ilomastat [Ligand Id: 7409] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL19611 (Galardin, Gm6001, Ilomastat) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ADAM10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5028] [GtoPdb: 1658] [UniProtKB: O14672] | ||||||||
| ChEMBL | Inhibition of ADAM10 | B | 6.58 | pIC50 | 263 | nM | IC50 | J Med Chem (2009) 52: 5732-5747 [PMID:19715320] |
| GtoPdb | Measured in an in vitro assay. | - | 8.09 | pIC50 | 8.1 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 6071-4 [PMID:15546732] |
| ChEMBL | In vitro inhibition of A disintegrin and metalloprotease domain 10 (ADAM10) | B | 8.09 | pIC50 | 8.1 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 6071-6074 [PMID:15546732] |
| ADAM12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5030] [GtoPdb: 1660] [UniProtKB: O43184] | ||||||||
| ChEMBL | Inhibition of A disintegrin and metalloprotease domain 12 (ADAM12) binding in cell based assay | B | 8.23 | pIC50 | 5.93 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 6071-6074 [PMID:15546732] |
| GtoPdb | Measured in a cell-based assay. | - | 8.23 | pIC50 | 5.93 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 6071-4 [PMID:15546732] |
| ADAM17 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3706] [GtoPdb: 1662] [UniProtKB: P78536] | ||||||||
| ChEMBL | Inhibition of TACE | B | 7.88 | pIC50 | 13.1 | nM | IC50 | J Med Chem (2009) 52: 5732-5747 [PMID:19715320] |
| GtoPdb | Measured in an in vitro assay. | - | 8.12 | pIC50 | 7.5 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 6071-4 [PMID:15546732] |
| ChEMBL | In vitro inhibition of A disintegrin and metalloprotease domain 17 (ADAM17, TACE) | B | 8.12 | pIC50 | 7.5 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 6071-6074 [PMID:15546732] |
| ADAM9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5982] [GtoPdb: 1657] [UniProtKB: Q13443] | ||||||||
| ChEMBL | Inhibition of ADAM9 | B | 7.25 | pIC50 | 56.3 | nM | IC50 | J Med Chem (2009) 52: 5732-5747 [PMID:19715320] |
| GtoPdb | Measured in an in vitro assay. | - | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 6071-4 [PMID:15546732] |
| ChEMBL | In vitro inhibition of A disintegrin and metalloprotease domain 9 (ADAM9) | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 6071-6074 [PMID:15546732] |
| ADAMTS4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2318] [GtoPdb: 1677] [UniProtKB: O75173] | ||||||||
| ChEMBL | Inhibition of human recombinant ADAMTS4 expressed in HEk293 cells using FAM-AEwLQGRPISIAK-TAMRA as substrate measured for 15 mins by fluorometric analysis | B | 6.32 | pIC50 | 480 | nM | IC50 | Eur J Med Chem (2013) 62: 379-394 [PMID:23376997] |
| ADAMTS5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2285] [GtoPdb: 1678] [UniProtKB: Q9UNA0] | ||||||||
| ChEMBL | Inhibition of human recombinant ADAMTS5 expressed in HEK293 cells using Abz-TESEwSRGAIY-Dpa-KK as substrate measured for 2 hrs by fluorometric analysis | B | 6.3 | pIC50 | 500 | nM | IC50 | Eur J Med Chem (2013) 62: 379-394 [PMID:23376997] |
| MMP1/Matrix metalloproteinase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956] | ||||||||
| ChEMBL | Evaluated for inhibitory activity against Human fibroblast collagenase (HFC) | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 337-342 |
| ChEMBL | Inhibition of human fibroblast collagenase, matrix metalloprotease-1 | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 349-352 |
