Page last updated: 2024-11-12
balicatib
Description
Research Excerpts
Clinical Trials
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Study Profile
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Description
balicatib: cathepsin K inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 10201696 |
| CHEMBL ID | 371064 |
| SCHEMBL ID | 1587772 |
| MeSH ID | M0522639 |
Synonyms (38)
| Synonym |
|---|
| chembl371064 , |
| balicatib |
| basic piperazine-containing compound, 10 |
| n-{1-[(cyanomethyl)carbamoyl]cyclohexyl}-4-(4-propylpiperazin-1-yl)benzamide |
| n-[1-(cyanomethylcarbamoyl)cyclohexyl]-4-(4-propylpiperazin-1-yl) |
| bdbm19855 |
| n-[1-(cyanomethylcarbamoyl)cyclohexyl]-4-(4-propylpiperazin-1-yl)benzamide |
| aae-581 |
| aae581 |
| aae 581 |
| unii-e00mvc7o57 |
| balicatib [inn] |
| 354813-19-7 |
| e00mvc7o57 , |
| n-(1-((cyanomethyl)carbamoyl)cyclohexyl)-4-(4-propylpiperazin-1-yl)benzamide |
| balicatib [who-dd] |
| HY-15100 |
| gtpl7861 |
| SCHEMBL1587772 |
| LLCRBOWRJOUJAE-UHFFFAOYSA-N |
| n-[1-(cyanomethyl-carbamoyl)-cyclohexyl]-4-[4-(1-propyl)-piperazin-1-yl]-benzamide |
| AKOS025149083 |
| n-(1-(cyanomethylcarbamoyl)cyclohexyl)-4-(4-propylpiperazin-1-yl)benzamide |
| J-690287 |
| DTXSID10188989 |
| EX-A362 |
| mfcd19443790 |
| NCGC00371151-06 |
| DB12239 |
| FT-0700298 |
| Q27074857 |
| BCP09098 |
| HMS3740C15 |
| AS-56087 |
| S0194 |
| balicatib (aae-581) |
| AC-35832 |
| NCGC00371151-01 |
Research Excerpts
Treatment
In balicatib-treated animals, BMD change in the spine was intermediate between group S and O, with groups L and M significantly different from group O.
| Excerpt | Reference | Relevance |
|---|---|---|
| "In balicatib-treated animals, BMD change in the spine was intermediate between group S and O, with groups L and M significantly different from group O." | ( Balicatib, a cathepsin K inhibitor, stimulates periosteal bone formation in monkeys. Gamse, R; Jerome, C; Missbach, M, 2011) | 2.33 |
| "In balicatib-treated animals, BMD change in the spine was intermediate between group S and O, with groups L and M significantly different from group O." | ( Balicatib, a cathepsin K inhibitor, stimulates periosteal bone formation in monkeys. Gamse, R; Jerome, C; Missbach, M, 2012) | 2.34 |
Bioavailability
Dosage Studied
Eighty adult female Macaca fascicularis underwent bilateral ovariectomies and were dosed twice daily by oral gavage with balicatib at 0, 3, 10, and 50 mg/kg for 18 months.
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (9)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Cathepsin S | Mus musculus (house mouse) | IC50 (µMol) | 3.2953 | 0.0003 | 2.4555 | 6.3500 | AID1797908; AID257094; AID257095 |
| Sterol O-acyltransferase 1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.2640 | 0.0058 | 0.6626 | 6.0000 | AID257087; AID257095 |
| Cathepsin D | Homo sapiens (human) | Ki | 0.0013 | 0.0000 | 0.0012 | 0.0020 | AID1168917 |
| Procathepsin L | Homo sapiens (human) | IC50 (µMol) | 1.1804 | 0.0002 | 1.6661 | 9.5100 | AID1797909; AID257086; AID257087; AID314232 |
| Procathepsin L | Homo sapiens (human) | Ki | 7.2543 | 0.0000 | 1.1013 | 9.3000 | AID1168923; AID1241504; AID256977 |
| Cathepsin B | Homo sapiens (human) | IC50 (µMol) | 2.4958 | 0.0002 | 1.8453 | 10.0000 | AID1797909; AID257084; AID257085; AID314231; AID699426 |
| Cathepsin B | Homo sapiens (human) | Ki | 3.3500 | 0.0000 | 1.2180 | 8.6000 | AID1168921; AID256976 |
| Cathepsin S | Homo sapiens (human) | IC50 (µMol) | 15.2206 | 0.0002 | 1.3191 | 10.0000 | AID1797909; AID257088; AID257089; AID314233 |
| Cathepsin S | Homo sapiens (human) | Ki | 41.0333 | 0.0000 | 0.4143 | 3.2900 | AID1168919; AID1241506; AID256978 |
| Sodium-dependent serotonin transporter | Rattus norvegicus (Norway rat) | IC50 (µMol) | 2.9000 | 0.0003 | 0.8197 | 8.4900 | AID257089 |
| Cathepsin K | Homo sapiens (human) | IC50 (µMol) | 0.0027 | 0.0001 | 0.8482 | 10.0000 | AID257083; AID314228; AID482895; AID699423; AID703434 |
| Cathepsin K | Homo sapiens (human) | Ki | 0.0014 | 0.0000 | 0.1537 | 2.1000 | AID1241503 |
| Cathepsin K | Oryctolagus cuniculus (rabbit) | IC50 (µMol) | 1.2719 | 0.0002 | 1.1018 | 6.3500 | AID1797908; AID1797910; AID257092; AID314229 |
| Cathepsin K | Oryctolagus cuniculus (rabbit) | Ki | 0.0014 | 0.0002 | 0.0007 | 0.0014 | AID256975 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Activation Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Procathepsin L | Homo sapiens (human) | EC50 (µMol) | 2.9000 | 0.0030 | 4.4874 | 9.8200 | AID1797909 |
| Cathepsin B | Homo sapiens (human) | EC50 (µMol) | 2.9000 | 0.7900 | 1.8450 | 2.9000 | AID1797909 |
| Cathepsin S | Homo sapiens (human) | EC50 (µMol) | 2.9000 | 0.7900 | 1.8450 | 2.9000 | AID1797909 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (50)
Molecular Functions (14)
Ceullar Components (30)
Bioassays (58)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID314229 | Inhibition of rabbit cathepsin K | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3 | The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. |
| AID703434 | Inhibition of cathepsin-k | 2012 | Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20 | Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors. |
