General Information of DTT (ID: TTDZN01)

DTT Name Cathepsin K (CTSK) DTT Info
Gene Name CTSK

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Clinical Trial Drug(s)
Preclinical Drug(s)
Patented Agent(s)
Investigative Drug(s)
3 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Odanacatib DM1EO3G Osteoporosis FB83.0 Phase 3 [1]
SAR-114137 DMZ1XR5 Pain MG30-MG3Z Phase 1 [2]
VEL-0230 DMDSC63 Rheumatoid arthritis FA20 Phase 1 [3]
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8 Patented Agent(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Oxotetrahydro-2-H-furo[3.2-b]pyrrol-4(5-H)-yl derivative 1 DM1SH5R Pain MG30-MG3Z Patented [4]
PMID25399719-Compound-17 DMRXKJZ N. A. N. A. Patented [5]
PMID27998201-Compound-10 DMVXTIL Osteoporosis FB83.0 Patented [4]
PMID27998201-Compound-12 DM8QZNC Bone cancer 2B5Z Patented [4]
PMID27998201-Compound-15 DMOB8LU Pain MG30-MG3Z Patented [4]
PMID27998201-Compound-5 DMVZ0ND Chronic obstructive pulmonary disease CA22 Patented [4]
PMID27998201-Compound-8 DMZK0SY N. A. N. A. Patented [4]
PMID27998201-Compound-9 DM1JOZN Rheumatoid arthritis FA20 Patented [4]
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⏷ Show the Full List of 8 Patented Agent(s)
4 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Balicatib DM06JTL Osteoporosis FB83.0 Discontinued in Phase 2 [6]
ONO-5334 DMWS7C2 Osteoporosis FB83.0 Discontinued in Phase 2 [7]
Relacatib DMLJEFH Bone metastases 2D50 Discontinued in Phase 2 [8]
MIV-701 DM23KBM Osteoporosis FB83.0 Discontinued in Phase 1 [9]
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2 Preclinical Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
GW-2592X DMNAT5V Osteoporosis FB83.0 Preclinical [10]
L-006235-1 DMMEH12 Osteoarthritis FA00-FA05 Preclinical [11]
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48 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
(S)-1-benzylcyclopentyl 1-oxohexan-2-ylcarbamate DMICUQK Discovery agent N.A. Investigative [12]
(S)-tert-butyl 1-oxohexan-2-ylcarbamate DMAQX4K Discovery agent N.A. Investigative [12]
(S)-tert-butyl 4-methyl-1-oxopentan-2-ylcarbamate DMR1HQ3 Discovery agent N.A. Investigative [12]
2-cyclohexylamino-pyridine-2-carbonitrile DMFMZRB Discovery agent N.A. Investigative [13]
2-cyclohexylamino-pyrimidine-4-carbonitrile DMMIGXO Discovery agent N.A. Investigative [13]
3-Amino-5-Phenylpentane DMHDFZE Discovery agent N.A. Investigative [14]
4-cycloheptyl-6-propylpyrimidine-2-carbonitrile DMNT5BF Discovery agent N.A. Investigative [15]
4-cyclohexyl-6-propylpyrimidine-2-carbonitrile DM10U6S Discovery agent N.A. Investigative [15]
4-cyclohexylamino-pyrimidine-2-carbonitrile DMGVIXW Discovery agent N.A. Investigative [13]
4-cyclooctyl-6-propylpyrimidine-2-carbonitrile DMS42TN Discovery agent N.A. Investigative [15]
4-phenyl-6-propylpyrimidine-2-carbonitrile DMMIB0R Discovery agent N.A. Investigative [16]
4-propyl-6-m-tolylpyrimidine-2-carbonitrile DMNM4GE Discovery agent N.A. Investigative [16]
AM-3701 DMZVLJH Bone metastases 2D50 Investigative [10]
BF/PC-21 DMCWB1V Inflammation 1A00-CA43.1 Investigative [10]
Boc-Agly-Val-Agly-OEt DMDX8M3 Discovery agent N.A. Investigative [17]
GNF-PF-5434 DMP9AIH Discovery agent N.A. Investigative [18]
L-873724 DMUP516 Asthma CA23 Investigative [8]
MIV-710 DM13TUY Bone metastases 2D50 Investigative [10]
N-(1-((cyanomethyl)carbamoyl)cyclohexyl)benzamide DMBQ5NS Discovery agent N.A. Investigative [19]
N-(4-phenylbenzoyl)-phenylalanyl-glycine-nitrile DMUJS4Y Discovery agent N.A. Investigative [20]
N-(benzyloxycarbonyl)-leucyl-glycine-nitrile DMR18YI Discovery agent N.A. Investigative [20]
N-(cyanomethyl)cyclohex-1-ene-1-carboxamide DMTKREZ Discovery agent N.A. Investigative [19]
N-(tert-butoxycarbonyl)-isoleucyl-glycine-nitrile DMJ0S5C Discovery agent N.A. Investigative [20]
N-(tert-butoxycarbonyl)-leucyl-glycine-nitrile DMXYQWG Discovery agent N.A. Investigative [20]
N-(tert-butoxycarbonyl)-methionyl-glycine-nitrile DM3I0WZ Discovery agent N.A. Investigative [20]
N-(tert-butoxycarbonyl)-norleucyl-glycine-nitrile DMGF4XC Discovery agent N.A. Investigative [20]
N-(tert-butoxycarbonyl)-norvalyl-glycine-nitrile DMOP5N7 Discovery agent N.A. Investigative [20]
N-(tert-butoxycarbonyl)-valyl-glycine-nitrile DMUQBOP Discovery agent N.A. Investigative [20]
N-acetyl-phenylalanyl-glycine-nitrile DME8O69 Discovery agent N.A. Investigative [20]
N-benzoyl-phenylalanyl-glycine-nitrile DMRJ4B1 Discovery agent N.A. Investigative [20]
P2,P3 Ketoamide derivative DMETL3Z Discovery agent N.A. Investigative [21]
PMID16290936C1b DMOP8YM Discovery agent N.A. Investigative [12]
Pyrrolidine-1-carbonitrile DM906JK Discovery agent N.A. Investigative [22]
Tert-butyl (2S)-1-cyanopyrrolidine-2-carboxylate DM8LI1K Discovery agent N.A. Investigative [22]
TERT-BUTYL 2-CYANO-2-METHYLHYDRAZINECARBOXYLATE DMZG5I7 Discovery agent N.A. Investigative [23]
Tert-Butyl(1s)-1-Cyclohexyl-2-Oxoethylcarbamate DM42WFH Discovery agent N.A. Investigative [23]
Z-Ala-Leu-His-Agly-Ile-Val-OMe DMMP0DT Discovery agent N.A. Investigative [17]
Z-Ala-Leu-lle-Agly-Ile-Val-NHBzl DM7IGRT Discovery agent N.A. Investigative [17]
Z-Ala-Leu-lle-Agly-Ile-Val-OMe DMVEUOL Discovery agent N.A. Investigative [17]
Z-Ala-Leu-Nal-Agly-Ile-Val-OMe DM3209T Discovery agent N.A. Investigative [17]
Z-Ala-Leu-Phe-Agly-Ile-Val-OMe DML16BT Discovery agent N.A. Investigative [17]
Z-Ala-Leu-Tyr(Me)-Agly-Ile-Val-OMe DMIB5O3 Discovery agent N.A. Investigative [17]
Z-Arg-Leu-Val-Agly-Ala-Gly-NH2 DM69FKN Discovery agent N.A. Investigative [17]
Z-Arg-Leu-Val-Agly-Ile-Val-Trp-NH2 DMZDGJO Discovery agent N.A. Investigative [17]
Z-Arg-Leu-Val-Agly-Ileu-Val-OMe DMT0UZ1 Discovery agent N.A. Investigative [17]
Z-Arg-Leu-Val-Agly-Trp-Val-Ala-NH2 DMM5O2V Discovery agent N.A. Investigative [17]
Z-Arg-Leu-Val-Agly-Val-Ala-NH2 DMTWNH7 Discovery agent N.A. Investigative [17]
Z-leu-Val-Agly-Val-OBzl DM6OGR9 Discovery agent N.A. Investigative [17]
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⏷ Show the Full List of 48 Investigative Drug(s)
Molecule Interaction Atlas

