marimastat [Ligand Id: 5220] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL279785 (BB 2516, BB-2516, GI 5712, GI-5712, KB-R 8898, Marimastat, NSC-719333, TA 2516, TA-2516) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ADAM17 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3706] [GtoPdb: 1662] [UniProtKB: P78536] | ||||||||
| ChEMBL | Inhibitory potency against Tumor necrosis factor alpha converting enzyme (TACE) | B | 8.2 | pKi | 6.3 | nM | Ki | J Med Chem (2002) 45: 2289-2293 [PMID:12014967] |
| ChEMBL | Inhibition of recombinant human TNF-alpha converting enzyme (TACE) | B | 9.4 | pKi | 0.4 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 2737-2740 [PMID:12873504] |
| ChEMBL | Inhibition of recombinant human tumor necrosis factor-alpha converting enzyme | B | 9.4 | pKi | 0.4 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 2741-2744 [PMID:12873505] |
| ChEMBL | Inhibition of TACE (unknown origin) using Mca-Pro-Leu-Ala-Gln-Ala-Val-Dpa-Arg-Ser-Ser-Ser-Arg-NH2 as substrate | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2016) 59: 313-327 [PMID:26653735] |
| ChEMBL | Inhibition of TNF(tumor necrosis factor) in human blood | F | 5.15 | pIC50 | 7000 | nM | IC50 | J Med Chem (1999) 42: 4890-4908 [PMID:10579851] |
| ChEMBL | Inhibition of LPS-stimulated TNF-alpha release in human whole blood | F | 5.39 | pIC50 | 4100 | nM | IC50 | J Med Chem (2001) 44: 2636-2660 [PMID:11472217] |
| ChEMBL | Inhibitory activity against Tumor necrosis factor alpha-converting enzyme (TACE) in blood. | B | 8.42 | pIC50 | 3.8 | nM | IC50 | J Med Chem (1999) 42: 4890-4908 [PMID:10579851] |
| ChEMBL | Inhibition of TACE | B | 8.42 | pIC50 | 3.8 | nM | IC50 | Bioorg Med Chem (2009) 17: 444-459 [PMID:19095454] |
| ADAMTS4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2318] [GtoPdb: 1677] [UniProtKB: O75173] | ||||||||
| ChEMBL | Inhibition of full length recombinant ADAMTS4 (unknown origin) expressed in insect Sf9 cells after 6 hrs by alkaline phosphatase-based assay | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2016) 59: 313-327 [PMID:26653735] |
| ADAMTS5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2285] [GtoPdb: 1678] [UniProtKB: Q9UNA0] | ||||||||
| ChEMBL | Inhibition of full length recombinant ADAMTS5 (unknown origin) expressed in insect Sf9 cells after 6 hrs by alkaline phosphatase-based assay | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2016) 59: 313-327 [PMID:26653735] |
| MMP1/Matrix metalloproteinase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956] | ||||||||
| ChEMBL | Inhibition of recombinant human matrix metalloprotease-1 | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 2737-2740 [PMID:12873504] |
| ChEMBL | Inhibition of Recombinant human matrix metalloprotease-1 | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 2741-2744 [PMID:12873505] |
| ChEMBL | In vitro inhibition of human MMP-1. | B | 9 | pKi | <1 | nM | Ki | J Med Chem (2001) 44: 2636-2660 [PMID:11472217] |
| ChEMBL | Inhibitory potency against Matrix metalloprotease-1 (MMP-1) | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (2002) 45: 2289-2293 [PMID:12014967] |
| ChEMBL | Inhibition of full length human recombinant MMP1 using MCA-Arg-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-Glu-Arg-NH2 as substrate preincubated for 60 mins followed by substrate addition by fluorescence assay | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2016) 59: 313-327 [PMID:26653735] |
| GtoPdb | - | - | 8.3 | pIC50 | 5 | nM | IC50 | Pharmacol Ther (1997) 75: 69-75 [PMID:9364582] |
| ChEMBL | Inhibitory activity against MMP-1 (Matrix metalloprotease-1) | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1999) 42: 4890-4908 [PMID:10579851] |
| ChEMBL | 50% inhibition of human recombinant fibroblast collagenase (MMP-1, HFC) | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 193-198 |
