Target Information
| Target General Information | Top | |||||
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| Target ID |
T20103
(Former ID: TTDR00563)
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| Target Name |
Vacuolar-type proton ATPase (v-ATPase)
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| Synonyms |
Vacuolar-ATPase; Vacuolar ATPase; V-ATPase
Click to Show/Hide
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| Gene Name |
NO-GeName
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| Target Type |
Preclinical target
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[1] | ||||
| Disease | [+] 4 Target-related Diseases | + | ||||
| 1 | Low bone mass disorder [ICD-11: FB83] | |||||
| 2 | Arteries/arterioles disorder [ICD-11: BD52] | |||||
| 3 | Malignant haematopoietic neoplasm [ICD-11: 2B33] | |||||
| 4 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||||
| BioChemical Class |
Acid anhydrides hydrolase
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| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
| 1 | WY-47766 | Drug Info | Discontinued in Phase 2 | Osteoporosis | [2] | |
| Preclinical Drug(s) | [+] 3 Preclinical Drugs | + | ||||
| 1 | FR167356 | Drug Info | Preclinical | Osteoporosis | [3] | |
| 2 | Salicylihalamide A | Drug Info | Preclinical | Solid tumour/cancer | [3] | |
| 3 | SB 242784 | Drug Info | Preclinical | Arterial calcification | [4] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Modulator | [+] 1 Modulator drugs | + | ||||
| 1 | WY-47766 | Drug Info | [1] | |||
| Inhibitor | [+] 12 Inhibitor drugs | + | ||||
| 1 | FR167356 | Drug Info | [5] | |||
| 2 | Salicylihalamide A | Drug Info | [6] | |||
| 3 | SB 242784 | Drug Info | [4] | |||
| 4 | Bafilomycin A1 | Drug Info | [7] | |||
| 5 | BRD1240 | Drug Info | [3] | |||
| 6 | Lobatamide A | Drug Info | [6] | |||
| 7 | Lobatamide B | Drug Info | [6] | |||
| 8 | Lobatamide C | Drug Info | [6] | |||
| 9 | Lobatamide D | Drug Info | [6] | |||
| 10 | Lobatamide F | Drug Info | [6] | |||
| 11 | Oximidine I | Drug Info | [6] | |||
| 12 | Oximidine II | Drug Info | [6] | |||
| 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 | ||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | A pharmacological assessment of the mammalian osteoclast vacuolar H(+)-ATPase. Bone Miner. 1994 Nov;27(2):159-66. | |||||
| REF 2 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003235) | |||||
| REF 3 | Lysosomes as a therapeutic target. Nat Rev Drug Discov. 2019 Dec;18(12):923-948. | |||||
| REF 4 | SB 242784, a selective inhibitor of the osteoclastic V-H+ATPase, inhibits arterial calcification in the rat. Circ Res. 2002 Sep 20;91(6):547-52. | |||||
| REF 5 | Therapeutic target database update 2012: a resource for facilitating target-oriented drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1128-36. | |||||
| REF 6 | Discovery of a novel antitumor benzolactone enamide class that selectively inhibits mammalian vacuolar-type (H+)-atpases. J Pharmacol Exp Ther. 2001 Apr;297(1):114-20. | |||||
| REF 7 | Molecular basis of V-ATPase inhibition by bafilomycin A1. Nat Commun. 2021 Mar 19;12(1):1782. | |||||
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