| AID482900 | Selectivity for cathepsin K over cathepsin S | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11 | Emerging targets in osteoporosis disease modification. |
| AID699426 | Inhibition of human recombinant CatB assessed as suppression of enzyme-mediated Z-Arg-Arg-AMC cleavage by QFRET assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | (1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): a potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis. |
| AID257084 | Inhibitory activity against human cathepsin B | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. |
| AID257087 | Inhibitory activity against human cathepsin L expressed in HepG2 cells | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. |
| AID257085 | Inhibitory activity against human cathepsin B expressed in HepG2 cells | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. |
| AID257096 | Volume of distribution in rat administered with 10 mg/kg, po | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. |
| AID257086 | Inhibitory activity against human cathepsin L | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. |
| AID699423 | Inhibition of human recombinant CatK assessed as suppression of enzyme-mediated Z-Phe-Arg-AMC cleavage incubated for 1 hrs by QFRET assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | (1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): a potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis. |
| AID1241503 | Inhibition of human cathepsin-K using Z-Gly-Pro-Arg-AMC as substrate preincubated for 30 mins measured after 10 mins by fluorescence assay | 2015 | Journal of medicinal chemistry, Sep-10, Volume: 58, Issue:17 | Development of N-(Functionalized benzoyl)-homocycloleucyl-glycinonitriles as Potent Cathepsin K Inhibitors. |
| AID256976 | Inhibitory constant against human cathepsin B using Boc-Leu-Lys-Arg-AMC substrate | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K. |
| AID1241504 | Inhibition of human cathepsin-L using Z-Phe-Arg-AMC as substrate preincubated for 30 mins measured after 10 mins by fluorescence assay | 2015 | Journal of medicinal chemistry, Sep-10, Volume: 58, Issue:17 | Development of N-(Functionalized benzoyl)-homocycloleucyl-glycinonitriles as Potent Cathepsin K Inhibitors. |
| AID314230 | Inhibition of bone resorption in rabbit osteoclast | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3 | The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. |
| AID257083 | Inhibitory activity against humanized rabbit cathepsin K | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. |
| AID1168919 | Inhibition of human cathepsin S using Z-Phe-Arg-AMC fluorogenic substrate fluorogenic substrate incubated for 60 mins | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10 | 3-Cyano-3-aza-β-amino Acid Derivatives as Inhibitors of Human Cysteine Cathepsins. |
| AID314228 | Inhibition of human cathepsin K | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3 | The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. |
| AID482424 | Antiosteoporotic activity in postmenopausal woman with osteoporosis assessed as decrease in bone resorption-associated serum CTX-1 level at 50 mg/kg | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11 | Emerging targets in osteoporosis disease modification. |
| AID314232 | Inhibition of cathepsin L in human HepG2 cells | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3 | The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. |
| AID1168921 | Inhibition of human cathepsin B using Z-Arg-Arg-pNA chromogenic substrate fluorogenic substrate incubated for 30 mins | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10 | 3-Cyano-3-aza-β-amino Acid Derivatives as Inhibitors of Human Cysteine Cathepsins. |
| AID256977 | Inhibitory constant against human cathepsin L using Z-Phe-Arg-AMC substrate | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K. |
| AID257092 | Inhibitory activity against rabbit cathepsin K | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. |
| AID1168923 | Inhibition of human cathepsin L using Z-Phe-Arg-pNA chromogenic substrate fluorogenic substrate incubated for 30 mins | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10 | 3-Cyano-3-aza-β-amino Acid Derivatives as Inhibitors of Human Cysteine Cathepsins. |
| AID257089 | Inhibitory activity against human cathepsin S expressed in ramos cells | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. |
| AID257090 | Partition co-efficient, logP of the compound | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. |
| AID392951 | Binding affinity to glutathione assessed as typical half life at 1.4 nM | 2009 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4 | A simple in vitro assay for assessing the reactivity of nitrile containing compounds. |
| AID256975 | Inhibitory constant against rabbit cathepsin K using Z-Phe-Arg-AMC substrate | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K. |
| AID482426 | Antiosteoporotic activity in postmenopausal woman with osteoporosis assessed as increase lumbar spine bone mineral density at 50 mg/kg | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11 | Emerging targets in osteoporosis disease modification. |
