Target Information
| Target General Information | Top | |||||
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| Target ID |
T57680
(Former ID: TTDR00186)
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| Target Name |
Soluble guanylate cyclase (GCS)
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| Synonyms |
GUCY1; GUCS; GUC1; GCS
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| Gene Name |
GUCY1A1; GUCY1B1
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 4 Target-related Diseases | + | ||||
| 1 | Angina pectoris [ICD-11: BA40] | |||||
| 2 | Diabetic foot ulcer [ICD-11: BD54] | |||||
| 3 | Hypertension [ICD-11: BA00-BA04] | |||||
| 4 | Respiratory failure [ICD-11: CB41] | |||||
| Function |
Probably plays a specific functional role in the rods and/or cones of photoreceptors. It may be the enzyme involved in the resynthesis of cGMP required for recovery of the dark state after phototransduction.
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| BioChemical Class |
Phosphorus-oxygen lyase
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| UniProt ID | ||||||
| Sequence |
MFCTKLKDLKITGECPFSLLAPGQVPNESSEEAAGSSESCKATVPICQDIPEKNIQESLP
QRKTSRSRVYLHTLAESICKLIFPEFERLNVALQRTLAKHKIKESRKSLEREDFEKTIAE QAVAAGVPVEVIKESLGEEVFKICYEEDENILGVVGGTLKDFLNSFSTLLKQSSHCQEAG KRGRLEDASILCLDKEDDFLHVYYFFPKRTTSLILPGIIKAAAHVLYETEVEVSLMPPCF HNDCSEFVNQPYLLYSVHMKSTKPSLSPSKPQSSLVIPTSLFCKTFPFHFMFDKDMTILQ FGNGIRRLMNRRDFQGKPNFEEYFEILTPKINQTFSGIMTMLNMQFVVRVRRWDNSVKKS SRVMDLKGQMIYIVESSAILFLGSPCVDRLEDFTGRGLYLSDIPIHNALRDVVLIGEQAR AQDGLKKRLGKLKATLEQAHQALEEEKKKTVDLLCSIFPCEVAQQLWQGQVVQAKKFSNV TMLFSDIVGFTAICSQCSPLQVITMLNALYTRFDQQCGELDVYKVETIGDAYCVAGGLHK ESDTHAVQIALMALKMMELSDEVMSPHGEPIKMRIGLHSGSVFAGVVGVKMPRYCLFGNN VTLANKFESCSVPRKINVSPTTYRLLKDCPGFVFTPRSREELPPNFPSEIPGICHFLDAY QQGTNSKPCFQKKDVEDGNANFLGKASGID Click to Show/Hide
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| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 3 Approved Drugs | + | ||||
| 1 | Nitric Oxide | Drug Info | Approved | Respiratory failure | [2], [3] | |
| 2 | Nitroglycerin | Drug Info | Approved | Diabetic foot ulcer | [4] | |
| 3 | Sodium nitroprusside | Drug Info | Approved | Hypertension | [5] | |
| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | IW-1973 | Drug Info | Phase 2 | Heart failure | [10] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Stimulator | [+] 1 Stimulator drugs | + | ||||
| 1 | Nitric Oxide | Drug Info | [11] | |||
| Modulator | [+] 2 Modulator drugs | + | ||||
| 1 | Nitroglycerin | Drug Info | [1], [5] | |||
| 2 | Sodium nitroprusside | Drug Info | [5] | |||
| Agonist | [+] 1 Agonist drugs | + | ||||
| 1 | IW-1973 | Drug Info | [10] | |||
| Activator | [+] 1 Activator drugs | + | ||||
| 1 | (5-(1-benzyl-1H-indazol-3-yl)furan-2-yl)methanol | Drug Info | [1] | |||
| 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 | ||
| References | Top | |||||
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| REF 1 | Activators of soluble guanylate cyclase for the treatment of male erectile dysfunction. Int J Impot Res. 2002 Feb;14(1):8-14. | |||||
| REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2509). | |||||
| REF 3 | Emerging therapies for treatment of acute lung injury and acute respiratory distress syndrome. Expert Opin Emerg Drugs. 2007 Sep;12(3):461-77. | |||||
| REF 4 | Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24. | |||||
| REF 5 | Stimulators and activators of soluble guanylate cyclase: review and potential therapeutic indications.Crit Care Res Pract.2012;2012:290805. | |||||
| REF 6 | ClinicalTrials.gov (NCT05579691) A Phase 2, Randomized, Double-Blind, Placebo-Controlled, Dose Exploration Study to Assess the Safety, Pharmacokinetics, and Pharmacodynamics of Subcutaneous CTI-1601 in Adult Subjects With Friedreich's Ataxia. U.S.National Institutes of Health. | |||||
| REF 7 | ClinicalTrials.gov (NCT04507061) A Randomized, Double-blind, Placebo-controlled, Multi-center Study to Assess the Safety and Efficacy of Individually Titrated Oral Doses of Runcaciguat in Subjects With Clinical Diagnosis of Chronic Kidney Disease With Diabetes and/or Hypertension and at Least One Cardiovascular Comorbidity. U.S.National Institutes of Health. | |||||
| REF 8 | ClinicalTrials.gov (NCT05612035) A Phase 2a Randomized, Placebo-Controlled Clinical Study to Evaluate the Efficacy and Safety of MK-5475 in Adults With Pulmonary Hypertension Associated With Chronic Obstructive Pulmonary Disease. U.S.National Institutes of Health. | |||||
| REF 9 | ClinicalTrials.gov (NCT04798989) A Phase 2a Study Evaluating the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of CY6463 When Administered to Participants With Alzheimer's Disease and Vascular Pathology. U.S.National Institutes of Health. | |||||
| REF 10 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 11 | Nitric oxide and nitrovasodilators: similarities, differences, and interactions. Am J Cardiol. 1996 May 30;77(13):2C-7C. | |||||
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