General Information of the Protein
Protein ID
PT00842
Protein Name
72 kDa type IV collagenase
Secondarily
Protein Name
72 kDa gelatinase
Gelatinase A
Matrix metalloproteinase-2
TBE-1
Gene Name
MMP2
Secondarily
Gene Name
CLG4A
Sequence
MEALMARGALTGPLRALCLLGCLLSHAAAAPSPIIKFPGDVAPKTDKELAVQYLNTFYGCPKESCNLFVLKDTLKKMQKFFGLPQTGDLDQNTIETMRKPRCGNPDVANYNFFPRKPKWDKNQITYRIIGYTPDLDPETVDDAFARAFQVWSDVTPLRFSRIHDGEADIMINFGRWEHGDGYPFDGKDGLLAHAFAPGTGVGGDSHFDDDELWTLGEGQVVRVKYGNADGEYCKFPFLFNGKEYNSCTDTGRSDGFLWCSTTYNFEKDGKYGFCPHEALFTMGGNAEGQPCKFPFRFQGTSYDSCTTEGRTDGYRWCGTTEDYDRDKKYGFCPETAMSTVGGNSEGAPCVFPFTFLGNKYESCTSAGRSDGKMWCATTANYDDDRKWGFCPDQGYSLFLVAAHEFGHAMGLEHSQDPGALMAPIYTYTKNFRLSQDDIKGIQELYGASPDIDLGTGPTPTLGPVTPEICKQDIVFDGIAQIRGEIFFFKDRFIWRTVTPRDKPMGPLLVATFWPELPEKIDAVYEAPQEEKAVFFAGNEYWIYSASTLERGYPKPLTSLGLPPDVQRVDAAFNWSKNKKTYIFAGDKFWRYNEVKKKMDPGFPKLIADAWNAIPDNLDAVVDLQGGGHSYFFKGAYYLKLENQSLKSVKFGSIKSDWLGC
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Protease
>
Metallo protease
>
Metallo protease MAM clan
>
Metallo protease M10A subfamily
Function
Ubiquitinous metalloproteinase that is involved in diverse functions such as remodeling of the vasculature, angiogenesis, tissue repair, tumor invasion, inflammation, and atherosclerotic plaque rupture. As well as degrading extracellular matrix proteins, can also act on several nonmatrix proteins such as big endothelial 1 and beta-type CGRP promoting vasoconstriction. Also cleaves KISS at a Gly-|-Leu bond. Appears to have a role in myocardial cell death pathways. Contributes to myocardial oxidative stress by regulating the activity of GSK3beta. Cleaves GSK3beta in vitro. Involved in the formation of the fibrovascular tissues in association with MMP14.
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Uniprot ID
Primary ID:
P08253

Secondarily ID:
B2R6U1
B4DWH3
E9PE45
Q9UCJ8
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Ensembl ID
ENSG00000087245
HGNC ID
HGNC:7166
Subcellular Location
Secreted
Extracellular space
Extracellular matrix
Membrane
Nucleus
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
CP0191287
N-[2-[[(2R)-1-(hydroxyamino)-3-methyl-1-oxobutan-2-yl]-(4-phenylphenyl)sulfonylamino]ethyl]benzamide
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C26H29N3O5S
 1
1
IC50 = 0.16 nM
   TI
   LI
   LO
   TS
CP0072521
3-[[[2-(hydroxyamino)-2-oxoethyl]-(4-methoxyphenyl)sulfonylamino]methyl]benzoic acid
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C17H18N2O7S
 1
1
IC50 = 2 nM
   TI
   LI
   LO
   TS
CP0091600
1-N,3-N-bis[2-[[(2R)-1-(hydroxyamino)-3-methyl-1-oxobutan-2-yl]-(4-phenylphenyl)sulfonylamino]ethyl]benzene-1,3-dicarboxamide
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C46H52N6O10S2
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0110637
1-N,3-N-bis[4-[[(3R)-4-(hydroxyamino)-4-oxo-3-[(4-phenylphenyl)sulfonyl-propan-2-yloxyamino]butyl]amino]-4-oxobutyl]benzene-1,3-dicarboxamide
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C54H66N8O14S2
 1
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0067113
(2R)-2-[2-[[3-[2-[[(1R)-1-carboxy-2-methylpropyl]-(4-phenylphenyl)sulfonylamino]ethylcarbamoyl]benzoyl]amino]ethyl-(4-phenylphenyl)sulfonylamino]-3-methylbutanoic acid
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C46H50N4O10S2
 1
1
IC50 = 63 nM
   TI
   LI
   LO
   TS
CP0333590
3-N-[2-[[(2R)-1-(dimethylamino)-3-methyl-1-oxobutan-2-yl]-(4-phenylphenyl)sulfonylamino]ethyl]-1-N-[2-[[(2R)-1-(hydroxyamino)-3-methyl-1-oxobutan-2-yl]-(4-phenylphenyl)sulfonylamino]ethyl]benzene-1,3-dicarboxamide
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C48H56N6O9S2
 1
1
IC50 = 107 nM
   TI
   LI
   LO
   TS
CP0174419
(2R)-2-[2-[[3-[2-[[(2R)-1-(dimethylamino)-3-methyl-1-oxobutan-2-yl]-(4-phenylphenyl)sulfonylamino]ethylcarbamoyl]benzoyl]amino]ethyl-(4-phenylphenyl)sulfonylamino]-3-methylbutanoic acid
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C48H55N5O9S2
