Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T13726 | Target Info | |||
| Target Name | Retinoic acid receptor RXR-alpha (RXRA) | ||||
| Synonyms |
Retinoid X receptor alpha; RXRalpha; Nuclear receptor subfamily 2 group B member 1; NR2B1
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| Target Type | Successful Target | ||||
| Gene Name | RXRA | ||||
| Biochemical Class | Nuclear hormone receptor | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 26 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Sulindac
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|
Approved | Compound Info | ||
| Synonyms |
Aclin; Aflodac; Arthrobid; Arthrocine; Chibret; Clinoril; Copal; Copals; Kenalin; Klinoril; Mobilin; Sulindaco; Sulindacum; Sulindal; Alphapharm Brand of Sulindac; Apo Sulin; Apotex Brand of Sulindac; Cahill May Roberts Brand of Sulindac; Chemia Brand of Sulindac; Copal resin; Copal rosin varnish; Gum copal; KendrickBrand of Sulindac; Merck Brand of Sulindac; Novo Sundac; Novopharm Brand of Sulindac; Nu Pharm Brand of Sulindac; Nu Sulindac; Resin copal; Sulindac sulfoxide; MK 231; MK231; S 8139; Apo-Sulin; Clinoril (TN); MK-231; Merck Sharp & Dohme Brand of Sulindac; Novo-Sundac; Nu-Pharm Brand of Sulindac; Nu-Sulindac; Sulindaco [INN-Spanish]; Sulindacum [INN-Latin]; Sulindac (JAN/USP/INN); Sulindac [USAN:BAN:INN:JAN]; Z-5-Fluoro-2-methyl-1-[p-(methlsulfinyl)benzylidene]indene-3-acetic acid; Cis-5-Fluoro-2-methyl-1-((p-methylsulfinyl)benzylidene)indene-3-acetic acid; {5-fluoro-2-methyl-1-[4-(methylsulfinyl)benzylidene]-1h-inden-3-yl}acetic acid; Cis-5-Fluoro-2-methyl-1-((4-(methylsulfinyl)phenyl)methylene)-1H-indene-3-acetic acid; [(1E)-5-fluoro-2-methyl-1-{[4-(methylsulfinyl)phenyl]methylidene}-1H-inden-3-yl]acetic acid; {(1E)-5-fluoro-2-methyl-1-[4-(methylsulfinyl)benzylidene]-1H-inden-3-yl}acetic acid; {(1Z)-5-fluoro-2-methyl-1-[4-(methylsulfinyl)benzylidene]-1H-inden-3-yl}acetic acid; (E)-(1)-5-Fluoro-2-methyl-1-((4-(methylsulphinyl)phenyl)methylene)-1H-indene-3-acetic acid; (Z)-5-Fluoro-2-methyl-1-((p-(methylsulfinyl)phenyl)methylene)-1H-indene-3-acetic acid; (Z)-5-Fluoro-2-methyl-1-[[4-(methyl-sulfinyl)phenyl]methylene]-1H-indene-3-acetic acid; (Z)-5-Fluoro-2-methyl-1-[p-(methylsulfinyl)benzylidene]indene-3-acetic acid; 2-[(3E)-6-fluoro-2-methyl-3-[(4-methylsulfinylphenyl)methylidene]inden-1-yl]acetic acid; 2-[(3Z)-6-fluoro-2-methyl-3-[(4-methylsulfinylphenyl)methylidene]inden-1-yl]acetic acid; 2-[6-fluoro-2-methyl-3-[(4-methylsulfinylphenyl)methylidene]inden-1-yl]acetic acid; 5-Fluoro-2-methyl-1-((4-(methylsulphinyl)phenyl)methylene)-1H-indene-3-acetic acid
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| Activity |
IC50 = 82900 nM
|
[1] | |||
| Compound Name |
2-[(3Z)-2,6-Dimethyl-3-[(4-propan-2-ylphenyl)methylidene]inden-1-yl]acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2337786; SCHEMBL12182063
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(3Z)-3-[[4-(Dimethylamino)phenyl]methylidene]-6-fluoro-2-methylinden-1-yl]acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2337800; SCHEMBL12182061
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4-[5,7,7,10,10-Pentamethyl-2-(methylamino)-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl]benzoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL236488; BDBM50218473
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
2-[(3Z)-3-[(3-Cyanophenyl)methylidene]-6-fluoro-2-methylinden-1-yl]acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2337777; SCHEMBL12181903
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(3Z)-6-Fluoro-2-methyl-3-[(4-pyridin-2-ylphenyl)methylidene]inden-1-yl]acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2337797
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(3Z)-6-Fluoro-2-methyl-3-[(4-propan-2-ylphenyl)methylidene]inden-1-yl]acetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2337781; SCHEMBL12181836
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4-[2-(Butylamino)-5,7,7,10,10-pentamethyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl]benzoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL436999; BDBM50218494
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
2-[3-[(4-Methylphenyl)carbamoyl]-4-piperidin-1-ylphenyl]indazole-6-carboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3746821; SCHEMBL17317386; BDBM50500150
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| Activity |
EC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
