Target Validation Information | |||||
---|---|---|---|---|---|
Target ID | T52450 | ||||
Target Name | Interstitial collagenase | ||||
Target Type | Successful |
||||
Drug Potency against Target | Ro-37-9790 | Drug Info | IC50 = 4.9 nM | ||
Marimastat | Drug Info | IC50 = 5 nM | [552497] | ||
4-Butoxy-N-hydroxycarbamoylmethyl-benzamide | Drug Info | IC50 = 920 nM | [527800] | ||
CIPEMASTAT | Drug Info | Ki = 0.3 nM | [528065] | ||
4-(4-Methoxy-benzenesulfonyl)-butane-2-thiol | Drug Info | IC50 = 8000 nM | [525485] | ||
3-(4-Phenoxy-benzenesulfonyl)-propane-1-thiol | Drug Info | IC50 = 1500 nM | [525485] | ||
N-(Ethylphosphoryl)-L-isoleucyl-L-Trp-NHCH3 | Drug Info | Ki = 900 nM | [531455] | ||
BMS 275291 | Drug Info | Ki = 9 nM | [537564] | ||
3-Benzenesulfonyl-heptanoic acid hydroxyamide | Drug Info | IC50 = 300 nM | [525813] | ||
PKF-242-484 | Drug Info | Ki = 1 nM | [528065] | ||
3-(4-Methoxy-benzenesulfonyl)-cyclohexanethiol | Drug Info | IC50 = 1000 nM | [525535] | ||
N-Hydroxy-4-(4-methoxy-phenyl)-4-oxo-butyramide | Drug Info | Ki = 33 nM | [527800] | ||
L-696418 | Drug Info | Ki = 760 nM | |||
Prinomastat | Drug Info | Ki = 8.3 nM | |||
BB-3644 | Drug Info | IC50 = 10 nM | [552497] | ||
ILOMASTAT | Drug Info | IC50 = 0.4 nM | [529683] | ||
TMI-05 | Drug Info | IC50 = 33 nM | [527982] | ||
4-(4-Butoxy-phenyl)-N-hydroxy-4-oxo-butyramide | Drug Info | IC50 = 920 nM | [527800] | ||
RS-39066 | Drug Info | IC50 = 6.9 nM | |||
3-(4-Phenoxy-benzenesulfonyl)-cyclohexanethiol | Drug Info | IC50 = 1700 nM | [525535] | ||
3-Benzenesulfinyl-heptanoic acid hydroxyamide | Drug Info | IC50 = 93 nM | [525813] | ||
3-Cyclohexanesulfonyl-heptanoic acid hydroxyamide | Drug Info | IC50 = 54 nM | [525813] | ||
Ro-31-4724 | Drug Info | IC50 = 40 nM | [527073] | ||
SR-973 | Drug Info | Ki = 21 nM | [528025] | ||
CIPEMASTAT | Drug Info | IC50 = 7 nM | |||
MMI270 | Drug Info | IC50 = 33 nM | [527922] | ||
N-Hydroxycarbamoylmethyl-4-phenoxy-benzamide | Drug Info | IC50 = 22 nM | [527800] | ||
3-(4-Methoxy-benzenesulfonyl)-hexane-1-thiol | Drug Info | IC50 = 1500 nM | [525485] | ||
3-(4-Methoxy-benzenesulfonyl)-pentane-1-thiol | Drug Info | IC50 = 600 nM | [525485] | ||
N-Hydroxycarbamoylmethyl-4-methoxy-benzamide | Drug Info | Ki = 33 nM | [527800] | ||
N-Hydroxy-4-oxo-4-(4-phenoxy-phenyl)-butyramide | Drug Info | IC50 = 22 nM | [527800] | ||
BB-1101 | Drug Info | IC50 = 2.2 nM | [534793] | ||
SC-44463 | Drug Info | IC50 = 20 nM | [526680] | ||
RS-130830 | Drug Info | Ki = 590 nM | [527412] | ||
RO-319790 | Drug Info | IC50 = 5 nM | [534791] | ||
Action against Disease Model | XL784 | Both a MMP-1 inhibitor and P1pal-7 significantly promote apoptosis in breast t uMor xenografts and inhibit metastasis to the lungs by up to 88%. Biochemical analysis of xenograft t uMors treated with P1pal-7 or MMP-1 inhibitor showed attenuated Akt activity | [552963] | Drug Info | |
The Effect of Target Knockout, Knockdown or Genetic Variations | Spontaneous retarded lung alveolar development and diminished surface area; Impaired osteocyte processes and collagen cleavage | ||||
References | |||||
Ref 552497 | Recent developments in the design of specific Matrix Metalloproteinase inhibitors aided by structural and computational studies. Curr Pharm Des. 2005;11(3):295-322. | ||||
Ref 552963 | Blockade of PAR1 signaling with cell-penetrating pepducins inhibits Akt survival pathways in breast cancer cells and suppresses tumor survival and metastasis. Cancer Res. 2009 Aug 1;69(15):6223-31. doi: 10.1158/0008-5472.CAN-09-0187. Epub 2009 Jul 21. | ||||
Ref 527800 | J Med Chem. 2005 Oct 20;48(21):6585-96.Receptor flexibility in de novo ligand design and docking. | ||||
Ref 528065 | Bioorg Med Chem Lett. 2006 May 15;16(10):2632-6. Epub 2006 Mar 3.A cassette-dosing approach for improvement of oral bioavailability of dual TACE/MMP inhibitors. | ||||
Ref 525485 | Bioorg Med Chem Lett. 1999 Apr 5;9(7):943-8.Discovery of a novel series of selective MMP inhibitors: identification of the gamma-sulfone-thiols. | ||||
