| 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] |