| AID482895 | Inhibition of cathepsin K | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11 | Emerging targets in osteoporosis disease modification. |
| AID314234 | Accumulation of intracellular type I collagen in human dermal fibroblast upto 10 uM | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3 | The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. |
| AID482899 | Selectivity for cathepsin K over cathepsin L | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11 | Emerging targets in osteoporosis disease modification. |
| AID257091 | Dissociation constant, pKa of the compound | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. |
| AID257093 | Effect of compound on degradation of collagen in osteoclast bone resorption assay | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. |
| AID257100 | Effect of compound on antigen presentation in mouse A20 cells transfected with PC-specific mIgM by IL-2 secretion | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. |
| AID257088 | Inhibitory activity against human cathepsin S | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. |
| AID482425 | Antiosteoporotic activity in postmenopausal woman with osteoporosis assessed as decrease in bone resorption-associated urinary CTX-1 level at 50 mg/kg | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11 | Emerging targets in osteoporosis disease modification. |
| AID314233 | Inhibition of cathepsin S in human ramos cells | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3 | The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. |
| AID703270 | Inhibition of osteoclastogenesis in human bone marrow-derived stem cells assessed as reduction of pit formation by measuring TRACP5b activity after 7 days by bone TRAP assay | 2012 | Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20 | Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors. |
| AID256978 | Inhibitory constant against human cathepsin S using Z-Val-Val-Arg-AMC substrate | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K. |
| AID1241506 | Inhibition of human cathepsin-S using Z-Phe-Val-Arg-AMC as substrate preincubated for 30 mins measured after 10 mins by fluorescence assay | 2015 | Journal of medicinal chemistry, Sep-10, Volume: 58, Issue:17 | Development of N-(Functionalized benzoyl)-homocycloleucyl-glycinonitriles as Potent Cathepsin K Inhibitors. |
| AID257095 | Inhibitory activity against mouse cathepsin S in mouse splenocytes | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. |
| AID314231 | Inhibition of cathepsin B in human HepG2 cells | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3 | The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. |
| AID482427 | Antiosteoporotic activity in postmenopausal woman with osteoporosis assessed as increase hip bone mineral density at 50 mg/kg | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11 | Emerging targets in osteoporosis disease modification. |
| AID1168917 | Inhibition of human cathepsin K using Z-Leu-Arg-AMC fluorogenic substrate incubated for 60 mins | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10 | 3-Cyano-3-aza-β-amino Acid Derivatives as Inhibitors of Human Cysteine Cathepsins. |
| AID392952 | Binding affinity to cysteine assessed as typical half life at 1.4 nM | 2009 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4 | A simple in vitro assay for assessing the reactivity of nitrile containing compounds. |
| AID257098 | Plasma concentration in rat at 10 mg/kg, po | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. |
| AID482898 | Selectivity for cathepsin K over cathepsin B | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11 | Emerging targets in osteoporosis disease modification. |
| AID257094 | Inhibitory activity against mouse cathepsin S | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1345903 | Human cathepsin K (C1: Papain) | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11 | Emerging targets in osteoporosis disease modification. |
| AID1797909 | Enzyme Inhibition Assay and Whole Cell Enzyme Occupancy Assay from Article 10.1021/jm0504961: \\Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.\\ | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. |
| AID1797908 | Enzyme Inhibition Assay from Article 10.1021/jm0504961: \\Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.\\ | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. |
| AID1797910 | Enzyme Inhibition Assay and Bone Resorption Assay from Article 10.1021/jm0504961: \\Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.\\ | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24 | Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (24)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 8 (33.33) | 29.6817 |
| 2010's | 11 (45.83) | 24.3611 |
| 2020's | 5 (20.83) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 24.69
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (24.69) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (4.17%) | 5.53% |
| Reviews | 4 (16.67%) | 6.00% |
| Case Studies | 2 (8.33%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 17 (70.83%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||