Target Poor or Non Binder(s) Information
Target General Information | Top | ||||
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Target ID | T95289 | Target Info | |||
Target Name | Retinoic acid receptor RXR (RXR) | ||||
Synonyms |
RXR
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Target Type | Clinical trial Target | ||||
Gene Name | NO-GeName | ||||
UniProt ID |
Poor Binders of This Target (in total, 5 binders) | Download | Top | |||
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Compound Name |
4-((+/-)-(1H-imidazol-1-yl)-(E)-retinoic acid
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Investigative | Compound Info | ||
Synonyms |
CHEMBL57765; 4-((+/-)-(1H-imidazol-1-yl)-(E)-retinoic acid; SCHEMBL1234027; 4-(1-Imidazolyl)retinoic acid; BDBM50091698; (2E,4E,6E,8E)-9-(3-Imidazol-1-yl-2,6,6-trimethyl-cyclohex-1-enyl)-3,7-dimethyl-nona-2,4,6,8-tetraenoic acid
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Activity | Retinoic acid receptor RXR beta |
IC50 = 175000 nM
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[1] | ||
Compound Name |
N-(1H-1,2,4-Triazol-1-yl)-(E)-retinamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL388283; SCHEMBL3706627; BDBM50158413
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Activity | Retinoic acid receptor RXR beta |
IC50 = 90000 nM
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[1] | ||
Compound Name |
(E)-3-[4-(4-Hydroxyphenyl)phenyl]prop-2-enoic Acid
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Investigative | Compound Info | ||
Synonyms |
CHEMBL187836; SCHEMBL3293830; SCHEMBL3293835; BDBM50170869; ZINC13648522; (E)-3-(4''-Hydroxy-biphenyl-4-yl)-acrylic acid
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Activity | Retinoic acid receptor RXR beta |
EC50 ~ 100000 nM
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[2] | ||
Compound Name |
4-((+/-)-(1H-Imidazol-1-yl)-(13Z)-retinoic acid
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Investigative | Compound Info | ||
Synonyms |
CHEMBL387639; SCHEMBL17769833; BDBM50158416
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Activity | Retinoic acid receptor RXR alpha |
IC50 = 100000 nM
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[1] | ||
Retinoic acid receptor RXR beta |
IC50 = 175000 nM
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[1] | |||
Compound Name |
(E)-3-[4-(4-Hydroxy-3-phenylphenyl)phenyl]prop-2-enoic acid
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Investigative | Compound Info | ||
Synonyms |
CHEMBL189565; BDBM50170868; (E)-3-(4''-Hydroxy-[1,1'';3'',1'''']terphenyl-4-yl)-acrylic acid
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Activity | Retinoic acid receptor RXR beta |
EC50 ~ 100000 nM
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[2] |
Non Binders of This Target (in total, 4 non binders) | Download | Top | |||
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Compound Name |
(2E,4E,6E,8E)-3,7-Dimethyl-9-(2,6,6-trimethyl-3-[1,2,4]triazol-4-yl-cyclohex-1-enyl)-nona-2,4,6,8-tetraenoic acid
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Investigative | Compound Info | ||
Synonyms |
CHEMBL53449; SCHEMBL1232072; BDBM50091699; 4-((+/-)-(1H-1,2,4-triazol-4-yl)-(E)-retinoic acid
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Activity | Retinoic acid receptor RXR beta |
IC50 = 250000 nM
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[1] | ||
Retinoic acid receptor RXR alpha |
IC50 = 410000 nM
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[1] | |||
Compound Name |
N-(1H-Imidazole-1-yl)-(E)-retinamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL388064; SCHEMBL3698734; BDBM50158412
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Activity | Retinoic acid receptor RXR beta |
IC50 = 500000 nM
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[1] | ||
Retinoic acid receptor RXR alpha |
IC50 > 1000000 nM
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[1] | |||
Compound Name |
6-(3-((S)-1-Methoxypropan-2-yloxy)-5-((S)-1-phenylpropan-2-yloxy)benzamido)nicotinic acid
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Investigative | Compound Info | ||
Synonyms |
GKA-50; GKA50; CHEMBL205627; SCHEMBL304693; GKA 50; GKA 50;GKA50; BCP24209; BDBM50320996; ZINC40556749; AKOS024458510; SB22875; NCGC00387236-02; HY-15671; CS-0008214
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Activity | Retinoic acid receptor RXR gamma |
IC50 > 1000000 nM
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[3] | ||
Compound Name |
(2E,4E,6E,8E)-3,7-Dimethyl-9-(2,6,6-trimethyl-3-[1,2,4]triazol-1-yl-cyclohex-1-enyl)-nona-2,4,6,8-tetraenoic acid
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Investigative | Compound Info | ||
Synonyms |
CHEMBL417769; SCHEMBL1233540; BDBM50091700; 4-((+/-)-(1H-1,2,4-triazol-1-yl)-(E)-retinoic acid
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Activity | Retinoic acid receptor RXR beta |
IC50 = 1000000 nM
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[1] | ||
Retinoic acid receptor RXR alpha |
IC50 > 1000000 nM
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[1] |
References | Top | ||||
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REF 1 | Novel retinoic acid metabolism blocking agents endowed with multiple biological activities are efficient growth inhibitors of human breast and pros... J Med Chem. 2004 Dec 30;47(27):6716-29. | ||||
REF 2 | Synthesis and structure-activity relationships of a new series of retinoid-related biphenyl-4-ylacrylic acids endowed with antiproliferative and proapoptotic activity. J Med Chem. 2005 Jul 28;48(15):4931-46. | ||||
REF 3 | Overcoming retinoic acid receptor-alpha based testicular toxicity in the optimisation of glucokinase activators. Medchemcomm. 2011;2:771-4. |
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