| ChEMBL | Inhibition of MMP-1 (unknown origin) | B | 9.4 | pKi | 0.4 | nM | Ki | J Med Chem (2022) 65: 10709-10754 [PMID:35969157] |
| GtoPdb | - | - | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 47-50 [PMID:14684295] |
| ChEMBL | Inhibition of matrix metalloprotease-1 (MMP-1) | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 47-50 [PMID:14684295] |
| ChEMBL | Inhibitory activity against MMP1 | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2006) 49: 456-458 [PMID:16420030] |
| ChEMBL | Inhibition of MMP1 | B | 8.48 | pIC50 | 3.3 | nM | IC50 | J Biol Chem (2007) 282: 27781-27791 [PMID:17623656] |
| ChEMBL | Inhibition of human recombinant MMP1 using Mca-Lys-Pro- Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate incubated for 2 hrs prior to substrate addition measured every 15 secs for 15 mins by fluorometric analysis | B | 8.48 | pIC50 | 3.3 | nM | IC50 | Eur J Med Chem (2013) 62: 379-394 [PMID:23376997] |
| ChEMBL | Inhibition of matrix metalloprotease-1 | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1783-1786 [PMID:12729664] |
| ChEMBL | Inhibition of human recombinant interstitial collagenase MMP-1 at 100 uM | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 1637-1642 |
| ChEMBL | Inhibition of MMP1 | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Bioorg Med Chem (2007) 15: 4753-4766 [PMID:17512742] |
| ChEMBL | Activity against Matrix metalloprotease-1 (MMP-1). | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (1998) 41: 1209-1217 [PMID:9548812] |
| ChEMBL | Inhibition of MMP-1 (unknown origin) | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2022) 65: 10709-10754 [PMID:35969157] |
| GtoPdb | - | - | 9.25 | pIC50 | 0.56 | nM | IC50 | J Med Chem (2022) 65: 8493-8510 [PMID:35687819] |
| ChEMBL | Inhibition of recombinant human MMP1 using MOCAc-Lys-Pro-Leu-Gly-Leu-A2pr(Dnp)-Ala-Arg-NH2 as substrate preincubated for 15 mins followed by substrate addition by fluroscence based assay | B | 9.25 | pIC50 | 0.56 | nM | IC50 | J Med Chem (2022) 65: 8493-8510 [PMID:35687819] |
| ChEMBL | Inhibition of human recombinant pro-MMP1 by spectrofluorimeter | B | 9.4 | pIC50 | 0.4 | nM | IC50 | Bioorg Med Chem (2008) 16: 8745-8759 [PMID:18782669] |
| ChEMBL | Inhibition of MMP1 | B | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2011) 54: 4350-4364 [PMID:21548582] |
| MMP12/Matrix metalloproteinase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4393] [GtoPdb: 1636] [UniProtKB: P39900] | ||||||||
| ChEMBL | Inhibition of human recombinant MMP12 using Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 as substrate incubated for 10 mins prior to substrate addition by spectrophotometry | B | 8.42 | pKi | 3.8 | nM | Ki | Medchemcomm (2013) 4: 432-442 |
| ChEMBL | Time dependent inhibition of human recombinant MMP12 by SPR assay | B | 9.28 | pKi | 0.52 | nM | Ki | Medchemcomm (2013) 4: 432-442 |
| ChEMBL | Inhibitory activity against MMP12 | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2006) 49: 456-458 [PMID:16420030] |
| ChEMBL | Inhibition of matrix metalloprotease-12 (MMP-12) | B | 7.89 | pIC50 | 13 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 47-50 [PMID:14684295] |
| GtoPdb | - | - | 7.89 | pIC50 | 13 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 47-50 [PMID:14684295] |
| ChEMBL | Inhibition of recombinant human MMP12 catalytic domain (Gly106 to Gly26 residues) expressed in Escherichia coli BL21 codon plus using Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 as substrate by fluorescence assay | B | 8.28 | pIC50 | 5.2 | nM | IC50 | ACS Med Chem Lett (2018) 9: 137-142 [PMID:29456802] |