| ChEMBL | Inhibition of HFC MMP-1 | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2887-2892 [PMID:10522712] |
| ChEMBL | Inhibition of MMP-1 (unknown origin) | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2022) 65: 10709-10754 [PMID:35969157] |
| ChEMBL | Inhibitory activity against human Matrix metalloprotease-1 | B | 8.54 | pIC50 | 2.9 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2723-2725 [PMID:11591510] |
| ChEMBL | 50 percent inhibition of human Matrix metalloprotease-1 by the cleavage of fluorogenic peptide MCA-Pro-Leu-Gly-Leu-Dpa-ala-Arg-NH2 | B | 8.54 | pIC50 | 2.9 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2815-2817 [PMID:11133099] |
| ChEMBL | Activity against Matrix metalloprotease-1 (MMP-1). | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1998) 41: 1209-1217 [PMID:9548812] |
| ChEMBL | Inhibition of matrix metalloprotease-1 | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1691-1696 [PMID:10397503] |
| ChEMBL | Inhibition of Matrix metalloprotease-1 | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 295-299 [PMID:11212095] |
| ChEMBL | Inhibitory activity against matrix metalloprotease-1 (MMP1) | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2003) 46: 3840-3852 [PMID:12930146] |
| ChEMBL | In vitro inhibitory activity against matrix metalloprotease 1 isolated from the culture medium of human skin fibroblasts induced with PMA | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 3251-3256 [PMID:9873712] |
| ChEMBL | Inhibition of human recombinant MMP-1 incubated for 30 mins by fluorescence based analysis | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2023) 66: 6682-6696 [PMID:37158732] |
| ChEMBL | In vitro selective inhibition against matrix metalloprotease-1 (MMP-1) using a fluorimetric assay | B | 9.11 | pIC50 | 0.78 | nM | IC50 | J Med Chem (2002) 45: 219-232 [PMID:11754593] |
| ChEMBL | Inhibition of MMP-1 (unknown origin) | B | 9.11 | pIC50 | 0.78 | nM | IC50 | Eur J Med Chem (2021) 223: 113623-113623 [PMID:34157437] |
| MMP10/Matrix metalloproteinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4270] [GtoPdb: 1634] [UniProtKB: P09238] | ||||||||
| ChEMBL | Inhibition of recombinant human MMP10 catalytic domain using MCA-Arg-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-Glu-Arg-NH2 as substrate preincubated for 60 mins followed by substrate addition by fluorescence assay | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2016) 59: 313-327 [PMID:26653735] |
| GtoPdb | - | - | 7.16 | pIC50 | 69 | nM | IC50 | J Med Chem (2023) 66: 6682-6696 [PMID:37158732] |
| ChEMBL | Inhibition of human recombinant MMP-10 using Mca-Aug-Pro-Lys-Pro-Val-Glu-Nval-Trp-Arg-Lys(Dnp)-NH2 as substrate preincubated for 30 mins followed by substrate addition by fluorescence based analysis | B | 7.16 | pIC50 | 69 | nM | IC50 | J Med Chem (2023) 66: 6682-6696 [PMID:37158732] |
| MMP12/Matrix metalloproteinase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4393] [GtoPdb: 1636] [UniProtKB: P39900] | ||||||||
| ChEMBL | Inhibition of MMP12 (unknown origin) catalytic domain using MCA-Arg-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-Glu-Arg-NH2 as substrate preincubated for 60 mins followed by substrate addition by fluorescence assay | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2016) 59: 313-327 [PMID:26653735] |
| ChEMBL | Inhibition of MMP-12 (unknown origin) | B | 8.3 | pIC50 | <5 | nM | IC50 | J Med Chem (2022) 65: 10709-10754 [PMID:35969157] |
| MMP13/Matrix metalloproteinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL280] [GtoPdb: 1637] [UniProtKB: P45452] | ||||||||
| ChEMBL | Inhibition of MMP13 in human U2OS cells by peptide microarray-based fluorescence assay | B | 6.89 | pIC50 | 128 | nM | IC50 | J Nat Prod (2022) 85: 2424-2432 [PMID:36122348] |
