batimastat [Ligand Id: 5145] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL279786 (Batimastat, BB-94)
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  • Fc fragment of IgE receptor II/Immunoglobulin epsilon Fc receptor in Human [ChEMBL: CHEMBL2940] [GtoPdb: 2935] [UniProtKB: P06734]
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  • MMP1/Matrix metalloproteinase-1 in Human [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956]
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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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  • MMP2/Matrix metalloproteinase-2 in Human [ChEMBL: CHEMBL333] [GtoPdb: 1629] [UniProtKB: P08253]
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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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  • Snake venom metalloproteinase Bap1 in Bothrops asper [ChEMBL: CHEMBL2079851] [UniProtKB: P83512]
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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 Inhibition of Tumor necrosis factor alpha converting enzyme (TACE) B 7.83 pIC50 14.9 nM IC50 J Med Chem (2003) 46: 3514-3525 [PMID:12877590]
ChEMBL Inhibition of TACE (unknown origin) using fluorogenic LAQAVRSSSR peptide as a substrate by fluorometric assay B 9.4 pIC50 0.4 nM IC50 Med Chem Res (2011) 20: 760-768
Fc fragment of IgE receptor II/Immunoglobulin epsilon Fc receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2940] [GtoPdb: 2935] [UniProtKB: P06734]
ChEMBL Tested for inhibition against CD23 (IgE receptor) proteolysis in membranes derived from RPM18866 cells ( a human B-cell line) B 7 pIC50 100 nM IC50 Bioorg Med Chem Lett (1998) 8: 23-28 [PMID:9871622]
ChEMBL Inhibition against CD23 (IgE receptor) proteolysis in membranes derived from RPM18866 cells B 7 pIC50 100 nM IC50 Bioorg Med Chem Lett (1998) 8: 29-34 [PMID:9871623]
MMP1/Matrix metalloproteinase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956]
GtoPdb - - 9.3 pKi 0.5 nM Ki Bioorg Med Chem Lett (1995) 5: 1415-1420
ChEMBL Inhibition of human fibroblast collagenase, matrix metalloprotease-1 B 9.3 pKi 0.5 nM Ki Bioorg Med Chem Lett (1995) 5: 1415-1420
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 towards human recombinant fibroblast collagenase B 8.3 pIC50 5 nM IC50 Bioorg Med Chem Lett (1998) 8: 23-28 [PMID:9871622]
ChEMBL Inhibitory activity towards human recombinant fibroblast collagenase B 8.59 pIC50 2.6 nM IC50 Bioorg Med Chem Lett (1998) 8: 29-34 [PMID:9871623]
ChEMBL In vitro inhibitory activity against matrix metalloprotease 1 isolated from the culture medium of human skin fibroblasts induced with PMA B 8.92 pIC50 1.2 nM IC50 Bioorg Med Chem Lett (1998) 8: 3251-3256 [PMID:9873712]
GtoPdb - - 9 pIC50 0.99 nM IC50 J Med Chem (2003) 46: 3514-25 [PMID:12877590]
ChEMBL Inhibition of human Matrix metalloprotease-1 (MMP-1) B 9 pIC50 0.99 nM IC50 J Med Chem (2003) 46: 3514-3525 [PMID:12877590]
ChEMBL Inhibition of Matrix metalloprotease-1 B 9.12 pIC50 0.75 nM IC50 Bioorg Med Chem Lett (2001) 11: 567-570 [PMID:11229773]
ChEMBL Activity against Matrix metalloprotease-1 (MMP-1). B 9.4 pIC50 0.4 nM IC50 J Med Chem (1998) 41: 1209-1217 [PMID:9548812]
MMP13/Matrix metalloproteinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL280] [GtoPdb: 1637] [UniProtKB: P45452]
GtoPdb - - 8.3 pIC50 5 nM IC50 J Med Chem (2003) 46: 3514-25 [PMID:12877590]
ChEMBL Inhibition of Matrix metalloprotease-13 B 8.3 pIC50 5 nM IC50 J Med Chem (2003) 46: 3514-3525 [PMID:12877590]
MMP14/Matrix metalloproteinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3869] [GtoPdb: 1638] [UniProtKB: P50281]
ChEMBL Inhibition of human matrix metalloprotease-14 expressed in Escherichia coli B 7.33 pIC50 47 nM IC50 Bioorg Med Chem Lett (2005) 15: 181-183 [PMID:15582436]
ChEMBL Inhibition of Matrix metalloprotease-14 B 8.34 pIC50 4.6 nM IC50 J Med Chem (2003) 46: 3514-3525 [PMID:12877590]