| ChEMBL | Inhibition of MMP12 catalytic domain | B | 8.29 | pIC50 | 5.1 | nM | IC50 | J Biol Chem (2007) 282: 27781-27791 [PMID:17623656] |
| ChEMBL | Inhibition of recombinant human MMP12 catalytic domain (Gly106 to Gly263 residues) expressed in Escherichia coli BL21 Codon Plus cells using 5-FAM/QXL520 FRET peptide as substrate preincubated for 15 mins followed by substrate addition and measured at 3 mins interval for 60 mins by fluorescence assay | B | 8.62 | pIC50 | 2.4 | nM | IC50 | J Med Chem (2020) 63: 12911-12920 [PMID:33107733] |
| ChEMBL | Inhibition of MMP12 | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2008) 51: 3449-3459 [PMID:18494455] |
| ChEMBL | Inhibition of recombinant human MMP12 using MOCAc-Pro-Leu-Gly-Leu-A2pr(Dnp)-Ala-Arg-NH2 as substrate preincubated for 15 mins followed by substrate addition by fluroscence based assay | B | 9.34 | pIC50 | 0.46 | nM | IC50 | J Med Chem (2022) 65: 8493-8510 [PMID:35687819] |
| GtoPdb | - | - | 9.34 | pIC50 | 0.46 | nM | IC50 | J Med Chem (2022) 65: 8493-8510 [PMID:35687819] |
| MMP13/Matrix metalloproteinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL280] [GtoPdb: 1637] [UniProtKB: P45452] | ||||||||
| ChEMBL | Inhibition of human recombinant MMP13 catalytic domain | B | 8.28 | pIC50 | 5.2 | nM | IC50 | J Biol Chem (2007) 282: 27781-27791 [PMID:17623656] |
| ChEMBL | Inhibition of human recombinant MMP13 using Mca-Lys-Pro- Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate incubated for 2 hrs prior to substrate addition measured every 15 secs for 15 mins by fluorometric analysis | B | 8.28 | pIC50 | 5.2 | nM | IC50 | Eur J Med Chem (2013) 62: 379-394 [PMID:23376997] |
| GtoPdb | - | - | 9.55 | pIC50 | 0.28 | nM | IC50 | J Med Chem (2022) 65: 8493-8510 [PMID:35687819] |
| ChEMBL | Inhibition of recombinant human MMP13 using MOCAc-Pro-Leu-Gly-Leu-A2pr(Dnp)-Ala-Arg-NH2 as substrate preincubated for 15 mins followed by substrate addition by fluroscence based assay | B | 9.55 | pIC50 | 0.28 | nM | IC50 | J Med Chem (2022) 65: 8493-8510 [PMID:35687819] |
| MMP14/Matrix metalloproteinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3869] [GtoPdb: 1638] [UniProtKB: P50281] | ||||||||
| ChEMBL | Inhibition of matrix metalloprotease-14 (MMP-14) | B | 7.64 | pIC50 | 23 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 47-50 [PMID:14684295] |
| ChEMBL | Inhibitory activity against MMP14 | B | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (2006) 49: 456-458 [PMID:16420030] |
| GtoPdb | - | - | 7.64 | pIC50 | 23 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 47-50 [PMID:14684295] |
| ChEMBL | Activity against deletion mutant of MT1-MMP lacking the transmembrane domain (deltaMT1) | B | 7.87 | pIC50 | 13.4 | nM | IC50 | J Med Chem (1998) 41: 1209-1217 [PMID:9548812] |
| ChEMBL | Inhibition of MMP14 | B | 7.87 | pIC50 | 13.4 | nM | IC50 | Bioorg Med Chem (2007) 15: 4753-4766 [PMID:17512742] |
| ChEMBL | Inhibition of MMP-14 (unknown origin) | B | 7.87 | pIC50 | 13.4 | nM | IC50 | J Med Chem (2022) 65: 10709-10754 [PMID:35969157] |
| ChEMBL | Inhibition of human recombinant MMP14 catalytic domain by spectrofluorimeter | B | 8.28 | pIC50 | 5.2 | nM | IC50 | Bioorg Med Chem (2008) 16: 8745-8759 [PMID:18782669] |
| ChEMBL | Inhibition of human recombinant MMP14 catalytic domain using Mca-Lys-Pro- Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate incubated for 2 hrs prior to substrate addition measured every 15 secs for 15 mins by fluorometric analysis | B | 8.33 | pIC50 | 4.7 | nM | IC50 | Eur J Med Chem (2013) 62: 379-394 [PMID:23376997] |