| ChEMBL | Inhibition of matrix metalloprotease-13 | B | 8.46 | pIC50 | 3.5 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1691-1696 [PMID:10397503] |
| ChEMBL | Inhibition of Matrix metalloprotease-13 | B | 8.47 | pIC50 | 3.4 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 295-299 [PMID:11212095] |
| ChEMBL | Inhibitory activity against matrix metalloprotease-13 (MMP13) | B | 8.47 | pIC50 | 3.4 | nM | IC50 | J Med Chem (2003) 46: 3840-3852 [PMID:12930146] |
| ChEMBL | Inhibition of human recombinant MMP-13 using Mca-Lys-Pro-Leu-GlyLeu-Dpa-Ala-Arg-NH2 as substrate preincubated for 30 mins followed by substrate addition by fluorescence based analysis | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2023) 66: 6682-6696 [PMID:37158732] |
| ChEMBL | 50 percent inhibition of human Matrix metalloprotease-13 by the cleavage of fluorogenic peptide MCA-Pro-Leu-Gly-Leu-Dpa-ala-Arg-NH2 | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2815-2817 [PMID:11133099] |
| ChEMBL | Inhibitory activity against human Matrix metalloprotease-13 | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2723-2725 [PMID:11591510] |
| ChEMBL | Inhibition of Coll-3 MMP-13 | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2887-2892 [PMID:10522712] |
| GtoPdb | - | - | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2023) 66: 6682-6696 [PMID:37158732] |
| ChEMBL | Inhibition of MMP-13 (unknown origin) | B | 8.92 | pIC50 | 1.2 | nM | IC50 | Eur J Med Chem (2021) 223: 113623-113623 [PMID:34157437] |
| ChEMBL | Inhibition of Matrix metalloprotease-13 (MMP-13) in fluorimetric assay | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2002) 45: 219-232 [PMID:11754593] |
| ChEMBL | Inhibition of MMP-13 (unknown origin) | B | 9.13 | pIC50 | 0.74 | nM | IC50 | J Med Chem (2022) 65: 10709-10754 [PMID:35969157] |
| MMP14/Matrix metalloproteinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3869] [GtoPdb: 1638] [UniProtKB: P50281] | ||||||||
| ChEMBL | Inhibition of MMP14 (unknown origin) catalytic domain using MCA-Arg-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-Glu-Arg-NH2 as substrate preincubated for 60 mins followed by substrate addition by fluorescence assay | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2016) 59: 313-327 [PMID:26653735] |
| ChEMBL | Activity against deletion mutant of MT1-MMP lacking the transmembrane domain (deltaMT1) | B | 8.74 | pIC50 | 1.82 | nM | IC50 | J Med Chem (1998) 41: 1209-1217 [PMID:9548812] |
| ChEMBL | Inhibition of MMP-14 (unknown origin) | B | 8.74 | pIC50 | 1.8 | nM | IC50 | J Med Chem (2022) 65: 10709-10754 [PMID:35969157] |
| MMP15/Matrix metalloproteinase 15 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2963] [GtoPdb: 1639] [UniProtKB: P51511] | ||||||||
| ChEMBL | Inhibition of MMP15 (unknown origin) catalytic domain using MCA-Arg-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-Glu-Arg-NH2 as substrate preincubated for 60 mins followed by substrate addition by fluorescence assay | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2016) 59: 313-327 [PMID:26653735] |
| MMP16/Matrix metalloproteinase 16 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2200] [GtoPdb: 1640] [UniProtKB: P51512] | ||||||||
| ChEMBL | Inhibition of MMP16 (unknown origin) catalytic domain using MCA-Arg-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-Glu-Arg-NH2 as substrate preincubated for 60 mins followed by substrate addition by fluorescence assay | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2016) 59: 313-327 [PMID:26653735] |
| MMP2/Matrix metalloproteinase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL333] [GtoPdb: 1629] [UniProtKB: P08253] | ||||||||
| ChEMBL | Inhibitory potency against Matrix metalloprotease-2 (MMP-2) | B | 9.22 | pKi | 0.6 | nM | Ki | J Med Chem (2002) 45: 2289-2293 [PMID:12014967] |
