Page last updated: 2024-08-07 16:41:17
Collagenase 3
A collagenase 3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P45452]
Synonyms
EC 3.4.24.-;
Matrix metalloproteinase-13;
MMP-13
Research
Bioassay Publications (58)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 3 (5.17) | 18.2507 |
2000's | 39 (67.24) | 29.6817 |
2010's | 12 (20.69) | 24.3611 |
2020's | 4 (6.90) | 2.80 |
Compounds (44)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
pimagedine | Homo sapiens (human) | IC50 | 72.0000 | 1 | 1 |
N-[4-(4-morpholinyl)butyl]-2-benzofurancarboxamide | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
way 151693 | Homo sapiens (human) | IC50 | 0.0097 | 5 | 6 |
nafamostat | Homo sapiens (human) | IC50 | 420.0000 | 1 | 1 |
ng-nitroarginine methyl ester | Homo sapiens (human) | IC50 | 2.7000 | 1 | 1 |
piloty's acid | Homo sapiens (human) | Ki | 83.0000 | 1 | 1 |
marimastat | Homo sapiens (human) | IC50 | 0.0162 | 9 | 9 |
sr 27897 | Homo sapiens (human) | IC50 | 0.0006 | 1 | 1 |
n-(2-isobutyl-3-(n'-hydroxycarbonylamido)propanoyl)-o-methyltyrosinemethylamide | Homo sapiens (human) | IC50 | 0.0010 | 1 | 0 |
ilomastat | Homo sapiens (human) | IC50 | 0.0036 | 3 | 3 |
omega-n-methylarginine | Homo sapiens (human) | IC50 | 0.3000 | 1 | 1 |
2-(4-aminophenyl)benzothiazole | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
taxifolin | Homo sapiens (human) | IC50 | 34.6000 | 1 | 1 |
devazepide | Homo sapiens (human) | Ki | 0.0018 | 1 | 1 |
cgs 27023a | Homo sapiens (human) | IC50 | 0.0210 | 2 | 4 |
cgs 27023a | Homo sapiens (human) | Ki | 0.0013 | 1 | 1 |
prinomastat | Homo sapiens (human) | IC50 | 0.0008 | 5 | 5 |
prinomastat | Homo sapiens (human) | Ki | 0.0000 | 2 | 2 |
isoliquiritigenin | Homo sapiens (human) | IC50 | 0.0140 | 1 | 1 |
2-[(4-phenylphenyl)sulfonylamino]pentanedioic acid | Homo sapiens (human) | IC50 | 5.1267 | 3 | 3 |
n(6)-(1-iminoethyl)lysine | Homo sapiens (human) | IC50 | 2.4000 | 1 | 1 |
4-oxido-3-(4-phenoxyphenyl)-4a,5,6,7,8,8a-hexahydroquinoxalin-1-ium 1-oxide | Homo sapiens (human) | IC50 | 6.8000 | 1 | 1 |
rs-130830 | Homo sapiens (human) | IC50 | 0.0367 | 9 | 11 |
rs-130830 | Homo sapiens (human) | Ki | 0.0823 | 5 | 10 |
quercetin | Homo sapiens (human) | IC50 | 8.4600 | 1 | 1 |
luteolin | Homo sapiens (human) | IC50 | 10.0500 | 1 | 1 |
tmi-1 | Homo sapiens (human) | IC50 | 0.0088 | 5 | 11 |
batimastat | Homo sapiens (human) | IC50 | 0.0050 | 1 | 1 |
isoacteoside | Homo sapiens (human) | IC50 | 11.0900 | 1 | 1 |
Methyl rosmarinate | Homo sapiens (human) | IC50 | 29.0300 | 1 | 1 |
ik 682 | Homo sapiens (human) | IC50 | 1.4170 | 1 | 1 |
ik 682 | Homo sapiens (human) | Ki | 1.4170 | 3 | 3 |
bay 12-9566 | Homo sapiens (human) | Ki | 1.4700 | 1 | 1 |
(11c)cgs 25966 | Homo sapiens (human) | IC50 | 0.0060 | 1 | 1 |
ro 32-3555 | Homo sapiens (human) | IC50 | 0.0172 | 4 | 6 |
ro 32-3555 | Homo sapiens (human) | Ki | 0.0013 | 4 | 4 |
pd 166793 | Homo sapiens (human) | IC50 | 0.0080 | 2 | 2 |
sc 78080 | Homo sapiens (human) | IC50 | 0.0001 | 2 | 2 |
2-[[4-(4-bromophenyl)phenyl]sulfonylamino]-3-methylbutanoic acid | Homo sapiens (human) | IC50 | 0.0000 | 1 | 1 |
arp-100 | Homo sapiens (human) | IC50 | 0.0350 | 2 | 2 |
arp-100 | Homo sapiens (human) | Ki | 0.0200 | 1 | 1 |
N(2)-([biphenyl]-4-ylsulfonyl)-N-hydroxy-N(2)-isopropoxy-D-valinamide | Homo sapiens (human) | IC50 | 0.0041 | 1 | 1 |
bms-566394 | Homo sapiens (human) | IC50 | 4.0007 | 1 | 2 |
bms-566394 | Homo sapiens (human) | Ki | 10.0000 | 2 | 2 |
apratastat | Homo sapiens (human) | IC50 | 0.0080 | 1 | 1 |
grassystatin a | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
tetracycline | Homo sapiens (human) | IC50 | 180.0000 | 1 | 1 |
2-[(4-chlorophenyl)methylthio]-1,5,6,7-tetrahydrocyclopenta[d]pyrimidin-4-one | Homo sapiens (human) | IC50 | 3.8240 | 5 | 5 |
