prinomastat [Ligand Id: 6505] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL75094 (AG-3340, AG3340, KB-R-9896, Prinomastat) |
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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 TNF(tumor necrosis factor) in human blood | F | 4.78 | pIC50 | 16600 | nM | IC50 | J Med Chem (1999) 42: 4890-4908 [PMID:10579851] |
| ChEMBL | Inhibition of TACE | B | 7.66 | pIC50 | 22 | nM | IC50 | Bioorg Med Chem (2009) 17: 444-459 [PMID:19095454] |
| ChEMBL | Inhibitory activity against Tumor necrosis factor alpha-converting enzyme (TACE) in blood. | B | 8.26 | pIC50 | 5.5 | nM | IC50 | J Med Chem (1999) 42: 4890-4908 [PMID:10579851] |
| MMP1/Matrix metalloproteinase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956] | ||||||||
| ChEMBL | Inhibition of matrix metalloprotease-1 (MMP-1). | B | 8.09 | pKi | 8.2 | nM | Ki | J Med Chem (2000) 43: 305-341 [PMID:10669559] |
| ChEMBL | Inhibition of collagenase-1 (Matrix metalloprotease-1) | B | 8.09 | pKi | 8.2 | nM | Ki | J Med Chem (1999) 42: 4547-4562 [PMID:10579818] |
| ChEMBL | Inhibition of human matrix metalloprotease-1 | B | 8.09 | pKi | 8.2 | nM | Ki | J Med Chem (2004) 47: 2761-2767 [PMID:15139754] |
| ChEMBL | Inhibition of Matrix metalloprotease-1 | B | 7.32 | pIC50 | 48 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 295-299 [PMID:11212095] |
| ChEMBL | Inhibitory activity against matrix metalloprotease-1 (MMP1) | B | 7.32 | pIC50 | 48 | nM | IC50 | J Med Chem (2003) 46: 3840-3852 [PMID:12930146] |
| 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 | 7.63 | pIC50 | 23.5 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2815-2817 [PMID:11133099] |
| ChEMBL | Inhibition of human matrix metalloprotease-1 | B | 8.09 | pIC50 | 8.2 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1321-1326 [PMID:15713379] |
| ChEMBL | Inhibitory activity against MMP-1 (Matrix metalloprotease-1) | B | 8.09 | pIC50 | 8.2 | nM | IC50 | J Med Chem (1999) 42: 4890-4908 [PMID:10579851] |
| ChEMBL | In vitro selective inhibition against matrix metalloprotease-1 (MMP-1) using a fluorimetric assay | B | 8.24 | pIC50 | 5.7 | nM | IC50 | J Med Chem (2002) 45: 219-232 [PMID:11754593] |
| ChEMBL | In vitro inhibitory activity against truncated collagenase-1 (matrix metalloprotease-1). | B | 8.31 | pIC50 | 4.9 | nM | IC50 | J Med Chem (1999) 42: 4547-4562 [PMID:10579818] |
| MMP13/Matrix metalloproteinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL280] [GtoPdb: 1637] [UniProtKB: P45452] | ||||||||
| ChEMBL | Inhibition of matrix metalloprotease-13 (MMP-13). | B | 10.42 | pKi | 0.04 | nM | Ki | J Med Chem (2000) 43: 305-341 [PMID:10669559] |
| ChEMBL | Inhibition of collagenase (Matrix metalloprotease-13) | B | 10.42 | pKi | 0.04 | nM | Ki | J Med Chem (1999) 42: 4547-4562 [PMID:10579818] |
| ChEMBL | Inhibitory activity against matrix metalloprotease-13 (MMP13) | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2003) 46: 3840-3852 [PMID:12930146] |
| ChEMBL | Inhibition of Matrix metalloprotease-13 | B | 8.82 | pIC50 | 1.5 | 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 | 9.3 | pIC50 | 0.5 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2815-2817 [PMID:11133099] |