| ChEMBL | Inhibition of full length human recombinant MMP2 using MCA-Arg-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-Glu-Arg-NH2 as substrate preincubated for 60 mins followed by substrate addition by fluorescence assay | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2016) 59: 313-327 [PMID:26653735] |
| ChEMBL | Inhibition of MMP2 in human U2OS cells by peptide microarray-based fluorescence assay | B | 8.1 | pIC50 | 8 | nM | IC50 | J Nat Prod (2022) 85: 2424-2432 [PMID:36122348] |
| GtoPdb | - | - | 8.22 | pIC50 | 6 | nM | IC50 | Pharmacol Ther (1997) 75: 69-75 [PMID:9364582] |
| ChEMBL | Inhibition of MMP-2 (unknown origin) | B | 8.22 | pIC50 | 6 | nM | IC50 | Eur J Med Chem (2020) 194: 112260-112260 [PMID:32224379] |
| ChEMBL | Compound concentration for 50% inhibition of human recombinant gelatinase A (MMP-2). | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 193-198 |
| ChEMBL | Inhibition of Gel-A MMP-2 | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2887-2892 [PMID:10522712] |
| ChEMBL | Inhibition of MMP-2 (unknown origin) | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2022) 65: 10709-10754 [PMID:35969157] |
| ChEMBL | Inhibition of human recombinant MMP-2 incubated for 30 mins by fluorescence based analysis | B | 8.25 | pIC50 | 5.6 | nM | IC50 | J Med Chem (2023) 66: 6682-6696 [PMID:37158732] |
| ChEMBL | Activity against Matrix metalloprotease-2 (MMP-2). | B | 8.29 | pIC50 | 5.1 | nM | IC50 | J Med Chem (1998) 41: 1209-1217 [PMID:9548812] |
| ChEMBL | Inhibition of matrix metalloprotease-2 | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1691-1696 [PMID:10397503] |
| ChEMBL | Inhibition of Matrix metalloprotease-2 | B | 8.74 | pIC50 | 1.8 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 295-299 [PMID:11212095] |
| ChEMBL | Inhibitory activity against matrix metalloprotease-2 (MMP2) | B | 8.74 | pIC50 | 1.8 | nM | IC50 | J Med Chem (2003) 46: 3840-3852 [PMID:12930146] |
| ChEMBL | In vitro inhibitory activity against matrix metalloprotease 2 isolated from human HT1080 fibrosarcoma cells induced with TNF | B | 9.07 | pIC50 | 0.85 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 3251-3256 [PMID:9873712] |
| ChEMBL | Inhibitory activity against human Matrix metalloprotease-2 | B | 9.12 | pIC50 | 0.75 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2723-2725 [PMID:11591510] |
| ChEMBL | 50 percent inhibition of human Matrix metalloprotease-2 by the cleavage of fluorogenic peptide MCA-Pro-Leu-Gly-Leu-Dpa-ala-Arg-NH2 | B | 9.12 | pIC50 | 0.75 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2815-2817 [PMID:11133099] |
| ChEMBL | Inhibition of MMP2 (unknown origin) preincubated for 1 hr followed by (QF)-24 substrate addition measured at 1 min time interval for 1 hr by fluorescence assay | B | 9.37 | pIC50 | 0.43 | nM | IC50 | J Med Chem (2019) 62: 622-640 [PMID:30537832] |
| ChEMBL | Inhibition of MMP2 (unknown origin) using QF-24 as substrate preincubated for 1 hr followed by substrate addition and measured at 1 min interval for 1 hr by fluorescence assay | B | 9.37 | pIC50 | 0.43 | nM | IC50 | J Med Chem (2019) 62: 7185-7209 [PMID:31251594] |
| ChEMBL | Inhibition of MMP-2 (unknown origin) | B | 9.39 | pIC50 | 0.41 | nM | IC50 | Eur J Med Chem (2021) 223: 113623-113623 [PMID:34157437] |
| ChEMBL | In vitro selective inhibition against matrix metalloprotease-2 (MMP-2) using fluorimetric assay | B | 9.39 | pIC50 | 0.41 | nM | IC50 | J Med Chem (2002) 45: 219-232 [PMID:11754593] |
| MMP20/Matrix metalloproteinase-20 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938226] [GtoPdb: 1643] [UniProtKB: O60882] | ||||||||