| ChEMBL | Inhibition of MMP14 catalytic domain | B | 8.33 | pIC50 | 4.7 | nM | IC50 | J Biol Chem (2007) 282: 27781-27791 [PMID:17623656] |
| ChEMBL | Inhibition of recombinant human MMP14 using MOCAc-Lys-Pro-Leu-Gly-Leu-A2pr(Dnp)-Ala-Arg-NH2 as substrate preincubated for 15 mins followed by substrate addition by fluroscence based assay | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2022) 65: 8493-8510 [PMID:35687819] |
| GtoPdb | - | - | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2022) 65: 8493-8510 [PMID:35687819] |
| ChEMBL | Inhibition of MMP14 | B | 9.39 | pIC50 | 0.41 | nM | IC50 | J Med Chem (2011) 54: 4350-4364 [PMID:21548582] |
| MMP15/Matrix metalloproteinase 15 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2963] [GtoPdb: 1639] [UniProtKB: P51511] | ||||||||
| GtoPdb | - | - | 8.1 | pIC50 | 8 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 47-50 [PMID:14684295] |
| ChEMBL | Inhibition of matrix metalloprotease-15 (MMP-15) | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 47-50 [PMID:14684295] |
| ChEMBL | Inhibitory activity against MMP15 | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2006) 49: 456-458 [PMID:16420030] |
| MMP16/Matrix metalloproteinase 16 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2200] [GtoPdb: 1640] [UniProtKB: P51512] | ||||||||
| ChEMBL | Inhibition of matrix metalloprotease-16 (MMP-16) | B | 8.1 | pIC50 | 8 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 47-50 [PMID:14684295] |
| ChEMBL | Inhibitory activity against MMP16 | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2006) 49: 456-458 [PMID:16420030] |
| GtoPdb | - | - | 8.1 | pIC50 | 8 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 47-50 [PMID:14684295] |
| MMP17/Matrix metalloproteinase 17 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2937] [GtoPdb: 1641] [UniProtKB: Q9ULZ9] | ||||||||
| ChEMBL | Inhibition of MMP17 catalytic domain | B | 8.47 | pIC50 | 3.4 | nM | IC50 | J Biol Chem (2007) 282: 27781-27791 [PMID:17623656] |
| GtoPdb | - | - | 8.47 | pIC50 | 3.4 | nM | IC50 | J Biol Chem (2007) 282: 27781-91 [PMID:17623656] |
| MMP2/Matrix metalloproteinase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL333] [GtoPdb: 1629] [UniProtKB: P08253] | ||||||||
| ChEMBL | Inhibition of Matrix metalloprotease-2 | B | 9.24 | pKi | 0.57 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 567-570 [PMID:11229773] |
| ChEMBL | Binding affinity towards 72 kDa gelatinase (Matrix metalloprotease-2) | B | 9.41 | pKi | 0.39 | nM | Ki | J Med Chem (1998) 41: 199-223 [PMID:9457244] |
| ChEMBL | Inhibition of MMP-2 (unknown origin) | B | 9.41 | pKi | 0.39 | nM | Ki | J Med Chem (2022) 65: 10709-10754 [PMID:35969157] |
| ChEMBL | Inhibition of recombinant human MMP2 using MOCAc-Lys-Pro-Leu-Gly-Leu-A2pr(Dnp)-Ala-Arg-N2 as substrate preincubated for 10 to 15 mins followed by substrate addition and measured after 60 to 120 mins by fluorescence based assay | B | 9.55 | pKi | 0.28 | nM | Ki | J Med Chem (2023) 66: 822-836 [PMID:36595440] |
| ChEMBL | Inhibition of MMP2 | B | 8 | pIC50 | 10 | nM | IC50 | J Biol Chem (2007) 282: 27781-27791 [PMID:17623656] |
| ChEMBL | Inhibition of human recombinant MMP2 using Mca-Lys-Pro- Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate incubated for 2 hrs prior to substrate addition measured every 15 secs for 15 mins by fluorometric analysis | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2013) 62: 379-394 [PMID:23376997] |