4-[(Z)-N-Ethoxy-C-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)carbonimidoyl]benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2110180; BDBM50408855
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
2-[(3Z)-6-Chloro-2-methyl-3-[(4-propan-2-ylphenyl)methylidene]inden-1-yl]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2337791; SCHEMBL17119518
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(3Z)-6-Ethyl-2-methyl-3-[(4-propan-2-ylphenyl)methylidene]inden-1-yl]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2337788; SCHEMBL17119517
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(3Z)-3-[(4-Tert-butylphenyl)methylidene]-6-fluoro-2-methylinden-1-yl]acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2337796; SCHEMBL12181842
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(3Z)-3-[(4-Cyanophenyl)methylidene]-6-fluoro-2-methylinden-1-yl]acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2337799; SCHEMBL12181885
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4-[(Z)-N-[(2-Methylpropan-2-yl)oxy]-C-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)carbonimidoyl]benzoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2110182; BDBM50408856
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|
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
2-[(3Z)-3-[(4-Ethoxyphenyl)methylidene]-6-fluoro-2-methylinden-1-yl]acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2337798; SCHEMBL12181904
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(3Z)-2-Methyl-3-[(4-propan-2-ylphenyl)methylidene]inden-1-yl]acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2337785; SCHEMBL12182062
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4-[[(E)-Tert-Butoxyimino]-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-methyl]-benzoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL162827; BDBM50074298
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|
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| Activity |
EC50 ~ 100000 nM
|
[4] | |||
| Compound Name |
1-[(Z)-3-Methoxybenzylidene]-2-methyl-5-fluoro-1H-indene-3-acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL163333; SCHEMBL12181898
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(3Z)-6-Methoxy-2-methyl-3-[(4-propan-2-ylphenyl)methylidene]inden-1-yl]acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2337787; SCHEMBL12181845
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4-[2-(Benzylamino)-5,7,7,10,10-pentamethyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl]benzoic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL391160; BDBM50218498
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|
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
1-[(Z)-4-Methoxybenzylidene]-2-methyl-5-fluoro-1H-indene-3-acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL163161; SCHEMBL8156624; SCHEMBL8156636; 2-[(3Z)-6-fluoro-3-[(4-methoxyphenyl)methylidene]-2-methylinden-1-yl]acetic acid
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
3-[(3Z)-6-Fluoro-2-methyl-3-[(4-propan-2-ylphenyl)methylidene]inden-1-yl]propanenitrile
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2337780; SCHEMBL17118989; SCHEMBL18245294
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(3E)-6-Fluoro-2-methyl-3-[(4-propan-2-ylphenyl)methylidene]inden-1-yl]acetamide
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2337782; SCHEMBL12181832
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|
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(3Z)-3-[(4-Acetamidophenyl)methylidene]-6-fluoro-2-methylinden-1-yl]acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2337778; SCHEMBL12181850
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
2-[(3Z)-2-Methyl-6-propan-2-yl-3-[(4-propan-2-ylphenyl)methylidene]inden-1-yl]acetic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2337790
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Synthesis and SAR study of modulators inhibiting tRXRalpha-dependent AKT activation. Eur J Med Chem. 2013 Apr;62:632-48. | ||||
| REF 2 | Synthesis and structure-activity relationship of RXR antagonists based on the diazepinylbenzoic acid structure. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4808-11. | ||||
| REF 3 | Structure-activity relationships for lipoprotein lipase agonists that lower plasma triglycerides in vivo. Eur J Med Chem. 2015 Oct 20;103:191-209. | ||||
| REF 4 | Synthesis of retinoid X receptor-specific ligands that are potent inducers of adipogenesis in 3T3-L1 cells. J Med Chem. 1999 Feb 25;42(4):742-50. | ||||
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