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 |
|---|---|---|---|---|---|---|---|---|
| ADAM17 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] |
| 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] |
| MMP1/Matrix metalloproteinase-1 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] |
| MMP10/Matrix metalloproteinase 10 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/Matrix metalloproteinase 11 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] |
| MMP12/Matrix metalloproteinase 12 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] |
| MMP13/Matrix metalloproteinase 13 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] |
| 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] |
| MMP2/Matrix metalloproteinase-2 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] |
| MMP3/Matrix metalloproteinase 3 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] |
| MMP7/Matrix metalloproteinase 7 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] |
| MMP8/Matrix metalloproteinase 8 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] |
| 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] |
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]