| GtoPdb | - | - | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 47-50 [PMID:14684295] |
| ChEMBL | Inhibition of matrix metalloprotease-2 (MMP-2) | B | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 47-50 [PMID:14684295] |
| ChEMBL | Inhibitory activity against MMP2 | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2006) 49: 456-458 [PMID:16420030] |
| ChEMBL | Activity against Matrix metalloprotease-2 (MMP-2). | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (1998) 41: 1209-1217 [PMID:9548812] |
| ChEMBL | Inhibition of MMP2 | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Bioorg Med Chem (2007) 15: 4753-4766 [PMID:17512742] |
| ChEMBL | Inhibition of MMP-2 (unknown origin) | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2022) 65: 10709-10754 [PMID:35969157] |
| ChEMBL | Inhibition of human recombinant MMP2 using Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 as substrate preincubated for 60 mins followed by substrate addition by fluorimetric analysis | B | 9.03 | pIC50 | 0.94 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 2174-2178 [PMID:27038494] |
| ChEMBL | Inhibition of human MMP-2 by fluorometric assay | B | 9.37 | pIC50 | 0.42 | nM | IC50 | J Med Chem (2020) 63: 14805-14820 [PMID:33210531] |
| ChEMBL | Inhibition of Matrix metalloprotease-2 | B | 9.4 | pIC50 | 0.4 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1783-1786 [PMID:12729664] |
| ChEMBL | Inhibition of human recombinant pro-MMP2 by spectrofluorimeter | B | 9.4 | pIC50 | 0.4 | nM | IC50 | Bioorg Med Chem (2008) 16: 8745-8759 [PMID:18782669] |
| ChEMBL | Inhibition of MMP-2 (unknown origin) assessed as inhibition constant | B | 9.41 | pIC50 | 0.39 | nM | IC50 | Eur J Med Chem (2020) 194: 112260-112260 [PMID:32224379] |
| GtoPdb | - | - | 9.72 | pIC50 | 0.19 | nM | IC50 | J Med Chem (2022) 65: 8493-8510 [PMID:35687819] |
| ChEMBL | Inhibition of recombinant human MMP2 using MOCAc-Lys-Pro-Leu-Gly-Leu-A2pr(Dnp)-Ala-Arg-N2 as substrate preincubated for 10 to 15 mins followed by substrate addition and measured after 60 to 120 mins by fluorescence based assay | B | 9.72 | pIC50 | 0.19 | nM | IC50 | J Med Chem (2023) 66: 822-836 [PMID:36595440] |
| ChEMBL | Inhibition of recombinant human MMP2 using MOCAc-Lys-Pro-Leu-Gly-Leu-A2pr(Dnp)-Ala-Arg-NH2 as a substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluroscence based assay | B | 9.72 | pIC50 | 0.19 | nM | IC50 | J Med Chem (2022) 65: 8493-8510 [PMID:35687819] |
| ChEMBL | Inhibition of human matrix metalloprotease-2 | B | 9.98 | pIC50 | 0.1 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2843-2846 [PMID:14611841] |
| MMP26/Matrix metalloproteinase 26 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4707] [GtoPdb: 1648] [UniProtKB: Q9NRE1] | ||||||||
| ChEMBL | Inhibition of matrix metalloprotease-26 (MMP-26) | B | 7.77 | pIC50 | 17 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 47-50 [PMID:14684295] |
| ChEMBL | Inhibitory activity against MMP26 | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2006) 49: 456-458 [PMID:16420030] |
| GtoPdb | - | - | 7.77 | pIC50 | 17 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 47-50 [PMID:14684295] |
| MMP3/Matrix metalloproteinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL283] [GtoPdb: 1630] [UniProtKB: P08254] | ||||||||