| ChEMBL | Inhibition of MMP20 (unknown origin) catalytic domain using MCA-Arg-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-Glu-Arg-NH2 as substrate preincubated for 60 mins followed by substrate addition by fluorescence assay | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2016) 59: 313-327 [PMID:26653735] |
| MMP24/Matrix metalloproteinase-24 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5050] [GtoPdb: 1646] [UniProtKB: Q9Y5R2] | ||||||||
| ChEMBL | Inhibition of MMP24 (unknown origin) catalytic domain using MCA-Arg-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-Glu-Arg-NH2 as substrate preincubated for 60 mins followed by substrate addition by fluorescence assay | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2016) 59: 313-327 [PMID:26653735] |
| MMP25/Matrix metalloproteinase-25 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795103] [GtoPdb: 1647] [UniProtKB: Q9NPA2] | ||||||||
| ChEMBL | Inhibition of MMP25 (unknown origin) catalytic domain using MCA-Arg-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-Glu-Arg-NH2 as substrate preincubated for 60 mins followed by substrate addition by fluorescence assay | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2016) 59: 313-327 [PMID:26653735] |
| MMP26/Matrix metalloproteinase 26 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4707] [GtoPdb: 1648] [UniProtKB: Q9NRE1] | ||||||||
| ChEMBL | Inhibition of full length human recombinant MMP26 using MCA-Arg-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-Glu-Arg-NH2 as substrate preincubated for 60 mins followed by substrate addition by fluorescence assay | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2016) 59: 313-327 [PMID:26653735] |
| MMP3/Matrix metalloproteinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL283] [GtoPdb: 1630] [UniProtKB: P08254] | ||||||||
| ChEMBL | Inhibition of recombinant human matrix metalloprotease-3 | B | 7.08 | pKi | 84 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 2737-2740 [PMID:12873504] |
| ChEMBL | Inhibition of recombinant human matrix metalloprotease-3 | B | 7.08 | pKi | 84 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 2741-2744 [PMID:12873505] |
| ChEMBL | Inhibitory potency against Matrix metalloprotease-3 (MMP-3) | B | 8.05 | pKi | 8.9 | nM | Ki | J Med Chem (2002) 45: 2289-2293 [PMID:12014967] |
| ChEMBL | Inhibition of human MMP-3. | B | 8.62 | pKi | 2.4 | nM | Ki | J Med Chem (2001) 44: 2636-2660 [PMID:11472217] |
| ChEMBL | Inhibition of MMP3 (unknown origin) catalytic domain using Mca-Arg-Pro-Lys-Pro-Val-Glu-Nva-Trp-Arg-Lys(Dnp)-NH2 as substrate preincubated for 60 mins followed by substrate addition by fluorescence assay | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2016) 59: 313-327 [PMID:26653735] |
| GtoPdb | - | - | 6.64 | pIC50 | 230 | nM | IC50 | Pharmacol Ther (1997) 75: 69-75 [PMID:9364582] |
| ChEMBL | Inhibition of MMP-3 (unknown origin) | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2022) 65: 10709-10754 [PMID:35969157] |
| ChEMBL | Inhibition of Strom-1 MMP-3 | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2887-2892 [PMID:10522712] |
| ChEMBL | 50% inhibition of human recombinant stromelysin (MMP-3, HFS) | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 193-198 |
| ChEMBL | Inhibition of MMP3 in human U2OS cells by peptide microarray-based fluorescence assay | B | 7.59 | pIC50 | 26 | nM | IC50 | J Nat Prod (2022) 85: 2424-2432 [PMID:36122348] |
| ChEMBL | Inhibition of matrix metalloprotease-3 | B | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1691-1696 [PMID:10397503] |
| ChEMBL | Inhibitory activity against matrix metalloprotease-3 (MMP3) | B | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (2003) 46: 3840-3852 [PMID:12930146] |
| ChEMBL | Inhibition of Matrix metalloprotease-3 | B | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 295-299 [PMID:11212095] |