2-[(4-chlorophenyl)methylthio]-1,5,6,7-tetrahydrocyclopenta[d]pyrimidin-4-one | Homo sapiens (human) | Ki | 3.8000 | 1 | 1 |
2-[(4-methoxyphenyl)methylthio]-6-methyl-1H-pyrimidin-4-one | Homo sapiens (human) | IC50 | 8.6333 | 3 | 3 |
4-[[(4-oxo-1,5,6,7-tetrahydrocyclopenta[d]pyrimidin-2-yl)thio]methyl]benzoic acid methyl ester | Homo sapiens (human) | IC50 | 2.5500 | 2 | 2 |
4-[[(4-oxo-1,5,6,7-tetrahydrocyclopenta[d]pyrimidin-2-yl)thio]methyl]benzoic acid methyl ester | Homo sapiens (human) | Ki | 1.5260 | 1 | 1 |
Drugs with Other Measurements
Matrix metalloproteinases (MMPs): chemical-biological functions and (Q)SARs.Bioorganic & medicinal chemistry, , Mar-15, Volume: 15, Issue:6, 2007
Heteroaryl and cycloalkyl sulfonamide hydroxamic acid inhibitors of matrix metalloproteinases.Bioorganic & medicinal chemistry letters, , Jan-22, Volume: 11, Issue:2, 2001
The discovery of anthranilic acid-based MMP inhibitors. Part 3: incorporation of basic amines.Bioorganic & medicinal chemistry letters, , Nov-19, Volume: 11, Issue:22, 2001
The discovery of anthranilic acid-based MMP inhibitors. Part 2: SAR of the 5-position and P1(1) groups.Bioorganic & medicinal chemistry letters, , Aug-20, Volume: 11, Issue:16, 2001
The discovery of anthranilic acid-based MMP inhibitors. Part 1: SAR of the 3-position.Bioorganic & medicinal chemistry letters, , Jan-22, Volume: 11, Issue:2, 2001
Selective Inhibitors of Medium-Size S1' Pocket Matrix Metalloproteinases: A Stepping Stone of Future Drug Discovery.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
Discovery of Phenolic Matrix Metalloproteinase Inhibitors by Peptide Microarray for Osteosarcoma Treatment.Journal of natural products, , 10-28, Volume: 85, Issue:10, 2022
Stereospecific synthesis of 5-substituted 2-bisarylthiocyclopentane carboxylic acids as specific matrix metalloproteinase inhibitors.Journal of medicinal chemistry, , Aug-28, Volume: 46, Issue:18, 2003
Phenoxyphenyl sulfone N-formylhydroxylamines (retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors.Journal of medicinal chemistry, , Jan-03, Volume: 45, Issue:1, 2002
Selective, orally active MMP inhibitors with an aryl backbone.Bioorganic & medicinal chemistry letters, , Sep-17, Volume: 11, Issue:18, 2001
General synthesis of alpha-substituted 3-bisaryloxy propionic acid derivatives as specific MMP inhibitors.Bioorganic & medicinal chemistry letters, , Feb-12, Volume: 11, Issue:3, 2001
alpha-Alkyl-alpha-amino-beta-sulphone hydroxamates as potent MMP inhibitors that spare MMP-1.Bioorganic & medicinal chemistry letters, , Oct-22, Volume: 11, Issue:20, 2001
Synthesis and activity of selective MMP inhibitors with an aryl backbone.Bioorganic & medicinal chemistry letters, , Dec-18, Volume: 10, Issue:24, 2000
The synthesis and biological evaluation of non-peptidic matrix metalloproteinase inhibitors.Bioorganic & medicinal chemistry letters, , Oct-04, Volume: 9, Issue:19, 1999
Picking the S1, S1' and S2' pockets of matrix metalloproteinases. A niche for potent acyclic sulfonamide inhibitors.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 9, Issue:12, 1999
Discovery of Aryloxyphenyl-Heptapeptide Hybrids as Potent and Selective Matrix Metalloproteinase-2 Inhibitors for the Treatment of Idiopathic Pulmonary Fibrosis.Journal of medicinal chemistry, , 06-23, Volume: 65, Issue:12, 2022
Arylsulfonamide inhibitors of aggrecanases as potential therapeutic agents for osteoarthritis: synthesis and biological evaluation.European journal of medicinal chemistry, , Volume: 62, 2013
Discovery and characterization of a novel inhibitor of matrix metalloprotease-13 that reduces cartilage damage in vivo without joint fibroplasia side effects.The Journal of biological chemistry, , Sep-21, Volume: 282, Issue:38, 2007
