| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T52450 | ||||
| Target Name | Matrix metalloproteinase-1 (MMP-1) | ||||
| Type of Target |
Successful |
||||
| Drug Potency against Target | BB-3644 | Drug Info | IC50 = 10 nM | [17] | |
| BMS 275291 | Drug Info | Ki = 9 nM | [16] | ||
| Marimastat | Drug Info | IC50 = 5 nM | [17] | ||
| Prinomastat | Drug Info | Ki = 8.3 nM | |||
| 3-(4-Methoxy-benzenesulfonyl)-cyclohexanethiol | Drug Info | IC50 = 1000 nM | [2] | ||
| 3-(4-Methoxy-benzenesulfonyl)-hexane-1-thiol | Drug Info | IC50 = 1500 nM | [1] | ||
| 3-(4-Methoxy-benzenesulfonyl)-pentane-1-thiol | Drug Info | IC50 = 600 nM | [1] | ||
| 3-(4-Phenoxy-benzenesulfonyl)-cyclohexanethiol | Drug Info | IC50 = 1700 nM | [2] | ||
| 3-(4-Phenoxy-benzenesulfonyl)-propane-1-thiol | Drug Info | IC50 = 1500 nM | [1] | ||
| 3-Benzenesulfinyl-heptanoic acid hydroxyamide | Drug Info | IC50 = 93 nM | [3] | ||
| 3-Benzenesulfonyl-heptanoic acid hydroxyamide | Drug Info | IC50 = 300 nM | [3] | ||
| 3-Cyclohexanesulfonyl-heptanoic acid hydroxyamide | Drug Info | IC50 = 54 nM | [3] | ||
| 4-(4-Butoxy-phenyl)-N-hydroxy-4-oxo-butyramide | Drug Info | IC50 = 920 nM | [7] | ||
| 4-(4-Methoxy-benzenesulfonyl)-butane-2-thiol | Drug Info | IC50 = 8000 nM | [1] | ||
| 4-Butoxy-N-hydroxycarbamoylmethyl-benzamide | Drug Info | IC50 = 920 nM | [7] | ||
| Apratastat | Drug Info | IC50 = 33 nM | [9] | ||
| BB-1101 | Drug Info | IC50 = 2.2 nM | [15] | ||
| CIPEMASTAT | Drug Info | Ki = 0.3 nM | [11] | ||
| CIPEMASTAT | Drug Info | IC50 = 7 nM | |||
| GM6001 | Drug Info | IC50 = 0.4 nM | [12] | ||
| L-696418 | Drug Info | Ki = 760 nM | |||
| MMI270 | Drug Info | IC50 = 33 nM | [8] | ||
| N-(Ethylphosphoryl)-L-isoleucyl-L-Trp-NHCH3 | Drug Info | Ki = 900 nM | [13] | ||
| N-Hydroxy-4-(4-methoxy-phenyl)-4-oxo-butyramide | Drug Info | Ki = 33 nM | [7] | ||
| N-Hydroxy-4-oxo-4-(4-phenoxy-phenyl)-butyramide | Drug Info | IC50 = 22 nM | [7] | ||
| N-Hydroxycarbamoylmethyl-4-methoxy-benzamide | Drug Info | Ki = 33 nM | [7] | ||
| N-Hydroxycarbamoylmethyl-4-phenoxy-benzamide | Drug Info | IC50 = 22 nM | [7] | ||
| PKF-242-484 | Drug Info | Ki = 1 nM | [11] | ||
| Ro-31-4724 | Drug Info | IC50 = 40 nM | [5] | ||
| RO-319790 | Drug Info | IC50 = 5 nM | [14] | ||
| Ro-37-9790 | Drug Info | IC50 = 4.9 nM | |||
| RS-130830 | Drug Info | Ki = 590 nM | [6] | ||
| RS-39066 | Drug Info | IC50 = 6.9 nM | |||
| SC-44463 | Drug Info | IC50 = 20 nM | [4] | ||
| SR-973 | Drug Info | Ki = 21 nM | [10] | ||
| Action against Disease Model | XL784 | Drug Info | 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 | [18] | |
| References | |||||
| REF 1 | Discovery of a novel series of selective MMP inhibitors: identification of the gamma-sulfone-thiols. Bioorg Med Chem Lett. 1999 Apr 5;9(7):943-8. | ||||
| REF 2 | Synthesis and identification of conformationally constrained selective MMP inhibitors. Bioorg Med Chem Lett. 1999 Jul 5;9(13):1757-60. | ||||
| REF 3 | Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents. J Med Chem. 2000 Jun 15;43(12):2324-31. | ||||
| REF 4 | A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers. J Med Chem. 2003 Jul 31;46(16):3514-25. | ||||
| REF 5 | Receptor flexibility in the in silico screening of reagents in the S1' pocket of human collagenase. J Med Chem. 2004 May 20;47(11):2761-7. | ||||
| REF 6 | Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13). Bioorg Med Chem Lett. 2005 Feb 15;15(4):1101-6. | ||||
| REF 7 | Receptor flexibility in de novo ligand design and docking. J Med Chem. 2005 Oct 20;48(21):6585-96. | ||||
| REF 8 | The discovery of a potent and selective lethal factor inhibitor for adjunct therapy of anthrax infection. Bioorg Med Chem Lett. 2006 Feb 15;16(4):964-8. | ||||
| REF 9 | Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates. Bioorg Med Chem Lett. 2006 Mar 15;16(6):1605-9. | ||||
| REF 10 | Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors. Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63. | ||||
| REF 11 | 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 12 | Introduction of the 4-(4-bromophenyl)benzenesulfonyl group to hydrazide analogs of Ilomastat leads to potent gelatinase B (MMP-9) inhibitors with i... Bioorg Med Chem. 2008 Sep 15;16(18):8745-59. | ||||
| REF 13 | Phosphoramidate peptide inhibitors of human skin fibroblast collagenase. J Med Chem. 1990 Jan;33(1):263-73. | ||||
| REF 14 | The asymmetric synthesis and in vitro characterization of succinyl mercaptoalcohol and mercaptoketone inhibitors of matrix metalloproteinases. Bioorg Med Chem Lett. 1998 May 19;8(10):1163-8. | ||||
| REF 15 | Broad spectrum matrix metalloproteinase inhibitors: an examination of succinamide hydroxamate inhibitors with P1 C alpha gem-disubstitution. Bioorg Med Chem Lett. 1998 Jun 16;8(12):1443-8. | ||||
| REF 16 | Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66. | ||||
| REF 17 | 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 18 | 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. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.