Target Information
| Target General Information | Top | |||||
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| Target ID |
T69506
(Former ID: TTDS00351)
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| Target Name |
Orphan nuclear receptor NR1I3 (NR1I3)
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| Synonyms |
Orphan nuclear receptor MB67; Orphan nuclear receptor CAR; Nuclear receptor subfamily 1 group I member 3; Nuclear receptor CAR; Constitutive androstane receptor; Constitutive active response; Constitutive activator of retinoid response; CAR
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| Gene Name |
NR1I3
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Dizziness and giddiness [ICD-11: MB48] | |||||
| Function |
Transactivates both the phenobarbital responsive element module of the human CYP2B6 gene and the CYP3A4 xenobiotic response element. Binds and transactivates the retinoic acid response elements that control expression of the retinoic acid receptor beta 2 and alcohol dehydrogenase 3 genes.
Click to Show/Hide
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| BioChemical Class |
Nuclear hormone receptor
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| UniProt ID | ||||||
| Sequence |
MASREDELRNCVVCGDQATGYHFNALTCEGCKGFFRRTVSKSIGPTCPFAGSCEVSKTQR
RHCPACRLQKCLDAGMRKDMILSAEALALRRAKQAQRRAQQTPVQLSKEQEELIRTLLGA HTRHMGTMFEQFVQFRPPAHLFIHHQPLPTLAPVLPLVTHFADINTFMVLQVIKFTKDLP VFRSLPIEDQISLLKGAAVEICHIVLNTTFCLQTQNFLCGPLRYTIEDGARVSPTVGFQV EFLELLFHFHGTLRKLQLQEPEYVLLAAMALFSPDRPGVTQRDEIDQLQEEMALTLQSYI KGQQRRPRDRFLYAKLLGLLAELRSINEAYGYQIQHIQGLSAMMPLLQEICS Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| HIT2.0 ID | T41INV | |||||
| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | Meclizine | Drug Info | Approved | Dizziness | [2] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Modulator | [+] 1 Modulator drugs | + | ||||
| 1 | Meclizine | Drug Info | [1] | |||
| Inhibitor | [+] 1 Inhibitor drugs | + | ||||
| 1 | (5BETA)-PREGNANE-3,20-DIONE | Drug Info | [3] | |||
| Antagonist | [+] 2 Antagonist drugs | + | ||||
| 1 | androstanol | Drug Info | [4] | |||
| 2 | androstenol | Drug Info | [3], [4] | |||
| Agonist | [+] 2 Agonist drugs | + | ||||
| 1 | CITCO | Drug Info | [5] | |||
| 2 | TCPOBOP | Drug Info | [6] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
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| Target-interacting Proteins | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| PID Pathway | [+] 1 PID Pathways | + | ||||
| 1 | Glucocorticoid receptor regulatory network | |||||
| WikiPathways | [+] 5 WikiPathways | + | ||||
| 1 | Nuclear Receptors in Lipid Metabolism and Toxicity | |||||
| 2 | Nuclear Receptors Meta-Pathway | |||||
| 3 | Constitutive Androstane Receptor Pathway | |||||
| 4 | Drug Induction of Bile Acid Pathway | |||||
| 5 | Nuclear Receptors | |||||
| References | Top | |||||
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| REF 1 | Synthetic drugs and natural products as modulators of constitutive androstane receptor (CAR) and pregnane X receptor (PXR). Drug Metab Rev. 2006;38(1-2):51-73. | |||||
| REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 3 | The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. | |||||
| REF 4 | Androstane metabolites bind to and deactivate the nuclear receptor CAR-beta. Nature. 1998 Oct 8;395(6702):612-5. | |||||
| REF 5 | Identification of a novel human constitutive androstane receptor (CAR) agonist and its use in the identification of CAR target genes. J Biol Chem. 2003 May 9;278(19):17277-83. | |||||
| REF 6 | The nuclear receptor CAR is a regulator of thyroid hormone metabolism during caloric restriction. J Biol Chem. 2004 May 7;279(19):19832-8. | |||||
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