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 MMP-1 (unknown origin) | B | 8.08 | pKi | 8.3 | nM | Ki | Eur J Med Chem (2021) 223: 113623-113623 [PMID:34157437] |
| 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 | Inhibition of MMP-13 (unknown origin) | B | 10.52 | pKi | 0.03 | nM | Ki | Eur J Med Chem (2021) 223: 113623-113623 [PMID:34157437] |
| 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 human MMP-2 assessed as inhibition constant using MCA-Pro-Leu-Gly-Leu-DPA-Ala-Arg-NH2 substrate by fluorimetric analysis | B | 10.3 | pKi | 0.05 | nM | Ki | Eur J Med Chem (2020) 194: 112260-112260 [PMID:32224379] |
| ChEMBL | Inhibition of MMP-2 (unknown origin) | B | 10.52 | pKi | 0.03 | nM | Ki | Eur J Med Chem (2021) 223: 113623-113623 [PMID:34157437] |
| 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 | Inhibition of MMP-3 (unknown origin) | B | 10.52 | pKi | 0.03 | nM | Ki | Eur J Med Chem (2021) 223: 113623-113623 [PMID:34157437] |
| 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 human MMP-9 assessed as inhibition constant using MCA-Pro-Leu-Gly-Leu-DPA-Ala-Arg-NH2 substrate by fluorimetric analysis | B | 9.59 | pKi | 0.26 | nM | Ki | Eur J Med Chem (2020) 194: 112260-112260 [PMID:32224379] |
| ChEMBL | Inhibition of MMP-9 (unknown origin) | B | 10.52 | pKi | 0.03 | nM | Ki | Eur J Med Chem (2021) 223: 113623-113623 [PMID:34157437] |
| 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
