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 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 | Inhibitory activity against MMP2 | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2006) 49: 456-458 [PMID:16420030] |
| 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 | Inhibition of MMP-2 (unknown origin) | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2022) 65: 10709-10754 [PMID:35969157] |
| 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 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 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 Matrix metalloprotease-2 | B | 9.4 | pIC50 | 0.4 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1783-1786 [PMID:12729664] |
| 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-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] |