batimastat [Ligand Id: 5145] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL279786 (Batimastat, BB-94) |
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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 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]