| ChEMBL | Inhibition of Matrix metalloprotease-3 (MMP-3) in fluorimetric assay | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2002) 45: 219-232 [PMID:11754593] |
| ChEMBL | Inhibition of MMP-3 (unknown origin) | B | 7.85 | pIC50 | 14 | nM | IC50 | Eur J Med Chem (2021) 223: 113623-113623 [PMID:34157437] |
| ChEMBL | In vitro inhibitory activity against human recombinant matrix metalloprotease 3 | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 3251-3256 [PMID:9873712] |
| ChEMBL | Activity against Matrix metalloprotease-3 (MMP-3). | B | 8.36 | pIC50 | 4.4 | nM | IC50 | J Med Chem (1998) 41: 1209-1217 [PMID:9548812] |
| MMP7/Matrix metalloproteinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4073] [GtoPdb: 1631] [UniProtKB: P09237] | ||||||||
| ChEMBL | Inhibition of MMP7 (unknown origin) catalytic domain using MCA-Arg-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-Glu-Arg-NH2 as substrate preincubated for 60 mins followed by substrate addition by fluorescence assay | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2016) 59: 313-327 [PMID:26653735] |
| ChEMBL | 50% inhibition of human recombinant Matrilysin | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 193-198 |
| ChEMBL | Inhibition of MMP-7 (unknown origin) | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2022) 65: 10709-10754 [PMID:35969157] |
| GtoPdb | - | - | 7.8 | pIC50 | 16 | nM | IC50 | Pharmacol Ther (1997) 75: 69-75 [PMID:9364582] |
| ChEMBL | In vitro inhibitory activity against human recombinant matrix metalloprotease 7 | B | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 3251-3256 [PMID:9873712] |
| ChEMBL | Inhibition of MMP7 in human U2OS cells by peptide microarray-based fluorescence assay | B | 8 | pIC50 | 10 | nM | IC50 | J Nat Prod (2022) 85: 2424-2432 [PMID:36122348] |
| ChEMBL | Inhibition of Matrix metalloprotease-7 (MMP-7) in fluorimetric assay | B | 8.39 | pIC50 | 4.1 | nM | IC50 | J Med Chem (2002) 45: 219-232 [PMID:11754593] |
| ChEMBL | Inhibition of MMP-7 (unknown origin) | B | 8.39 | pIC50 | 4.1 | nM | IC50 | Eur J Med Chem (2021) 223: 113623-113623 [PMID:34157437] |
| MMP8/Matrix metalloproteinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4588] [GtoPdb: 1632] [UniProtKB: P22894] | ||||||||
| ChEMBL | Inhibition of MMP8 (unknown origin) catalytic domain using MCA-Arg-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-Glu-Arg-NH2 as substrate preincubated for 60 mins followed by substrate addition by fluorescence assay | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2016) 59: 313-327 [PMID:26653735] |
| ChEMBL | Inhibition of MMP-8 (matrix metalloprotease-8) | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1999) 42: 4890-4908 [PMID:10579851] |
| ChEMBL | Inhibition of HNC MMP-8 | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2887-2892 [PMID:10522712] |
| ChEMBL | Inhibition of MMP-8 (unknown origin) | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2022) 65: 10709-10754 [PMID:35969157] |
| ChEMBL | Inhibition of human recombinant MMP-8 incubated for 30 mins by fluorescence based analysis | B | 8.89 | pIC50 | 1.3 | nM | IC50 | J Med Chem (2023) 66: 6682-6696 [PMID:37158732] |
| GtoPdb | - | - | 8.89 | pIC50 | 1.3 | nM | IC50 | J Med Chem (2023) 66: 6682-6696 [PMID:37158732] |
| ChEMBL | Inhibition of Matrix metalloprotease-8 (MMP-8) in fluorimetric assay | B | 9.33 | pIC50 | 0.47 | nM | IC50 | J Med Chem (2002) 45: 219-232 [PMID:11754593] |
| ChEMBL | Inhibition of MMP-8 (unknown origin) | B | 9.33 | pIC50 | 0.47 | nM | IC50 | Eur J Med Chem (2021) 223: 113623-113623 [PMID:34157437] |
| MMP9/Matrix metalloproteinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL321] [GtoPdb: 1633] [UniProtKB: P14780] | ||||||||
| ChEMBL | Inhibition of recombinant human matrix metalloprotease-9 | B | 7.96 | pKi | 11 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 2737-2740 [PMID:12873504] |
