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 | Inhibition of HFC MMP-1 | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2887-2892 [PMID:10522712] |
| 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 | 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 | 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] |
| 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] |
| 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] |
| MMP13/Matrix metalloproteinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL280] [GtoPdb: 1637] [UniProtKB: P45452] | ||||||||
| 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 | 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 Matrix metalloprotease-13 | B | 8.47 | pIC50 | 3.4 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 295-299 [PMID:11212095] |
| 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 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] |
| 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] |
| 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] |
| GtoPdb | - | - | 8.22 | pIC50 | 6 | nM | IC50 | Pharmacol Ther (1997) 75: 69-75 [PMID:9364582] |
| 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 | 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 | 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 | Inhibition of Matrix metalloprotease-2 | B | 8.74 | pIC50 | 1.8 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 295-299 [PMID:11212095] |
| 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 | 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 | 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 Strom-1 MMP-3 | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2887-2892 [PMID:10522712] |
| 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 | 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 |
| 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 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] |
| 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 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 (matrix metalloprotease-8) | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1999) 42: 4890-4908 [PMID:10579851] |
| 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] |
| 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 | 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 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 | 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 | 8.8 | pIC50 | 1.6 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 295-299 [PMID:11212095] |
| 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 | 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
