CGS-27023A [Ligand Id: 8846] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL267178 (CGS-27023A) |
|---|
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
| 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] |
| ChEMBL | Inhibition of MMP-1 (unknown origin) | B | 7.48 | pIC50 | 33 | nM | IC50 | Eur J Med Chem (2020) 194: 112260-112260 [PMID:32224379] |
| MMP13/Matrix metalloproteinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL280] [GtoPdb: 1637] [UniProtKB: P45452] | ||||||||
| ChEMBL | Inhibition of MMP-13 (unknown origin) | B | 8.22 | pIC50 | 6 | nM | IC50 | Eur J Med Chem (2020) 194: 112260-112260 [PMID:32224379] |
| 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] |
| ChEMBL | Inhibition of MMP-2 (unknown origin) | B | 7.96 | pIC50 | 11 | nM | IC50 | Eur J Med Chem (2020) 194: 112260-112260 [PMID:32224379] |
| 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] |
| ChEMBL | Inhibition of MMP-3 (unknown origin) | B | 7.89 | pIC50 | 13 | nM | IC50 | Eur J Med Chem (2020) 194: 112260-112260 [PMID:32224379] |
| 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 MMP-9 (unknown origin) | B | 8.1 | pIC50 | 8 | nM | IC50 | Eur J Med Chem (2020) 194: 112260-112260 [PMID:32224379] |
| 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 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]
