CGS-27023A [Ligand Id: 8846] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL267178 (CGS-27023A) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| MMP1/Matrix metalloproteinase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956] | ||||||||
| GtoPdb | - | - | 7.25 | pIC50 | 56 | nM | IC50 | Eur J Med Chem (2011) 46: 2617-29 [PMID:21514700] |
| ChEMBL | Inhibition of recombinant human pro-MMP1 using Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate preincubated for 3 hrs followed by substrate addition and measured every 10 secs for 15 mins in presence of APMA by fluorometric assay | B | 7.25 | pIC50 | 56 | nM | IC50 | Bioorg Med Chem (2019) 27: 196-207 [PMID:30522899] |
| MMP14/Matrix metalloproteinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3869] [GtoPdb: 1638] [UniProtKB: P50281] | ||||||||
| ChEMBL | Inhibition of recombinant human MT1-MMP catalytic domain using Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate preincubated for 3 hrs followed by substrate addition and measured every 10 secs for 15 min by fluorometric assay | B | 7.64 | pIC50 | 23 | nM | IC50 | Bioorg Med Chem (2019) 27: 196-207 [PMID:30522899] |
| GtoPdb | - | - | 7.64 | pIC50 | 23 | nM | IC50 | Eur J Med Chem (2011) 46: 2617-29 [PMID:21514700] |
| MMP2/Matrix metalloproteinase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL333] [GtoPdb: 1629] [UniProtKB: P08253] | ||||||||
| ChEMBL | Inhibition of recombinant human MMP2 preincubated for 30 mins followed by McaPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 substrate addition measured by fluorescence assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2413-2417 [PMID:29921475] |
| GtoPdb | - | - | 7.6 | pIC50 | 25 | nM | IC50 | Eur J Med Chem (2011) 46: 2617-29 [PMID:21514700] |
| ChEMBL | Inhibition of recombinant human proMMP2 using Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate preincubated for 3 hrs followed by substrate addition and measured every 10 secs for 15 mins in presence of APMA by fluorometric assay | B | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem (2019) 27: 196-207 [PMID:30522899] |
| MMP3/Matrix metalloproteinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL283] [GtoPdb: 1630] [UniProtKB: P08254] | ||||||||
| ChEMBL | Inhibition of recombinant human MMP3 (Tyr18 to Cys477 residues) expressed in mouse myeloma cells using Mca-Pro-LeuGly-Leu-Dpa-Ala-Arg-NH2 as substrate preincubated for 30 mins followed by substrate addition by fluorescence assay | B | 7.52 | pIC50 | 30 | nM | IC50 | Eur J Med Chem (2017) 138: 979-992 [PMID:28756264] |
| ChEMBL | Inhibition of recombinant human MMP3 preincubated for 30 mins followed by McaPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 substrate addition measured by fluorescence assay | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2413-2417 [PMID:29921475] |
| GtoPdb | - | - | 7.8 | pIC50 | 16 | nM | IC50 | Eur J Med Chem (2011) 46: 2617-29 [PMID:21514700] |
| MMP8/Matrix metalloproteinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4588] [GtoPdb: 1632] [UniProtKB: P22894] | ||||||||
| ChEMBL | Inhibition of recombinant human MMP8 (Phe21 to Gly467 residues) expressed in mouse myeloma cells using Mca-Pro-LeuGly-Leu-Dpa-Ala-Arg-NH2 as substrate preincubated for 30 mins followed by substrate addition by fluorescence assay | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2017) 138: 979-992 [PMID:28756264] |
| GtoPdb | - | - | 8.11 | pIC50 | 7.7 | nM | IC50 | Eur J Med Chem (2011) 46: 2617-29 [PMID:21514700] |
| MMP9/Matrix metalloproteinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL321] [GtoPdb: 1633] [UniProtKB: P14780] | ||||||||
| ChEMBL | Inhibition of recombinant human MMP9 preincubated for 30 mins followed by McaPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 substrate addition measured by fluorescence assay | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2413-2417 [PMID:29921475] |
| ChEMBL | Inhibition of recombinant human MMP9 (Ala20 to Asp707 residues) expressed in CHO cells using Mca-Pro-LeuGly-Leu-Dpa-Ala-Arg-NH2 as substrate preincubated for 30 mins followed by substrate addition by fluorescence assay | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2017) 138: 979-992 [PMID:28756264] |
| ChEMBL | Inhibition of recombinant human proMMP9 using Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate preincubated for 3 hrs followed by substrate addition and measured every 10 secs for 15 mins in presence of APMA by fluorometric assay | B | 8.32 | pIC50 | 4.8 | nM | IC50 | Bioorg Med Chem (2019) 27: 196-207 [PMID:30522899] |
| GtoPdb | - | - | 8.32 | pIC50 | 4.8 | nM | IC50 | Eur J Med Chem (2011) 46: 2617-29 [PMID:21514700] |
| MMP25 in Human [GtoPdb: 1647] [UniProtKB: Q9NPA2] | ||||||||
| GtoPdb | - | - | 8.82 | pIC50 | 1.5 | nM | IC50 | Eur J Med Chem (2011) 46: 2617-29 [PMID:21514700] |
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]
