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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  • MMP1/Matrix metalloproteinase-1 in Human [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956]
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  • MMP10/Matrix metalloproteinase 10 in Human [ChEMBL: CHEMBL4270] [GtoPdb: 1634] [UniProtKB: P09238]
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  • MMP12/Matrix metalloproteinase 12 in Human [ChEMBL: CHEMBL4393] [GtoPdb: 1636] [UniProtKB: P39900]
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  • MMP13/Matrix metalloproteinase 13 in Human [ChEMBL: CHEMBL280] [GtoPdb: 1637] [UniProtKB: P45452]
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  • MMP14/Matrix metalloproteinase 14 in Human [ChEMBL: CHEMBL3869] [GtoPdb: 1638] [UniProtKB: P50281]
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  • MMP15/Matrix metalloproteinase 15 in Human [ChEMBL: CHEMBL2963] [GtoPdb: 1639] [UniProtKB: P51511]
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  • MMP16/Matrix metalloproteinase 16 in Human [ChEMBL: CHEMBL2200] [GtoPdb: 1640] [UniProtKB: P51512]
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  • MMP2/Matrix metalloproteinase-2 in Human [ChEMBL: CHEMBL333] [GtoPdb: 1629] [UniProtKB: P08253]
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  • MMP24/Matrix metalloproteinase-24 in Human [ChEMBL: CHEMBL5050] [GtoPdb: 1646] [UniProtKB: Q9Y5R2]
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  • MMP26/Matrix metalloproteinase 26 in Human [ChEMBL: CHEMBL4707] [GtoPdb: 1648] [UniProtKB: Q9NRE1]
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  • MMP3/Matrix metalloproteinase 3 in Human [ChEMBL: CHEMBL283] [GtoPdb: 1630] [UniProtKB: P08254]
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  • MMP9/Matrix metalloproteinase 9 in Human [ChEMBL: CHEMBL321] [GtoPdb: 1633] [UniProtKB: P14780]
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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 32:

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]