495
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| Activity |
Ki = 126000 nM
|
[5] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 4 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
2-[[(4R)-4-[(2S,18R)-6-(2-Hydroxyethyl)-2,18-dimethyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4,7-dien-17-yl]pentanoyl]amino]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL185033; BDBM50157076
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| Activity |
IC50 > 300000 nM
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[3] | |||
| Compound Name |
2-[(4R)-4-[(2S,18R)-6-[(3-{[(2S)-2-(6-Methoxynaphthalen-2-yl)propanoyl]oxy}phenyl)methyl]-2,18-dimethyl-6,7-diazapentacyclo[11.7.0.0^{2,10}.0^{4,8}.0^{14,18}]icosa-4,7-dien-17-yl]pentanamido]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL182965; BDBM50157073
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| Activity |
IC50 > 300000 nM
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[3] | |||
| Compound Name |
2-[(4R)-4-[(2S,12R,18R)-12-Hydroxy-6-[(3-{[(2S)-2-(6-methoxynaphthalen-2-yl)propanoyl]oxy}phenyl)methyl]-2,18-dimethyl-6,7-diazapentacyclo[11.7.0.0^{2,10}.0^{4,8}.0^{14,18}]icosa-4,7-dien-17-yl]pentanamido]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL362668; BDBM50157080
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| Activity |
IC50 > 300000 nM
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[3] | |||
| Compound Name |
2-[[(4R)-4-[(2S,12R,18R,19S)-12,19-Dihydroxy-6-[(3-hydroxyphenyl)methyl]-2,18-dimethyl-6,7-diazapentacyclo[11.7.0.02,10.04,8.014,18]icosa-4,7-dien-17-yl]pentanoyl]amino]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL179911; BDBM50157081
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| Activity |
IC50 > 300000 nM
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[3] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Expression and transport properties of the human ileal and renal sodium-dependent bile acid transporter. Am J Physiol. 1998 Jan;274(1 Pt 1):G157-69. | ||||
| REF 2 | Discovery of potent, nonsystemic apical sodium-codependent bile acid transporter inhibitors (Part 1). J Med Chem. 2005 Sep 8;48(18):5837-52. | ||||
| REF 3 | Synthesis and biological evaluation of novel steroidal pyrazoles as substrates for bile acid transporters. Bioorg Med Chem Lett. 2005 Jan 3;15(1):85-7. | ||||
| REF 4 | A novel class of apical sodium-dependent bile acid transporter inhibitors: the amphiphilic 4-oxo-1-phenyl-1,4-dihydroquinoline derivatives. Bioorg Med Chem Lett. 2004 Mar 8;14(5):1183-6. | ||||
| REF 5 | Molecular switch controlling the binding of anionic bile acid conjugates to human apical sodium-dependent bile acid transporter. J Med Chem. 2010 Jun 24;53(12):4749-60. | ||||
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