| ChEMBL | In vitro inhibitory activity against collagenase-3 (matrix metalloprotease-13). | B | 9.4 | pIC50 | <0.4 | nM | IC50 | J Med Chem (1999) 42: 4547-4562 [PMID:10579818] |
| ChEMBL | Inhibition of Matrix metalloprotease-13 (MMP-13) in fluorimetric assay | B | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2002) 45: 219-232 [PMID:11754593] |
| GtoPdb | - | - | 10.4 | pIC50 | 0.04 | nM | IC50 | Med Chem (2005) 1: 71-104 [PMID:16789888] |
| MMP14/Matrix metalloproteinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3869] [GtoPdb: 1638] [UniProtKB: P50281] | ||||||||
| ChEMBL | Inhibition of human matrix metalloprotease-14 | B | 9.52 | pIC50 | 0.3 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1321-1326 [PMID:15713379] |
| MMP2/Matrix metalloproteinase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL333] [GtoPdb: 1629] [UniProtKB: P08253] | ||||||||
| ChEMBL | Inhibition of matrix metalloprotease-2 (MMP-2). | B | 10.08 | pKi | 0.08 | nM | Ki | J Med Chem (2000) 43: 305-341 [PMID:10669559] |
| ChEMBL | Inhibition of gelatinase-A (Matrix metalloprotease-2) | B | 10.08 | pKi | 0.08 | nM | Ki | J Med Chem (1999) 42: 4547-4562 [PMID:10579818] |
| ChEMBL | Inhibition of human matrix metalloprotease-2 | B | 10.1 | pKi | 0.08 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 2667-2672 [PMID:12217351] |
| ChEMBL | Inhibition of Matrix metalloprotease-2 | B | 10.3 | pKi | 0.05 | nM | Ki | J Med Chem (2004) 47: 325-336 [PMID:14711305] |
| ChEMBL | Inhibition of recombinant human MMP2 using thiopeptide as substrate preincubated for 30 mins followed by substrate addition and measured every mins for 20 min by colorimetric assay | B | 8.74 | pIC50 | 1.8 | nM | IC50 | Eur J Med Chem (2019) 181: 111563-111563 [PMID:31415980] |
| ChEMBL | Inhibitory activity against matrix metalloprotease-2 (MMP2) | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2003) 46: 3840-3852 [PMID:12930146] |
| ChEMBL | Inhibition of Matrix metalloprotease-2 | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 295-299 [PMID:11212095] |
| ChEMBL | In vitro inhibitory activity against gelatinase-A (matrix metalloprotease-2). | B | 9.4 | pIC50 | <0.4 | nM | IC50 | J Med Chem (1999) 42: 4547-4562 [PMID:10579818] |
| 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 | 9.52 | pIC50 | 0.3 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2815-2817 [PMID:11133099] |
| ChEMBL | Inhibition of human matrix metalloprotease-2 | B | 10.05 | pIC50 | 0.09 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1321-1326 [PMID:15713379] |
| ChEMBL | In vitro selective inhibition against matrix metalloprotease-2 (MMP-2) using fluorimetric assay | B | 10.32 | pIC50 | 0.05 | nM | IC50 | J Med Chem (2002) 45: 219-232 [PMID:11754593] |
| MMP3/Matrix metalloproteinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL283] [GtoPdb: 1630] [UniProtKB: P08254] | ||||||||
| ChEMBL | Inhibition of matrix metalloprotease-3 (MMP-3). | B | 9.57 | pKi | 0.27 | nM | Ki | J Med Chem (2000) 43: 305-341 [PMID:10669559] |
| ChEMBL | Inhibition of Matrix metalloprotease-3 | B | 9.57 | pKi | 0.27 | nM | Ki | J Med Chem (1999) 42: 4547-4562 [PMID:10579818] |
| ChEMBL | In vitro inhibitory activity against matrix metalloprotease-3. | B | 8.31 | pIC50 | 4.9 | nM | IC50 | J Med Chem (1999) 42: 4547-4562 [PMID:10579818] |
