Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T52450 Target Info
Target Name Matrix metalloproteinase-1 (MMP-1)
Synonyms
Interstitial collagenase; Fibroblast collagenase; CLG
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Target Type Successful Target
Gene Name MMP1
Biochemical Class Peptidase
UniProt ID
MMP1_HUMAN
Co-Targets of This Target  Top
Co-Target Name Matrix metalloproteinase-2 (MMP-2) Successful Target
UniProt ID MMP2_HUMAN
Gene Name MMP2
Synonyms
TBE-1; Matrix metalloproteinase 2; CLG4A; 72 kDa type IV collagenase; 72 kDa gelatinase
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Representative Drug(s) Prinomastat Drug Info IC50 = 0.048 nM Click to Show More [1]
2 Marimastat Drug Info IC50 = 0.41 nM [1]
3 CIPEMASTAT Drug Info IC50 = 154 nM [4]
Co-Target Name Matrix metalloproteinase-7 (MMP-7) Successful Target
UniProt ID MMP7_HUMAN
Gene Name MMP7
Synonyms
Uterine metalloproteinase; Pump-1 protease; PUMP1; Matrin; Matrilysin; MPSL1
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Representative Drug(s) Marimastat Drug Info IC50 = 4.1 nM Click to Show More [1]
2 CIPEMASTAT Drug Info IC50 = 18.5 nM [2]
3 Prinomastat Drug Info IC50 = 54 nM [3]
Co-Target Name Matrix metalloproteinase-13 (MMP-13) Clinical trial Target
UniProt ID MMP13_HUMAN
Gene Name MMP13
Synonyms
Matrix metalloproteinase 13; Collagenase-3; Collagenase 3
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Representative Drug(s) Prinomastat Drug Info Ki = 0.038 nM Click to Show More [5]
2 CIPEMASTAT Drug Info Ki = 0.53 nM [2]
3 Marimastat Drug Info IC50 = 1.2 nM [1]
4 Apratastat Drug Info IC50 = 8 nM [11]
Co-Target Name Matrix metalloproteinase-9 (MMP-9) Clinical trial Target
UniProt ID MMP9_HUMAN
Gene Name MMP9
Synonyms
Matrix metalloproteinase 9; GELB; CLG4B; 92 kDa type IV collagenase; 92 kDa gelatinase
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Representative Drug(s) Prinomastat Drug Info IC50 = 0.048 nM Click to Show More [1]
2 Marimastat Drug Info IC50 = 0.79 nM [1]
3 CIPEMASTAT Drug Info IC50 = 2.4 nM [2]
Co-Target Name Matrix metalloproteinase-14 (MMP-14) Clinical trial Target
UniProt ID MMP14_HUMAN
Gene Name MMP14
Synonyms
Membrane-type-1 matrix metalloproteinase; Membrane-type matrix metalloproteinase 1; MTMMP1; MT1MMP; MT1-MMP; MT-MMP 1; MMP-X1
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Representative Drug(s) Prinomastat Drug Info IC50 = 0.3 nM Click to Show More [3]
2 Marimastat Drug Info IC50 = 1.82 nM [8]
3 CIPEMASTAT Drug Info IC50 = 23 nM [2]
Co-Target Name Matrix metalloproteinase-8 (MMP-8) Clinical trial Target
UniProt ID MMP8_HUMAN
Gene Name MMP8
Synonyms
PMNL-CL; PMNL collagenase; Neutrophil collagenase; CLG1
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Representative Drug(s) Prinomastat Drug Info IC50 < 0.4 nM Click to Show More [6]
2 Marimastat Drug Info IC50 = 0.47 nM [1]
3 CIPEMASTAT Drug Info Ki = 4 nM [5]
Co-Target Name TNF alpha converting enzyme (ADAM17) Clinical trial Target
UniProt ID ADA17_HUMAN
Gene Name ADAM17
Synonyms
TNFalpha converting enzyme; TNF-alpha-converting enzyme; TNF-alpha converting enzyme; TNF-alpha convertase; TACE; Snake venom-like protease; Disintegrin and metalloproteinase domain-containing protein 17; CSVP; CD156b antigen; CD156b; ADAM 17; A disintegrin and metalloproteinase domain 17
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Representative Drug(s) Marimastat Drug Info Ki = 0.4 nM Click to Show More [7]
2 Apratastat Drug Info IC50 = 4 nM [9]
3 Prinomastat Drug Info IC50 = 5.5 nM [10]
4 CIPEMASTAT Drug Info Ki = 230 nM [12]
Co-Target Name Matrix metalloproteinase-3 (MMP-3) Patented-recorded Target
UniProt ID MMP3_HUMAN
Gene Name MMP3
Synonyms
Transin-1; Stromelysin-1; STMY1; SL-1; MMP-3
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Representative Drug(s) Prinomastat Drug Info IC50 = 0.23 nM Click to Show More [3]
2 Marimastat Drug Info Ki = 2.4 nM [13]
3 CIPEMASTAT Drug Info Ki = 56 nM [12]
References  Top
REF 1 Phenoxyphenyl sulfone N-formylhydroxylamines (retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors. J Med Chem. 2002 Jan 3;45(1):219-32.
REF 2 Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13. J Med Chem. 2009 Jun 11;52(11):3523-38.
REF 3 N-i-Propoxy-N-biphenylsulfonylaminobutylhydroxamic acids as potent and selective inhibitors of MMP-2 and MT1-MMP. Bioorg Med Chem Lett. 2005 Mar 1;15(5):1321-6.
REF 4 Stereospecific synthesis of 5-substituted 2-bisarylthiocyclopentane carboxylic acids as specific matrix metalloproteinase inhibitors. J Med Chem. 2003 Aug 28;46(18):3840-52.
REF 5 Protease inhibitors: current status and future prospects. J Med Chem. 2000 Feb 10;43(3):305-41.
REF 6 Design, synthesis, and biological evaluation of potent thiazine- and thiazepine-based matrix metalloproteinase inhibitors. J Med Chem. 1999 Nov 4;42(22):4547-62.
REF 7 Design, synthesis and evaluation of novel azasugar-based MMP/ADAM inhibitors. Bioorg Med Chem Lett. 2003 Aug 18;13(16):2741-4.
REF 8 Inhibition of membrane-type 1 matrix metalloproteinase by hydroxamate inhibitors: an examination of the subsite pocket. J Med Chem. 1998 Apr 9;41(8):1209-17.
REF 9 Identification of novel TACE inhibitors compatible with topical application. Bioorg Med Chem Lett. 2017 Apr 15;27(8):1848-53.
REF 10 New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors. J Med Chem. 1999 Nov 18;42(23):4890-908.
REF 11 Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates. Bioorg Med Chem Lett. 2006 Mar 15;16(6):1605-9.
REF 12 A cassette-dosing approach for improvement of oral bioavailability of dual TACE/MMP inhibitors. Bioorg Med Chem Lett. 2006 May 15;16(10):2632-6.
REF 13 Design, synthesis, and structure-activity relationships of macrocyclic hydroxamic acids that inhibit tumor necrosis factor alpha release in vitro and in vivo. J Med Chem. 2001 Aug 2;44(16):2636-60.

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