Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T82146 Target Info
Target Name Retinoic acid receptor gamma (RARG)
Synonyms
RAR-gamma; Nuclear receptor subfamily 1 group B member 3; NR1B3
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Target Type Successful Target
Gene Name RARG
Biochemical Class Nuclear hormone receptor
UniProt ID
RARG_HUMAN
Co-Targets of This Target  Top
Co-Target Name Retinoic acid receptor RXR-alpha (RXRA) Successful Target
UniProt ID RXRA_HUMAN
Gene Name RXRA
Synonyms
Retinoid X receptor alpha; RXRalpha; Nuclear receptor subfamily 2 group B member 1; NR2B1
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Representative Drug(s) Tretinoin Drug Info EC50 ~ 0.001 nM Click to Show More [1]
2 Alitretinoin Drug Info EC50 = 1.5 nM [5]
Co-Target Name Retinoic acid receptor beta (RARB) Successful Target
UniProt ID RARB_HUMAN
Gene Name RARB
Synonyms
RAR-epsilon; RAR-beta; Nuclear receptor subfamily 1 group B member 2; NR1B2; HBV-activated protein; HAP
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Representative Drug(s) Tretinoin Drug Info Ki = 0.4 nM Click to Show More [2]
2 Alitretinoin Drug Info Ki = 0.5 nM [2]
3 Tazarotene Drug Info EC50 = 0.8 nM [4]
4 Trifarotene Drug Info EC50 = 125 nM [8]
Co-Target Name Retinoic acid receptor RXR-beta (RXRB) Successful Target
UniProt ID RXRB_HUMAN
Gene Name RXRB
Synonyms
Retinoid X receptor beta; Nuclear receptor subfamily 2 group B member 2; NR2B2
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Representative Drug(s) Tretinoin Drug Info Ki = 0.5 nM Click to Show More [3]
2 Alitretinoin Drug Info EC50 = 2.6 nM [6]
Co-Target Name Retinoic acid receptor RXR-gamma (RXRG) Successful Target
UniProt ID RXRG_HUMAN
Gene Name RXRG
Synonyms
Retinoid X receptor gamma; Nuclear receptor subfamily 2 group B member 3; NR2B3
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Representative Drug(s) Tretinoin Drug Info Ki = 1.4 nM Click to Show More [3]
2 Alitretinoin Drug Info IC50 = 4 nM [7]
Co-Target Name Retinoic acid receptor alpha (RARA) Clinical trial Target
UniProt ID RARA_HUMAN
Gene Name RARA
Synonyms
RAR-alpha; RAR alpha; Nuclear receptor subfamily 1 group B member 1; NR1B1
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Representative Drug(s) Tretinoin Drug Info Ki = 0.1 nM Click to Show More [2]
2 Alitretinoin Drug Info IC50 = 7 nM [7]
3 Tazarotene Drug Info EC50 = 63 nM [4]
4 Trifarotene Drug Info EC50 = 500 nM [8]
Co-Target Name Nuclear receptor ROR-gamma (RORG) Clinical trial Target
UniProt ID RORG_HUMAN
Gene Name RORC
Synonyms
Retinoid-related orphan receptor-gamma; RZRG; RORG; RAR-related orphan receptor C; Nuclear receptor subfamily 1 group F member 3; Nuclear receptor RZR-gamma; NR1F3
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Representative Drug(s) Tretinoin Drug Info IC50 = 199.53 nM [9]
Co-Target Name Rotamase Pin1 (PIN1) Clinical trial Target
UniProt ID PIN1_HUMAN
Gene Name PIN1
Synonyms
Prolyl isomerase Pin1; Peptidyl-prolyl cis-trans isomerase Pin1; Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1; Peptidyl prolyl cis/trans isomerase Pin1; PPIase Pin1
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Representative Drug(s) Tretinoin Drug Info IC50 = 820 nM [10]
Co-Target Name RAR-related orphan receptor-beta (RORB) Patented-recorded Target
UniProt ID RORB_HUMAN
Gene Name RORB
Synonyms
Retinoid-related orphan receptor-beta; RZRB; Nuclear receptor subfamily 1 group F member 2; Nuclear receptor RZR-beta; Nuclear receptor ROR-beta; NR1F2
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Representative Drug(s) Tretinoin Drug Info IC50 = 0.15 nM [11]
Co-Target Name Nuclear receptor ROR-alpha (RORA) Patented-recorded Target
UniProt ID RORA_HUMAN
Gene Name RORA
Synonyms
Retinoid-related orphan receptor-alpha; Retinoic acid-related orphan receptor alpha; RZRA; RAR-related orphan receptor A; Nuclear receptor subfamily 1 group F member 1; Nuclear receptor RZR-alpha; NR1F1
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Representative Drug(s) Tretinoin Drug Info IC50 = 199.53 nM [9]
References  Top
REF 1 Synthesis and structure-activity relationships of stilbene retinoid analogs substituted with heteroaromatic carboxylic acids. J Med Chem. 1995 Jul 21;38(15):2820-9.
REF 2 Synthesis and receptor binding affinity of conformationally restricted retinoic acid analogues. Bioorg Med Chem Lett. 1997 Sep 9;7(17):2313-8.
REF 3 An improved synthesis of the C-linked glucuronide of N-(4-hydroxyphenyl)retinamide. Bioorg Med Chem Lett. 2002 Sep 2;12(17):2447-50.
REF 4 Novel non-carboxylic acid retinoids: 1,2,4-oxadiazol-5-one derivatives. Bioorg Med Chem Lett. 2009 Jan 15;19(2):489-92.
REF 5 Enantioselective syntheses of potent retinoid X receptor ligands: differential biological activities of individual antipodes. J Med Chem. 2001 Jul 5;44(14):2298-303.
REF 6 Conformational effects on retinoid receptor selectivity. 2. Effects of retinoid bridging group on retinoid X receptor activity and selectivity. J Med Chem. 1995 Aug 18;38(17):3368-83.
REF 7 Synthesis of high specific activity [3H]-9-cis-retinoic acid and its application for identifying retinoids with unusual binding properties. J Med Chem. 1994 Feb 4;37(3):408-14.
REF 8 Structure-based design of Trifarotene (CD5789), a potent and selective RARgamma agonist for the treatment of acne. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1736-41.
REF 9 Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORbeta and RORgammat. Bioorg Med Chem Lett. 2014 Nov 15;24(22):5265-7.
REF 10 Synthesis and biological evaluation of pyrimidine derivatives as novel human Pin1 inhibitors. Bioorg Med Chem. 2018 May 1;26(8):2186-2197.
REF 11 Synthetic modulators of the retinoic acid receptor-related orphan receptors. Medchemcomm. 2013;4:764-76.

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