Target Information
| Target General Information | Top | |||||
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| Target ID |
T84726
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| Target Name |
Rho-associated protein kinase (ROCK)
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| Synonyms |
Rho-associated, coiled-coil-containing protein kinase; Rho associated protein kinase
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| Gene Name |
NO-GeName
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Glaucoma [ICD-11: 9C61] | |||||
| 2 | Myocardial infarction [ICD-11: BA41-BA43] | |||||
| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 2 Approved Drugs | + | ||||
| 1 | Netarsudil | Drug Info | Approved | Open-angle glaucoma | [2] | |
| 2 | Ximelegatran | Drug Info | Approved | Myocardial infarction | [3] | |
| Clinical Trial Drug(s) | [+] 5 Clinical Trial Drugs | + | ||||
| 1 | Roclatan | Drug Info | Phase 3 | Glaucoma/ocular hypertension | [4] | |
| 2 | AMA-76 | Drug Info | Phase 2 | Glaucoma/ocular hypertension | [5] | |
| 3 | AR-12286 | Drug Info | Phase 2 | Glaucoma/ocular hypertension | [6] | |
| 4 | Cethrin | Drug Info | Phase 1/2 | Spinal cord injury | [8] | |
| 5 | AT13148 | Drug Info | Phase 1 | Solid tumour/cancer | [10] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Modulator | [+] 7 Modulator drugs | + | ||||
| 1 | Netarsudil | Drug Info | [11] | |||
| 2 | Ximelegatran | Drug Info | [1], [12] | |||
| 3 | Roclatan | Drug Info | [13] | |||
| 4 | AMA-76 | Drug Info | [14] | |||
| 5 | AR-12286 | Drug Info | [15] | |||
| 6 | Cethrin | Drug Info | [16] | |||
| 7 | AT13148 | Drug Info | [17] | |||
| Inhibitor | [+] 7 Inhibitor drugs | + | ||||
| 1 | Hexahydro azepinone derivative 1 | Drug Info | [18] | |||
| 2 | Isoquinoline derivative 4 | Drug Info | [18] | |||
| 3 | Isoquinoline derivative 5 | Drug Info | [18] | |||
| 4 | Isoquinoline sulfonamide derivative 1 | Drug Info | [18] | |||
| 5 | Isoquinoline sulfonamide derivative 2 | Drug Info | [18] | |||
| 6 | Isoquinoline sulfonyl derivative 2 | Drug Info | [18] | |||
| 7 | Isoquinoline sulfonyl derivative 3 | Drug Info | [18] | |||
| 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 | ||
| Co-Targets | Top | |||||
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| Co-Targets | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases. Mol Pharmacol. 2000 May;57(5):976-83. | |||||
| REF 2 | 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85. | |||||
| REF 3 | Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90. | |||||
| REF 4 | ClinicalTrials.gov (NCT02558400) Double-masked Study of PG324 Ophthalmic Solution in Patients With Glaucoma or Ocular Hypertension. | |||||
| REF 5 | ClinicalTrials.gov (NCT02136940) Multiple Dose-parallel-group Study of AMA0076 in Patients With Primary Open-Angle Glaucoma or Ocular Hypertension. U.S. National Institutes of Health. | |||||
| REF 6 | ClinicalTrials.gov (NCT01699464) A Study Assessing the Safety and Ocular Hypotensive Efficacy of AR-12286 in Patients With Elevated Intraocular Pressure for 3 Months. U.S. National Institutes of Health. | |||||
| REF 7 | ClinicalTrials.gov (NCT00846989) Efficacy, Tolerability and Safety of RKI983 (0.05% & 0.10%) vs Xalatan in Patients With POAG or Ocular Hypertension. U.S. National Institutes of Health. | |||||
| REF 8 | Emerging drugs for spinal cord injury. Expert Opin Emerg Drugs. 2008 Mar;13(1):63-80. | |||||
| REF 9 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 10 | ClinicalTrials.gov (NCT01585701) Phase I Study of AT13148, a Novel AGC Kinase Inhibitor. U.S. National Institutes of Health. | |||||
| REF 11 | Effect of 0.04% AR-13324, a ROCK, and norepinephrine transporter inhibitor, on aqueous humor dynamics in normotensive monkey eyes. J Glaucoma. 2015 Jan;24(1):51-4. | |||||
| REF 12 | Molecular characterization of the effects of Y-27632. Cell Motil Cytoskeleton. 2007 Feb;64(2):97-109. | |||||
| REF 13 | Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41. | |||||
| REF 14 | AMA0076, a novel, locally acting Rho kinase inhibitor, potently lowers intraocular pressure in New Zealand white rabbits with minimal hyperemia. Invest Ophthalmol Vis Sci. 2014 Feb 18;55(2):1006-16. | |||||
| REF 15 | Ocular hypotensive effect of the Rho kinase inhibitor AR-12286 in patients with glaucoma and ocular hypertension. Am J Ophthalmol. 2011 Nov;152(5):834-41.e1. | |||||
| REF 16 | A phase I/IIa clinical trial of a recombinant Rho protein antagonist in acute spinal cord injury. J Neurotrauma. 2011 May;28(5):787-96. | |||||
| REF 17 | Company report (Astex) | |||||
| REF 18 | Rho kinase inhibitors: a patent review (2014 - 2016).Expert Opin Ther Pat. 2017 Apr;27(4):507-515. | |||||
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