RXP470.1 [Ligand Id: 7812] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL507420 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| MMP2/72 kDa type IV collagenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL333] [GtoPdb: 1629] [UniProtKB: P08253] | ||||||||
| ChEMBL | Inhibition of MMP2 | B | 6.72 | pKi | 192 | nM | Ki | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| Angiotensin-converting enzyme in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1808] [GtoPdb: 1613] [UniProtKB: P12821] | ||||||||
| ChEMBL | Inhibition of ACE | B | 4 | pKi | >100000 | nM | Ki | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| MMP13/Collagenase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL280] [GtoPdb: 1637] [UniProtKB: P45452] | ||||||||
| ChEMBL | Inhibition of human MMP13 catalytic domain using Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 fluorogenic substrate by spectrophotometric analysis | B | 6.86 | pKi | 139 | nM | Ki | J Med Chem (2017) 60: 403-414 [PMID:27996256] |
| ChEMBL | Inhibition of MMP13 | B | 7.31 | pKi | 49 | nM | Ki | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| ADAM17/Disintegrin and metalloproteinase domain-containing protein 17 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3706] [GtoPdb: 1662] [UniProtKB: P78536] | ||||||||
| ChEMBL | Inhibition of TACE | B | 4 | pKi | >100000 | nM | Ki | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| MMP1/Interstitial collagenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956] | ||||||||
| ChEMBL | Inhibition of MMP1 | B | 4.17 | pKi | 67000 | nM | Ki | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| MMP12/Macrophage metalloelastase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4393] [GtoPdb: 1636] [UniProtKB: P39900] | ||||||||
| GtoPdb | - | - | 8.62 | pKi | 2.4 | nM | Ki | J Med Chem (2013) 56: 1149-59 [PMID:23343195] |
| ChEMBL | Binding affinity to human MMP12 catalytic domain (98 to 266) by isothermal titration calorimetry | B | 9.59 | pKi | 0.26 | nM | Ki | J Med Chem (2013) 56: 1149-1159 [PMID:23343195] |
| ChEMBL | Inhibition of human MMP12 catalytic domain (98 to 266) at pH 6.8 by isothermal titration calorimetry | B | 9.62 | pKi | 0.24 | nM | Ki | J Med Chem (2013) 56: 1149-1159 [PMID:23343195] |
| ChEMBL | Inhibition of MMP12 | B | 9.72 | pKi | 0.19 | nM | Ki | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| MMP7/Matrilysin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4073] [GtoPdb: 1631] [UniProtKB: P09237] | ||||||||
| ChEMBL | Inhibition of MMP7 | B | 6.2 | pKi | 626 | nM | Ki | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| MMP14/Matrix metalloproteinase-14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3869] [GtoPdb: 1638] [UniProtKB: P50281] | ||||||||
| ChEMBL | Inhibition of MMP14 | B | 6.85 | pKi | 140 | nM | Ki | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| MMP9/Matrix metalloproteinase-9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL321] [GtoPdb: 1633] [UniProtKB: P14780] | ||||||||
| ChEMBL | Inhibition of MMP9 | B | 5.9 | pKi | 1265 | nM | Ki | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| Neutral endopeptidase/Neprilysin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944] [GtoPdb: 1611] [UniProtKB: P08473] | ||||||||
| ChEMBL | Inhibition of NEP | B | 4 | pKi | >100000 | nM | Ki | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| MMP8/Neutrophil collagenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4588] [GtoPdb: 1632] [UniProtKB: P22894] | ||||||||
| ChEMBL | Inhibition of MMP8 | B | 6.57 | pKi | 271 | nM | Ki | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| MMP3/Stromelysin-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL283] [GtoPdb: 1630] [UniProtKB: P08254] | ||||||||
| ChEMBL | Inhibition of MMP3 | B | 7.4 | pKi | 40 | nM | Ki | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| MMP10/Stromelysin-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4270] [GtoPdb: 1634] [UniProtKB: P09238] | ||||||||
| ChEMBL | Inhibition of human MMP10 catalytic domain using Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 fluorogenic substrate by spectrophotometric analysis | B | 6.83 | pKi | 149 | nM | Ki | J Med Chem (2017) 60: 403-414 [PMID:27996256] |
| MMP11/Stromelysin-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2867] [GtoPdb: 1635] [UniProtKB: P24347] | ||||||||
| ChEMBL | Inhibition of MMP11 | B | 4.74 | pKi | 18400 | nM | Ki | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
ChEMBL data shown on this page come from version 36:
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]