Proline-based hydroxamates targeting the zinc-dependent deacetylase LpxC: Synthesis, antibacterial properties, and docking studies.Bioorganic & medicinal chemistry, , 05-15, Volume: 27, Issue:10, 2019
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.Journal of medicinal chemistry, , Jun-11, Volume: 52, Issue:11, 2009
Stereospecific synthesis of 5-substituted 2-bisarylthiocyclopentane carboxylic acids as specific matrix metalloproteinase inhibitors.Journal of medicinal chemistry, , Aug-28, Volume: 46, Issue:18, 2003
Phenoxyphenyl sulfone N-formylhydroxylamines (retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors.Journal of medicinal chemistry, , Jan-03, Volume: 45, Issue:1, 2002
Selective, orally active MMP inhibitors with an aryl backbone.Bioorganic & medicinal chemistry letters, , Sep-17, Volume: 11, Issue:18, 2001
General synthesis of alpha-substituted 3-bisaryloxy propionic acid derivatives as specific MMP inhibitors.Bioorganic & medicinal chemistry letters, , Feb-12, Volume: 11, Issue:3, 2001
Synthesis and activity of selective MMP inhibitors with an aryl backbone.Bioorganic & medicinal chemistry letters, , Dec-18, Volume: 10, Issue:24, 2000
Protease inhibitors: current status and future prospects.Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Design, synthesis, and biological evaluation of potent thiazine- and thiazepine-based matrix metalloproteinase inhibitors.Journal of medicinal chemistry, , Nov-04, Volume: 42, Issue:22, 1999
High throughput screening of potentially selective MMP-13 exosite inhibitors utilizing a triple-helical FRET substrate.Bioorganic & medicinal chemistry, , Feb-01, Volume: 17, Issue:3, 2009
Ranking the selectivity of PubChem screening hits by activity-based protein profiling: MMP13 as a case study.Bioorganic & medicinal chemistry, , Feb-01, Volume: 17, Issue:3, 2009
Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach.Journal of medicinal chemistry, , 01-26, Volume: 60, Issue:2, 2017
Design, synthesis, and biological activity of novel, potent, and highly selective fused pyrimidine-2-carboxamide-4-one-based matrix metalloproteinase (MMP)-13 zinc-binding inhibitors.Bioorganic & medicinal chemistry, , 12-01, Volume: 24, Issue:23, 2016
Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach.Journal of medicinal chemistry, , Nov-13, Volume: 57, Issue:21, 2014
Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1″ binding site.Bioorganic & medicinal chemistry, , Oct-01, Volume: 22, Issue:19, 2014
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.Journal of medicinal chemistry, , Jun-11, Volume: 52, Issue:11, 2009
Synthesis and structure-activity relationships of beta- and alpha-piperidine sulfone hydroxamic acid matrix metalloproteinase inhibitors with oral antitumor efficacy.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13).Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 15, Issue:4, 2005
Synthesis and structure-activity relationship of N-substituted 4-arylsulfonylpiperidine-4-hydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis.Journal of medicinal chemistry, , Jun-05, Volume: 46, Issue:12, 2003
Selective, orally active MMP inhibitors with an aryl backbone.Bioorganic & medicinal chemistry letters, , Sep-17, Volume: 11, Issue:18, 2001
Synthesis and activity of selective MMP inhibitors with an aryl backbone.Bioorganic & medicinal chemistry letters, , Dec-18, Volume: 10, Issue:24, 2000
Protease inhibitors: current status and future prospects.Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Current perspective of TACE inhibitors: a review.Bioorganic & medicinal chemistry, , Jan-15, Volume: 17, Issue:2, 2009
Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket.Bioorganic & medicinal chemistry, , Sep-15, Volume: 15, Issue:18, 2007
Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 16, Issue:6, 2006
Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-converting enzyme/matrix metalloprotease inhibitor for the treatment of rheuThe Journal of pharmacology and experimental therapeutics, , Volume: 309, Issue:1, 2004
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.Bioorganic & medicinal chemistry, , Oct-01, Volume: 16, Issue:19, 2008
Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).Bioorganic & medicinal chemistry letters, , May-15, Volume: 17, Issue:10, 2007
Identification of potent and selective TACE inhibitors via the S1 pocket.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 17, Issue:1, 2007
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.Journal of medicinal chemistry, , Nov-07, Volume: 45, Issue:23, 2002
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.Journal of medicinal chemistry, , Jun-11, Volume: 52, Issue:11, 2009
A cassette-dosing approach for improvement of oral bioavailability of dual TACE/MMP inhibitors.Bioorganic & medicinal chemistry letters, , May-15, Volume: 16, Issue:10, 2006
Stereospecific synthesis of 5-substituted 2-bisarylthiocyclopentane carboxylic acids as specific matrix metalloproteinase inhibitors.Journal of medicinal chemistry, , Aug-28, Volume: 46, Issue:18, 2003
Protease inhibitors: current status and future prospects.Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
MMP-13 selective α-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.Bioorganic & medicinal chemistry letters, , May-15, Volume: 21, Issue:10, 2011
Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.Journal of medicinal chemistry, , Sep-23, Volume: 53, Issue:18, 2010
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.Bioorganic & medicinal chemistry, , Oct-01, Volume: 16, Issue:19, 2008
Potent, exceptionally selective, orally bioavailable inhibitors of TNF-alpha Converting Enzyme (TACE): novel 2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamide P1' substituents.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 18, Issue:5, 2008
Characterization of selective exosite-binding inhibitors of matrix metalloproteinase 13 that prevent articular cartilage degradation in vitro.Journal of medicinal chemistry, , Nov-26, Volume: 57, Issue:22, 2014
Identification of novel, exosite-binding matrix metalloproteinase-13 inhibitor scaffolds.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 21, Issue:23, 2011
High throughput screening of potentially selective MMP-13 exosite inhibitors utilizing a triple-helical FRET substrate.Bioorganic & medicinal chemistry, , Feb-01, Volume: 17, Issue:3, 2009
Ranking the selectivity of PubChem screening hits by activity-based protein profiling: MMP13 as a case study.Bioorganic & medicinal chemistry, , Feb-01, Volume: 17, Issue:3, 2009
High throughput screening of potentially selective MMP-13 exosite inhibitors utilizing a triple-helical FRET substrate.Bioorganic & medicinal chemistry, , Feb-01, Volume: 17, Issue:3, 2009
Ranking the selectivity of PubChem screening hits by activity-based protein profiling: MMP13 as a case study.Bioorganic & medicinal chemistry, , Feb-01, Volume: 17, Issue:3, 2009
Characterization of selective exosite-binding inhibitors of matrix metalloproteinase 13 that prevent articular cartilage degradation in vitro.Journal of medicinal chemistry, , Nov-26, Volume: 57, Issue:22, 2014
Identification of novel, exosite-binding matrix metalloproteinase-13 inhibitor scaffolds.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 21, Issue:23, 2011
Enables
This protein enables 6 target(s):
Target | Category | Definition |
endopeptidase activity | molecular function | Catalysis of the hydrolysis of internal, alpha-peptide bonds in a polypeptide chain. [http://merops.sanger.ac.uk/about/glossary.htm#ENDOPEPTIDASE] |