| ChEMBL | Inhibition of Matrix metalloprotease-3 (MMP-3) in fluorimetric assay | B | 8.46 | pIC50 | 3.5 | nM | IC50 | J Med Chem (2002) 45: 219-232 [PMID:11754593] |
| ChEMBL | Inhibitory activity against matrix metalloprotease-3 (MMP3) | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2003) 46: 3840-3852 [PMID:12930146] |
| ChEMBL | Inhibition of Matrix metalloprotease-3 | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 295-299 [PMID:11212095] |
| ChEMBL | Inhibition of human matrix metalloprotease-3 | B | 9.64 | pIC50 | 0.23 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1321-1326 [PMID:15713379] |
| MMP7/Matrix metalloproteinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4073] [GtoPdb: 1631] [UniProtKB: P09237] | ||||||||
| ChEMBL | Inhibition of matrilysin (Matrix metalloprotease-7) | B | 7.27 | pKi | 54 | nM | Ki | J Med Chem (1999) 42: 4547-4562 [PMID:10579818] |
| ChEMBL | In vitro inhibitory activity against matrilysin (matrix metalloprotease-7). | B | 7.04 | pIC50 | 91 | nM | IC50 | J Med Chem (1999) 42: 4547-4562 [PMID:10579818] |
| ChEMBL | Inhibition of Matrix metalloprotease-7 (MMP-7) in fluorimetric assay | B | 7.14 | pIC50 | 72 | nM | IC50 | J Med Chem (2002) 45: 219-232 [PMID:11754593] |
| ChEMBL | Inhibition of human matrix metalloprotease-7 | B | 7.27 | pIC50 | 54 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1321-1326 [PMID:15713379] |
| MMP8/Matrix metalloproteinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4588] [GtoPdb: 1632] [UniProtKB: P22894] | ||||||||
| ChEMBL | Inhibition of Matrix metalloprotease-8 (MMP-8) in fluorimetric assay | B | 9.27 | pIC50 | 0.54 | nM | IC50 | J Med Chem (2002) 45: 219-232 [PMID:11754593] |
| ChEMBL | Inhibition of neutrophil collagenase (Matrix metalloprotease-8) | B | 9.4 | pIC50 | <0.4 | nM | IC50 | J Med Chem (1999) 42: 4547-4562 [PMID:10579818] |
| MMP9/Matrix metalloproteinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL321] [GtoPdb: 1633] [UniProtKB: P14780] | ||||||||
| ChEMBL | Inhibition of recombinant human MMP9 using thiopeptide as substrate preincubated for 30 mins followed by substrate addition and measured every min for 20 mins by colorimetric assay | B | 8.48 | pIC50 | 3.3 | nM | IC50 | Eur J Med Chem (2019) 181: 111563-111563 [PMID:31415980] |
| ChEMBL | Inhibition of gelatinase-B (Matrix metalloprotease-9) | B | 9.4 | pIC50 | <0.4 | nM | IC50 | J Med Chem (1999) 42: 4547-4562 [PMID:10579818] |
| ChEMBL | Inhibition of human matrix metalloprotease-9 | B | 9.59 | pIC50 | 0.26 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1321-1326 [PMID:15713379] |
| ChEMBL | Inhibitory activity against matrix metalloprotease-9 (MMP9) | B | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2003) 46: 3840-3852 [PMID:12930146] |
| ChEMBL | Inhibition of Matrix metalloprotease-9 | B | 9.7 | pIC50 | 0.2 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 295-299 [PMID:11212095] |
| ChEMBL | In vitro selective inhibition against Matrix metalloprotease-9 (MMP-9) using fluorimetric assay | B | 10.32 | pIC50 | 0.05 | nM | IC50 | J Med Chem (2002) 45: 219-232 [PMID:11754593] |
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]