ChEMBL Activity against deletion mutant of MT1-MMP lacking the transmembrane domain (deltaMT1) B 8.52 pIC50 3 nM IC50 J Med Chem (1998) 41: 1209-1217 [PMID:9548812]
ChEMBL Inhibition of Matrix metalloprotease-14 B 8.54 pIC50 2.9 nM IC50 Bioorg Med Chem Lett (2001) 11: 567-570 [PMID:11229773]
MMP2/Matrix metalloproteinase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL333] [GtoPdb: 1629] [UniProtKB: P08253]
ChEMBL Inhibition of human matrix metalloprotease-2 expressed in Sf9 insect cells B 7.89 pIC50 13 nM IC50 Bioorg Med Chem Lett (2005) 15: 181-183 [PMID:15582436]
ChEMBL Compound concentration for 50% inhibition of human recombinant gelatinase A (MMP-2). B 8.4 pIC50 4 nM IC50 Bioorg Med Chem Lett (1997) 7: 193-198
ChEMBL In vitro inhibitory activity against matrix metalloprotease 2 isolated from human HT1080 fibrosarcoma cells induced with TNF B 8.68 pIC50 2.1 nM IC50 Bioorg Med Chem Lett (1998) 8: 3251-3256 [PMID:9873712]
ChEMBL Activity against Matrix metalloprotease-2 (MMP-2). B 9 pIC50 1 nM IC50 J Med Chem (1998) 41: 1209-1217 [PMID:9548812]
ChEMBL Inhibition of human matrix metalloprotease-2 (MMP-2) B 9.14 pIC50 0.73 nM IC50 J Med Chem (2003) 46: 3514-3525 [PMID:12877590]
ChEMBL Ability to inhibit the matrix metalloprotease-2 by method of Knight et al using the fluorogenic peptide substrate. B 9.3 pIC50 0.5 nM IC50 Bioorg Med Chem Lett (2001) 11: 567-570 [PMID:11229773]
MMP3/Matrix metalloproteinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL283] [GtoPdb: 1630] [UniProtKB: P08254]
ChEMBL 50% inhibition of human recombinant stromelysin (MMP-3, HFS) B 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (1997) 7: 193-198
ChEMBL In vitro inhibitory activity against human recombinant matrix metalloprotease 3 B 9.12 pIC50 0.75 nM IC50 Bioorg Med Chem Lett (1998) 8: 3251-3256 [PMID:9873712]
ChEMBL Ability to inhibit the matrix metalloprotease-3 by method of Knight et al using the fluorogenic peptide substrate. B 9.14 pIC50 0.73 nM IC50 Bioorg Med Chem Lett (2001) 11: 567-570 [PMID:11229773]
ChEMBL Activity against Matrix metalloprotease-3 (MMP-3). B 9.19 pIC50 0.65 nM IC50 J Med Chem (1998) 41: 1209-1217 [PMID:9548812]
GtoPdb - - 9.19 pIC50 0.65 nM IC50 J Med Chem (1998) 41: 1209-17 [PMID:9548812]
ChEMBL Inhibition of human matrix metalloprotease-3 (MMP-3) B 9.25 pIC50 0.56 nM IC50 J Med Chem (2003) 46: 3514-3525 [PMID:12877590]
MMP7/Matrix metalloproteinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4073] [GtoPdb: 1631] [UniProtKB: P09237]
ChEMBL 50% inhibition of human recombinant Matrilysin B 8.22 pIC50 6 nM IC50 Bioorg Med Chem Lett (1997) 7: 193-198
ChEMBL In vitro inhibitory activity against human recombinant matrix metalloprotease 7 B 8.62 pIC50 2.4 nM IC50 Bioorg Med Chem Lett (1998) 8: 3251-3256 [PMID:9873712]
MMP9/Matrix metalloproteinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL321] [GtoPdb: 1633] [UniProtKB: P14780]
ChEMBL Inhibition of human matrix metalloprotease-9 expressed in Sf9 insect cells B 7.6 pIC50 25 nM IC50 Bioorg Med Chem Lett (2005) 15: 181-183 [PMID:15582436]
ChEMBL Inhibition of Matrix metalloprotease-9 B 9.17 pIC50 0.67 nM IC50 Bioorg Med Chem Lett (2001) 11: 567-570 [PMID:11229773]
ChEMBL Inhibition of human matrix metalloprotease-9 (MMP-9) B 9.22 pIC50 0.6 nM IC50 J Med Chem (2003) 46: 3514-3525 [PMID:12877590]
ChEMBL Activity against Matrix metalloprotease-9 (MMP-9). B 9.7 pIC50 0.2 nM IC50 J Med Chem (1998) 41: 1209-1217 [PMID:9548812]
Snake venom metalloproteinase Bap1 in Bothrops asper (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2079851] [UniProtKB: P83512]
ChEMBL Inhibition of snake venom BaP1 using Abz-Ala-Gly-Leu-Ala-Nba as substrate incubated for 30 mins prior to substrate addition by fluorescence spectrophotometry B 5.92 pIC50 1200 nM IC50 ACS Med Chem Lett (2012) 3: 540-543 [PMID:24900507]

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]