| ChEMBL | Inhibition of human fibroblast stromelysin, matrix metalloprotease-3 | B | 7.34 | pKi | 46 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 349-352 |
| ChEMBL | Inhibition of MMP-3 (unknown origin) | B | 7.57 | pKi | 27 | nM | Ki | J Med Chem (2022) 65: 10709-10754 [PMID:35969157] |
| ChEMBL | Inhibition of Matrix metalloprotease-3 | B | 7.59 | pKi | 26 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 567-570 [PMID:11229773] |
| GtoPdb | - | - | 7.49 | pIC50 | 32 | nM | IC50 | J Med Chem (2022) 65: 8493-8510 [PMID:35687819] |
| ChEMBL | Inhibition of recombinant human MMP3 using MOCAc-Lys-Pro-Leu-Gly-Leu-A2pr(Dnp)-Ala-Arg-N2 as substrate preincubated for 15 mins followed by substrate addition by fluroscence based assay | B | 7.49 | pIC50 | 32 | nM | IC50 | J Med Chem (2022) 65: 8493-8510 [PMID:35687819] |
| ChEMBL | Inhibition of human recombinant matrix metalloprotease-3 (Stromelysin) at 100 uM | B | 7.55 | pIC50 | 28 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 1637-1642 |
| ChEMBL | Inhibition of human recombinant MMP3 catalytic domain by spectrofluorimeter | B | 7.59 | pIC50 | 26 | nM | IC50 | Bioorg Med Chem (2008) 16: 8745-8759 [PMID:18782669] |
| ChEMBL | Inhibition of human MMP-3 by fluorometric assay | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2020) 63: 14805-14820 [PMID:33210531] |
| ChEMBL | Inhibition of MMP3 | B | 8.12 | pIC50 | 7.62 | nM | IC50 | J Med Chem (2011) 54: 4350-4364 [PMID:21548582] |
| ChEMBL | Inhibition of MMP3 catalytic domain | B | 8.15 | pIC50 | 7 | nM | IC50 | J Biol Chem (2007) 282: 27781-27791 [PMID:17623656] |
| ChEMBL | Activity against Matrix metalloprotease-3 (MMP-3). | B | 8.72 | pIC50 | 1.9 | nM | IC50 | J Med Chem (1998) 41: 1209-1217 [PMID:9548812] |
| ChEMBL | Inhibition of MMP3 | B | 8.72 | pIC50 | 1.9 | nM | IC50 | Bioorg Med Chem (2007) 15: 4753-4766 [PMID:17512742] |
| ChEMBL | Inhibition of MMP-3 (unknown origin) | B | 8.72 | pIC50 | 1.9 | nM | IC50 | J Med Chem (2022) 65: 10709-10754 [PMID:35969157] |
| ChEMBL | Inhibition of human matrix metalloprotease-3 | B | 9.72 | pIC50 | 0.19 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2843-2846 [PMID:14611841] |
| MMP7/Matrix metalloproteinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4073] [GtoPdb: 1631] [UniProtKB: P09237] | ||||||||
| ChEMBL | Inhibition of MMP7 | B | 7.48 | pIC50 | 33 | nM | IC50 | J Biol Chem (2007) 282: 27781-27791 [PMID:17623656] |
| GtoPdb | - | - | 8.29 | pIC50 | 5.1 | nM | IC50 | J Med Chem (2022) 65: 8493-8510 [PMID:35687819] |
| ChEMBL | Inhibition of recombinant human MMP7 using MOCAc-Pro-Leu-Gly-Leu-A2pr(Dnp)-Ala-Arg-NH2 as substrate preincubated for 15 mins followed by substrate addition by fluroscence based assay | B | 8.29 | pIC50 | 5.1 | nM | IC50 | J Med Chem (2022) 65: 8493-8510 [PMID:35687819] |
| MMP8/Matrix metalloproteinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4588] [GtoPdb: 1632] [UniProtKB: P22894] | ||||||||
| ChEMBL | Inhibition of human Matrix metalloprotease-8 | B | 9 | pKi | <1 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 349-352 |
| ChEMBL | The compound was tested for its binding affinity towards neutrophil collagenase (Matrix metalloprotease-8) | B | 9.74 | pKi | 0.18 | nM | Ki | J Med Chem (1998) 41: 199-223 [PMID:9457244] |
| ChEMBL | Inhibition of MMP-8 (unknown origin) | B | 9.74 | pKi | 0.18 | nM | Ki | J Med Chem (2022) 65: 10709-10754 [PMID:35969157] |
| ChEMBL | Inhibition of MMP8 catalytic domain | B | 8.01 | pIC50 | 9.7 | nM | IC50 | J Biol Chem (2007) 282: 27781-27791 [PMID:17623656] |
