General Information of the Protein
Protein ID
PT01276
Protein Name
Collagenase 3
Secondarily
Protein Name
Matrix metalloproteinase-13
Gene Name
MMP13
Sequence
MHPGVLAAFLFLSWTHCRALPLPSGGDEDDLSEEDLQFAERYLRSYYHPTNLAGILKENAASSMTERLREMQSFFGLEVTGKLDDNTLDVMKKPRCGVPDVGEYNVFPRTLKWSKMNLTYRIVNYTPDMTHSEVEKAFKKAFKVWSDVTPLNFTRLHDGIADIMISFGIKEHGDFYPFDGPSGLLAHAFPPGPNYGGDAHFDDDETWTSSSKGYNLFLVAAHEFGHSLGLDHSKDPGALMFPIYTYTGKSHFMLPDDDVQGIQSLYGPGDEDPNPKHPKTPDKCDPSLSLDAITSLRGETMIFKDRFFWRLHPQQVDAELFLTKSFWPELPNRIDAAYEHPSHDLIFIFRGRKFWALNGYDILEGYPKKISELGLPKEVKKISAAVHFEDTGKTLLFSGNQVWRYDDTNHIMDKDYPRLIEEDFPGIGDKVDAVYEKNGYIYFFNGPIQFEYSIWSNRIVRVMPANSILWC
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Protease
>
Metallo protease
>
Metallo protease MAM clan
>
Metallo protease M10A subfamily
Function
Plays a role in the degradation of extracellular matrix proteins including fibrillar collagen, fibronectin, TNC and ACAN. Cleaves triple helical collagens, including type I, type II and type III collagen, but has the highest activity with soluble type II collagen. Can also degrade collagen type IV, type XIV and type X. May also function by activating or degrading key regulatory proteins, such as TGFB1 and CCN2. Plays a role in wound healing, tissue remodeling, cartilage degradation, bone development, bone mineralization and ossification. Required for normal embryonic bone development and ossification. Plays a role in the healing of bone fractures via endochondral ossification. Plays a role in wound healing, probably by a mechanism that involves proteolytic activation of TGFB1 and degradation of CCN2. Plays a role in keratinocyte migration during wound healing. May play a role in cell migration and in tumor cell invasion.
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Uniprot ID
Primary ID:
P45452

Secondarily ID:
A8K846
B2RCZ3
Q6NWN6
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Ensembl ID
ENSG00000137745
HGNC ID
HGNC:7159
Subcellular Location
Secreted
Extracellular space
Extracellular matrix
Secreted
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0069428
US9206139, 1
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C18H20F3N3O3
 1
1
IC50 = 1110 nM
   TI
   LI
   LO
   TS
CP0199497
US9206139, 2
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C19H22F3N3O3
 1
1
IC50 = 4189 nM
   TI
   LI
   LO
   TS
CP0069431
US9206139, 5
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C19H22F3N3O3
 1
1
IC50 = 4808 nM
   TI
   LI
   LO
   TS
CP0118960
US9206139, 3
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C20H22F3N3O3
 1
1
IC50 = 46952 nM
   TI
   LI
   LO
   TS
CP0069429
US9206139, 4
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C20H24F3N3O3
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0048641
(2S,3R)-N(4)-[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]-N(1),2-dihydroxy-3-(2-methylpropyl)butanediamide
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C15H29N3O5
 6
1 Activity = 2 nM
2 IC50 = 0.74 nM
3 IC50 = 1.2 nM
4 IC50 = 2 nM
5 IC50 = 3.4 nM
6 IC50 = 3.5 nM
CP0081310
N-(2-aminoethyl)-4-[4-[(4-oxo-3,5,6,7-tetrahydrocyclopenta[d]pyrimidin-2-yl)sulfanylmethyl]phenyl]benzenesulfonamide
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C22H24N4O3S2
 2
1 IC50 = 3.4 nM
2 IC50 = 8.3 nM
CP0228998
N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]-5-[3-fluoro-4-[(4-oxo-3,5,6,7-tetrahydrocyclopenta[d]pyrimidin-2-yl)sulfanylmethyl]phenyl]furan-2-carboxamide
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C28H31FN4O4S
 1
1 IC50 = 7.9 nM
CP0099232
5-[3-fluoro-4-[(4-oxo-3,5,6,7-tetrahydrocyclopenta[d]pyrimidin-2-yl)sulfanylmethyl]phenyl]-N-[(2S)-3-methyl-1-(methylamino)-1-oxobutan-2-yl]furan-2-carboxamide
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C25H27FN4O4S
 1
1 IC50 = 8.1 nM
CP0228996
N-(2-hydroxyethyl)-4-[4-[(4-oxo-3,5,6,7-tetrahydrocyclopenta[d]pyrimidin-2-yl)sulfanylmethyl]phenyl]benzenesulfonamide
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C22H23N3O4S2
 1
1 IC50 = 12 nM
CP0065111
2-[(4-methylphenyl)methylsulfanyl]-3,5,6,7-tetrahydrocyclopenta[d]pyrimidin-4-one
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C15H16N2OS
 3
1 IC50 = 400 nM
2 IC50 = 2400 nM
3 Ki = 824 nM
CP0069428
US9206139, 1
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C18H20F3N3O3
 1
1 IC50 = 1100 nM
CP0199497
US9206139, 2
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C19H22F3N3O3
 1
1 IC50 = 4200 nM
CP0069431
US9206139, 5
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C19H22F3N3O3
 1
1 IC50 = 4800 nM
CP0118960
US9206139, 3
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C20H22F3N3O3
 1
1 IC50 = 47000 nM
CP0069429
US9206139, 4
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C20H24F3N3O3
 1
1 IC50 > 100000 nM
Clinical Information about the Protein
Target 1 ( Matrix metalloproteinase-13 (MMP-13) )
Target Type Clinical trial Target
Disease 5 Target-related Diseases  5
1 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
2 Rheumatoid arthritis [ICD-11: FA20]
3 Pain [ICD-11: MG30-MG3Z]
4 Corneal ulcer [ICD-11: 9A76]
5 Hepatitis C virus infection [ICD-11: 1E51.1]
Clinical Trial Drug(s) 3 Clinical Trial Drugs  3
1 Curcumin Phase 3
Solid tumour/cancer
2 Apratastat Phase 2
Rheumatoid arthritis
3 PMID17935984C1 Clinical trial
Pain
Discontinued Drug(s) 2 Discontinued Drugs  2
1 GM6001 Discontinued in Phase 2
Corneal ulcer
2 RS-130830 Discontinued in Phase 2
Hepatitis C virus infection