Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T71167
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| Target Name |
Oxysterols receptor LXR (NR1H)
|
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| Gene Name |
NO-GeName
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| Target Type |
Clinical trial target
|
[1] | ||||
| Disease | [+] 7 Target-related Diseases | + | ||||
| 1 | Atopic eczema [ICD-11: EA80] | |||||
| 2 | Lung cancer [ICD-11: 2C25] | |||||
| 3 | Arterial occlusive disease [ICD-11: BD40] | |||||
| 4 | Cardiovascular disease [ICD-11: BA00-BE2Z] | |||||
| 5 | Lymphoma [ICD-11: 2A80-2A86] | |||||
| 6 | Metabolic disorder [ICD-11: 5C50-5D2Z] | |||||
| 7 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||||
| BioChemical Class |
Nuclear hormone receptor
|
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| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Clinical Trial Drug(s) | [+] 8 Clinical Trial Drugs | + | ||||
| 1 | ALX-101 | Drug Info | Phase 2 | Atopic dermatitis | [2] | |
| 2 | RGX-104 | Drug Info | Phase 1/2 | Non-small-cell lung cancer | [3] | |
| 3 | BMS-779788 | Drug Info | Phase 1 | Arteriosclerosis | [4] | |
| 4 | BMS-852927 | Drug Info | Phase 1 | Arteriosclerosis | [5] | |
| 5 | CS-8080 | Drug Info | Phase 1 | Arteriosclerosis | [6] | |
| 6 | LXR 623 | Drug Info | Phase 1 | Arteriosclerosis | [1] | |
| 7 | XL-041 | Drug Info | Phase 1 | Arteriosclerosis | [7] | |
| 8 | XL652/XL014 | Drug Info | Phase 1 | Metabolic disorder | [8] | |
| Mode of Action | [+] 3 Modes of Action | + | ||||
| Agonist | [+] 2 Agonist drugs | + | ||||
| 1 | ALX-101 | Drug Info | [2] | |||
| 2 | RGX-104 | Drug Info | [9] | |||
| Modulator | [+] 6 Modulator drugs | + | ||||
| 1 | BMS-779788 | Drug Info | [1] | |||
| 2 | BMS-852927 | Drug Info | [1] | |||
| 3 | CS-8080 | Drug Info | [1] | |||
| 4 | LXR 623 | Drug Info | [1] | |||
| 5 | XL-041 | Drug Info | [10] | |||
| 6 | XL652/XL014 | Drug Info | [8] | |||
| Binder | [+] 1 Binder drugs | + | ||||
| 1 | T0901317 | Drug Info | [11] | |||
| Drug Property Profile of Target | Top | |
|---|---|---|
| (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 | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Liver X receptors in lipid metabolism: opportunities for drug discovery. Nat Rev Drug Discov. 2014 Jun;13(6):433-44. | |||||
| REF 2 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 3 | Clinical pipeline report, company report or official report of Rgenix. | |||||
| REF 4 | ClinicalTrials.gov (NCT00836602) Multiple-Dose Study to Evaluate the Safety, Pharmacokinetics and Pharmacodynamics of BMS-779788 in Healthy Subjects. U.S. National Institutes of Health. | |||||
| REF 5 | ClinicalTrials.gov (NCT01651273) A Safety Study of BMS-852927 in Subjects With Hypercholesterolemia. U.S. National Institutes of Health. | |||||
| REF 6 | ClinicalTrials.gov (NCT00796575) Effects of Multiple Doses of CS-8080 in Healthy Volunteers. U.S. National Institutes of Health. | |||||
| REF 7 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029634) | |||||
| REF 8 | Clinical pipeline report, company report or official report of Exelixis (2011). | |||||
| REF 9 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 10 | Emerging small molecule drugs. Handb Exp Pharmacol. 2015;224:617-30. | |||||
| REF 11 | The LXR ligand T0901317 induces severe lipogenesis in the db/db diabetic mouse. J Lipid Res. 2003 Nov;44(11):2039-48. | |||||
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