| ChEMBL | Inhibition of recombinant human MMP8 using MOCAc-Pro-Leu-Gly-Leu-A2pr(Dnp)-Ala-Arg-NH2 as substrate preincubated for 15 mins followed by substrate addition by fluroscence based assay | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2022) 65: 8493-8510 [PMID:35687819] |
| GtoPdb | - | - | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2022) 65: 8493-8510 [PMID:35687819] |
| MMP9/Matrix metalloproteinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL321] [GtoPdb: 1633] [UniProtKB: P14780] | ||||||||
| ChEMBL | Inhibition of human Matrix metalloprotease-9 | B | 9.16 | pKi | 0.69 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 349-352 |
| ChEMBL | The compound was tested for its binding affinity towards 92 kDa gelatinase (Matrix metalloprotease-9) | B | 9.24 | pKi | 0.57 | nM | Ki | J Med Chem (1998) 41: 199-223 [PMID:9457244] |
| ChEMBL | Inhibition of MMP-9 (unknown origin) assessed as inhibition constant | B | 9.24 | pKi | 0.57 | nM | Ki | Eur J Med Chem (2020) 194: 112260-112260 [PMID:32224379] |
| ChEMBL | Inhibition of MMP-9 (unknown origin) | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (2022) 65: 10709-10754 [PMID:35969157] |
| GtoPdb | - | - | 7.82 | pIC50 | 15 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 47-50 [PMID:14684295] |
| ChEMBL | Inhibition of matrix metalloprotease-9 (MMP-9) | B | 7.82 | pIC50 | 15 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 47-50 [PMID:14684295] |
| ChEMBL | Inhibitory activity against MMP9 | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2006) 49: 456-458 [PMID:16420030] |
| ChEMBL | Inhibition of MMP9 | B | 8.17 | pIC50 | 6.7 | nM | IC50 | J Biol Chem (2007) 282: 27781-27791 [PMID:17623656] |
| ChEMBL | Inhibition of recombinant human MMP9 using MOCAc-Pro-Leu-Gly-Leu-A2pr(Dnp)-Ala-Arg-NH2 as substrate preincubated for 15 mins followed by substrate addition by fluroscence based assay | B | 9.01 | pIC50 | 0.98 | nM | IC50 | J Med Chem (2022) 65: 8493-8510 [PMID:35687819] |
| GtoPdb | - | - | 9.03 | pIC50 | 0.93 | nM | IC50 | J Med Chem (2022) 65: 8493-8510 [PMID:35687819] |
| ChEMBL | Inhibition of human recombinant pro-MMP9 by spectrofluorimeter | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Bioorg Med Chem (2008) 16: 8745-8759 [PMID:18782669] |
| ChEMBL | Inhibition of human recombinant MMP9 using Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 as substrate preincubated for 60 mins followed by substrate addition by fluorimetric analysis | B | 9.26 | pIC50 | 0.55 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 2174-2178 [PMID:27038494] |
| ChEMBL | Inhibition of MMP9 | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Bioorg Med Chem (2007) 15: 4753-4766 [PMID:17512742] |
| ChEMBL | Inhibition of MMP-9 (unknown origin) | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2022) 65: 10709-10754 [PMID:35969157] |
| ChEMBL | Activity against Matrix metalloprotease-9 (MMP-9). | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (1998) 41: 1209-1217 [PMID:9548812] |
| ChEMBL | Inhibition of human recombinant 92 kDa gelatinase MMP-9 at 100 uM | B | 9.7 | pIC50 | 0.2 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 1637-1642 |
| ChEMBL | Inhibition of human MMP-9 by fluorometric assay | B | 9.75 | pIC50 | 0.18 | nM | IC50 | J Med Chem (2020) 63: 14805-14820 [PMID:33210531] |
| ChEMBL | Inhibition of MMP9 | B | 10.3 | pIC50 | 0.05 | nM | IC50 | J Med Chem (2011) 54: 4350-4364 [PMID:21548582] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