 1
1
IC50 = 110 nM
   TI
   LI
   LO
   TS
CP0211045
(2R)-2-[2-benzamidoethyl-(4-phenylphenyl)sulfonylamino]-3-methylbutanoic acid
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C26H28N2O5S
 1
1
IC50 = 170 nM
   TI
   LI
   LO
   TS
CP0199497
US9206139, 2
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C19H22F3N3O3
 1
1
IC50 = 704 nM
   TI
   LI
   LO
   TS
CP0069428
US9206139, 1
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C18H20F3N3O3
 1
1
IC50 = 1750 nM
   TI
   LI
   LO
   TS
CP0069431
US9206139, 5
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C19H22F3N3O3
 1
1
IC50 = 4652 nM
   TI
   LI
   LO
   TS
CP0118960
US9206139, 3
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C20H22F3N3O3
 1
1
IC50 = 35000 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
 10
1 Activity = 0.75 nM
2 IC50 = 0.41 nM
3 IC50 = 0.43 nM
4 IC50 = 0.75 nM
5 IC50 = 1.8 nM
6 IC50 = 2 nM
7 IC50 = 5.1 nM
8 IC50 = 6 nM
9 IC50 = 10000 nM
10 Ki = 0.6 nM
CP0042804
(2R,3S)-N*4*-Hydroxy-2-isobutyl-N*1*-((S)-1-methylcarbamoyl-2-phenyl-ethyl)-3-(thiophen-2-ylsulfanylmethyl)-succinamide
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C23H31N3O4S2
 5
1 IC50 = 0.5 nM
2 IC50 = 0.73 nM
3 IC50 = 1 nM
4 IC50 = 4 nM
5 IC50 = 1800 nM
CP0110637
1-N,3-N-bis[4-[[(3R)-4-(hydroxyamino)-4-oxo-3-[(4-phenylphenyl)sulfonyl-propan-2-yloxyamino]butyl]amino]-4-oxobutyl]benzene-1,3-dicarboxamide
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C54H66N8O14S2
 1
1 IC50 = 9.8 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
 1
1 IC50 = 730 nM
CP0069428
US9206139, 1
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C18H20F3N3O3
 1
1 IC50 = 1800 nM
CP0199497
US9206139, 2
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C19H22F3N3O3
 1
1 IC50 = 3000 nM
CP0069431
US9206139, 5
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C19H22F3N3O3
 1
1 IC50 = 4700 nM
CP0118960
US9206139, 3
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C20H22F3N3O3
 1
1 IC50 = 35000 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 > 5000 nM
CP0117835
5-[3-fluoro-4-[(4-oxo-3,5,6,7-tetrahydrocyclopenta[d]pyrimidin-2-yl)sulfanylmethyl]phenyl]-N-[(2R)-3-methyl-1-(methylamino)-1-oxobutan-2-yl]furan-2-carboxamide
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C25H27FN4O4S
 1
1 IC50 > 5000 nM
CP0159081
N-[(1R)-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 > 5000 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 > 5000 nM
CP0069429
US9206139, 4
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C20H24F3N3O3
 1
1 IC50 > 100000 nM
CP0169348
4-[4-(thiiran-2-ylmethylsulfonyl)phenoxy]phenol
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C15H14O4S2
 1
1 Ki = 6 nM
CP0103388
2-((4-phenoxyphenylsulfonyl)methyl)thiirane
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C15H14O3S2
 2
1 Ki = 13.9 nM
2 Ki = 28 nM
Clinical Information about the Protein
Target 1 ( Matrix metalloproteinase-2 (MMP-2) )
Target Type Successful Target
Disease 8 Target-related Diseases  8
1 Lung cancer [ICD-11: 2C25.0]
2 Hepatic fibrosis [ICD-11: DB93.0]
3 Pancreatic cancer [ICD-11: 2C10]
4 Osteoarthritis [ICD-11: FA00-FA05]
5 Corneal ulcer [ICD-11: 9A76]
6 Hepatitis C virus infection [ICD-11: 1E51.1]
7 Multiple sclerosis [ICD-11: 8A40]
8 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Approved Drug(s) 1 Approved Drug  1
1 Prinomastat Approved
Lung cancer
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 Epigallocatechin gallate Phase 3
Hepatic fibrosis
2 Marimastat Phase 3
Pancreatic cancer
Discontinued Drug(s) 5 Discontinued Drugs  5
1 Tanomastat Discontinued in Phase 3
Osteoarthritis
2 GM6001 Discontinued in Phase 2
Corneal ulcer
3 RS-130830 Discontinued in Phase 2
Hepatitis C virus infection
4 BB-1101 Terminated
Multiple sclerosis
5 BB-3644 Terminated
Solid tumour/cancer
Target 2 ( MMP2 messenger RNA (MMP2 mRNA) )
Target Type Literature-reported Target