Ref 525485 | Bioorg Med Chem Lett. 1999 Apr 5;9(7):943-8.Discovery of a novel series of selective MMP inhibitors: identification of the gamma-sulfone-thiols. | ||||
Ref 531455 | J Med Chem. 1990 Jan;33(1):263-73.Phosphoramidate peptide inhibitors of human skin fibroblast collagenase. | ||||
Ref 537564 | Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66. | ||||
Ref 525813 | J Med Chem. 2000 Jun 15;43(12):2324-31.Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents. | ||||
Ref 528065 | Bioorg Med Chem Lett. 2006 May 15;16(10):2632-6. Epub 2006 Mar 3.A cassette-dosing approach for improvement of oral bioavailability of dual TACE/MMP inhibitors. | ||||
Ref 525535 | Bioorg Med Chem Lett. 1999 Jul 5;9(13):1757-60.Synthesis and identification of conformationally constrained selective MMP inhibitors. | ||||
Ref 527800 | J Med Chem. 2005 Oct 20;48(21):6585-96.Receptor flexibility in de novo ligand design and docking. | ||||
Ref 552497 | Recent developments in the design of specific Matrix Metalloproteinase inhibitors aided by structural and computational studies. Curr Pharm Des. 2005;11(3):295-322. | ||||
Ref 529683 | Bioorg Med Chem. 2008 Sep 15;16(18):8745-59. Epub 2008 Jul 20.Introduction of the 4-(4-bromophenyl)benzenesulfonyl group to hydrazide analogs of Ilomastat leads to potent gelatinase B (MMP-9) inhibitors with improved selectivity. | ||||
Ref 527982 | Bioorg Med Chem Lett. 2006 Mar 15;16(6):1605-9. Epub 2006 Jan 19.Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates. | ||||
Ref 527800 | J Med Chem. 2005 Oct 20;48(21):6585-96.Receptor flexibility in de novo ligand design and docking. | ||||
Ref 525535 | Bioorg Med Chem Lett. 1999 Jul 5;9(13):1757-60.Synthesis and identification of conformationally constrained selective MMP inhibitors. | ||||
Ref 525813 | J Med Chem. 2000 Jun 15;43(12):2324-31.Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents. | ||||
Ref 525813 | J Med Chem. 2000 Jun 15;43(12):2324-31.Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents. | ||||
Ref 527073 | J Med Chem. 2004 May 20;47(11):2761-7.Receptor flexibility in the in silico screening of reagents in the S1' pocket of human collagenase. | ||||
Ref 528025 | Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63. Epub 2006 Feb 10.Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors. | ||||
Ref 527922 | Bioorg Med Chem Lett. 2006 Feb 15;16(4):964-8. Epub 2005 Dec 9.The discovery of a potent and selective lethal factor inhibitor for adjunct therapy of anthrax infection. | ||||
Ref 527800 | J Med Chem. 2005 Oct 20;48(21):6585-96.Receptor flexibility in de novo ligand design and docking. | ||||
Ref 525485 | Bioorg Med Chem Lett. 1999 Apr 5;9(7):943-8.Discovery of a novel series of selective MMP inhibitors: identification of the gamma-sulfone-thiols. | ||||
Ref 525485 | Bioorg Med Chem Lett. 1999 Apr 5;9(7):943-8.Discovery of a novel series of selective MMP inhibitors: identification of the gamma-sulfone-thiols. | ||||
Ref 527800 | J Med Chem. 2005 Oct 20;48(21):6585-96.Receptor flexibility in de novo ligand design and docking. | ||||
Ref 527800 | J Med Chem. 2005 Oct 20;48(21):6585-96.Receptor flexibility in de novo ligand design and docking. | ||||
Ref 534793 | Bioorg Med Chem Lett. 1998 Jun 16;8(12):1443-8.Broad spectrum matrix metalloproteinase inhibitors: an examination of succinamide hydroxamate inhibitors with P1 C alpha gem-disubstitution. | ||||
Ref 526680 | J Med Chem. 2003 Jul 31;46(16):3514-25.A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers. | ||||
Ref 527412 | Bioorg Med Chem Lett. 2005 Feb 15;15(4):1101-6.Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13). | ||||
Ref 534791 | Bioorg Med Chem Lett. 1998 May 19;8(10):1163-8.The asymmetric synthesis and in vitro characterization of succinyl mercaptoalcohol and mercaptoketone inhibitors of matrix metalloproteinases. |
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