metalloendopeptidase activity | molecular function | Catalysis of the hydrolysis of internal, alpha-peptide bonds in a polypeptide chain by a mechanism in which water acts as a nucleophile, one or two metal ions hold the water molecule in place, and charged amino acid side chains are ligands for the metal ions. [GOC:mah, https://www.ebi.ac.uk/merops/about/glossary.shtml#CATTYPE, https://www.ebi.ac.uk/merops/about/glossary.shtml#ENDOPEPTIDASE] |
serine-type endopeptidase activity | molecular function | Catalysis of the hydrolysis of internal, alpha-peptide bonds in a polypeptide chain by a catalytic mechanism that involves a catalytic triad consisting of a serine nucleophile that is activated by a proton relay involving an acidic residue (e.g. aspartate or glutamate) and a basic residue (usually histidine). [GOC:mah, https://www.ebi.ac.uk/merops/about/glossary.shtml#CATTYPE] |
calcium ion binding | molecular function | Binding to a calcium ion (Ca2+). [GOC:ai] |
collagen binding | molecular function | Binding to collagen, a group of fibrous proteins of very high tensile strength that form the main component of connective tissue in animals. Collagen is highly enriched in glycine (some regions are 33% glycine) and proline, occurring predominantly as 3-hydroxyproline (about 20%). [GOC:ai, ISBN:0198506732] |
zinc ion binding | molecular function | Binding to a zinc ion (Zn). [GOC:ai] |
Located In
This protein is located in 2 target(s):
Target | Category | Definition |
extracellular region | cellular component | The space external to the outermost structure of a cell. For cells without external protective or external encapsulating structures this refers to space outside of the plasma membrane. This term covers the host cell environment outside an intracellular parasite. [GOC:go_curators] |
extracellular matrix | cellular component | A structure lying external to one or more cells, which provides structural support, biochemical or biomechanical cues for cells or tissues. [GOC:BHF, GOC:mah, GOC:rph, NIF_Subcellular:nlx_subcell_20090513, PMID:21123617, PMID:28089324] |
Active In
This protein is active in 1 target(s):
Target | Category | Definition |
extracellular space | cellular component | That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684] |
Involved In
This protein is involved in 9 target(s):
Target | Category | Definition |
endochondral ossification | biological process | Replacement ossification wherein bone tissue replaces cartilage. [GO_REF:0000034, ISBN:0878932437] |
growth plate cartilage development | biological process | The process whose specific outcome is the progression of the cartilage that will provide a scaffold for mineralization of endochondral bones as they elongate or grow. [GOC:ascb_2009, GOC:dph, GOC:tb] |
proteolysis | biological process | The hydrolysis of proteins into smaller polypeptides and/or amino acids by cleavage of their peptide bonds. [GOC:bf, GOC:mah] |
extracellular matrix disassembly | biological process | A process that results in the breakdown of the extracellular matrix. [GOC:jid] |
bone mineralization | biological process | The deposition of hydroxyapatite, a form of calcium phosphate with the formula Ca10(PO4)6(OH)2, in bone tissue. [GOC:mah, PMID:22936354] |
collagen catabolic process | biological process | The proteolytic chemical reactions and pathways resulting in the breakdown of collagen in the extracellular matrix, usually carried out by proteases secreted by nearby cells. [GOC:mah, ISBN:0815316194] |
bone morphogenesis | biological process | The process in which bones are generated and organized. [GOC:dph] |
response to amyloid-beta | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a amyloid-beta stimulus. [GO_REF:0000071, GOC:TermGenie, PMID:23555824] |
extracellular matrix organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of an extracellular matrix. [GOC:mah] |