References

1 A novel c-Met inhibitor, MK8033, synergizes with carboplatin plus paclitaxel to inhibit ovarian cancer cell growth. Oncol Rep. 2013 May;29(5):2011-8.
2 From laboratory to pilot plant: the solid-state process development of a highly potent cathepsin S/K inhibitor. Eur J Pharm Biopharm. 2013 Apr;83(3):436-48.
3 Discovery and parallel synthesis of a new class of cathepsin K inhibitors. Bioorg Med Chem Lett. 2001 Nov 19;11(22):2951-4.
4 Cathepsin B and L inhibitors: a patent review (2010 - present).Expert Opin Ther Pat. 2017 Jun;27(6):643-656.
5 An updated patent review of calpain inhibitors (2012 - 2014).Expert Opin Ther Pat. 2015 Jan;25(1):17-31.
6 Current and future treatments of bone metastases. Expert Opin Emerg Drugs. 2008 Dec;13(4):609-27.
7 New approach for osteoporosis treatment: cathepsin K inhibitor, ONO-5334. Clin Calcium. 2011 Jan;21(1):64-9.
8 The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8.
9 Medivir designates MIV-710 a Candidate Drug (CD) for Osteoporosis and Osteoarthritis, 2009
10 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. (Target id: 2350).
11 Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional se... J Med Chem. 2005 Dec 1;48(24):7535-43.
12 Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors Bioorg Med Chem Lett. 2006 Feb 15;16(4):978-83.
13 2-Cyano-pyrimidines: a new chemotype for inhibitors of the cysteine protease cathepsin K. J Med Chem. 2007 Feb 22;50(4):591-4.
14 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
15 Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1524-7.
16 2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4447-50.
17 Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases. J Med Chem. 2002 Sep 12;45(19):4202-11.
18 Substrate optimization for monitoring cathepsin C activity in live cells. Bioorg Med Chem. 2009 Feb 1;17(3):1064-70.
19 Beta-substituted cyclohexanecarboxamide: a nonpeptidic framework for the design of potent inhibitors of cathepsin K. J Med Chem. 2006 Feb 9;49(3):1066-79.
20 Interaction of papain-like cysteine proteases with dipeptide-derived nitriles. J Med Chem. 2005 Dec 1;48(24):7688-707.
21 Potent and selective P2-P3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P1', P1, and/or P3 substitutions. Bioorg Med Chem Lett. 2004 Oct 4;14(19):4897-902.
22 Acyclic cyanamide-based inhibitors of cathepsin K. Bioorg Med Chem Lett. 2005 Jun 15;15(12):3039-43.
23 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.