| ChEMBL | Inhibition of recombinant human matrix metalloprotease-9 (gelatinase B) | B | 7.96 | pKi | 11 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 2741-2744 [PMID:12873505] |
| ChEMBL | In vitro inhibition of human MMP-9. | B | 9 | pKi | <1 | nM | Ki | J Med Chem (2001) 44: 2636-2660 [PMID:11472217] |
| ChEMBL | Inhibition of full length human recombinant MMP9 using MCA-Arg-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-Glu-Arg-NH2 as substrate preincubated for 60 mins followed by substrate addition by fluorescence assay | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2016) 59: 313-327 [PMID:26653735] |
| ChEMBL | Inhibition of MMP9 in human U2OS cells by peptide microarray-based fluorescence assay | B | 6.1 | pIC50 | 795 | nM | IC50 | J Nat Prod (2022) 85: 2424-2432 [PMID:36122348] |
| ChEMBL | Activity against Matrix metalloprotease-9 (MMP-9). | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (1998) 41: 1209-1217 [PMID:9548812] |
| ChEMBL | Inhibition of human recombinant MMP-9 incubated for 30 mins by fluorescence based analysis | B | 8.33 | pIC50 | 4.7 | nM | IC50 | J Med Chem (2023) 66: 6682-6696 [PMID:37158732] |
| ChEMBL | Inhibition of MMP9 (unknown origin) preincubated for 1 hr followed by (QF)-24 substrate addition measured at 1 min time interval for 1 hr by fluorescence assay | B | 8.51 | pIC50 | 3.1 | nM | IC50 | J Med Chem (2019) 62: 622-640 [PMID:30537832] |
| ChEMBL | Inhibition of MMP9 (unknown origin) using QF-24 as substrate preincubated for 1 hr followed by substrate addition and measured at 1 min interval for 1 hr by fluorescence assay | B | 8.51 | pIC50 | 3.1 | nM | IC50 | J Med Chem (2019) 62: 7185-7209 [PMID:31251594] |
| GtoPdb | - | - | 8.52 | pIC50 | 3 | nM | IC50 | Pharmacol Ther (1997) 75: 69-75 [PMID:9364582] |
| ChEMBL | Inhibition of MMP-9 (unknown origin) | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2022) 65: 10709-10754 [PMID:35969157] |
| ChEMBL | Inhibition of MMP-9 (unknown origin) | B | 8.52 | pIC50 | 3 | nM | IC50 | Eur J Med Chem (2020) 194: 112260-112260 [PMID:32224379] |
| ChEMBL | Inhibition of Matrix metalloprotease-9 | B | 8.8 | pIC50 | 1.6 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 295-299 [PMID:11212095] |
| ChEMBL | Inhibitory activity against matrix metalloprotease-9 (MMP9) | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2003) 46: 3840-3852 [PMID:12930146] |
| ChEMBL | Inhibition of matrix metalloprotease-9 | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1691-1696 [PMID:10397503] |
| ChEMBL | Inhibition of MMP-9 (unknown origin) | B | 9.1 | pIC50 | 0.79 | nM | IC50 | Eur J Med Chem (2021) 223: 113623-113623 [PMID:34157437] |
| ChEMBL | In vitro selective inhibition against Matrix metalloprotease-9 (MMP-9) using fluorimetric assay | B | 9.1 | pIC50 | 0.79 | nM | IC50 | J Med Chem (2002) 45: 219-232 [PMID:11754593] |
| Metalloendopeptidase in Teladorsagia circumcincta (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3739251] [UniProtKB: A0A0C5PRQ1] | ||||||||
| ChEMBL | Inhibition of recombinant Teladorsagia circumcincta DPY-31 astacin domain expressed in Escherichia coli using Suc-Ala-Ala-Ala-pNA as substrate preincubated for 3 hrs followed by substrate addition measured after 3 hrs by microplate reader assay | B | 4.1 | pIC50 | 79432.82 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 5752-5755 [PMID:26546217] |
| TNF-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1825] [UniProtKB: P01375] | ||||||||
| ChEMBL | Inhibitory activity against tumor necrosis factor alpha (TNF-alpha) production in LPS-stimulated human PBMCs | F | 6 | pIC50 | 1001 | nM | IC50 | J Med Chem (2002) 45: 2289-2293 [PMID:12014967] |
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]
