compound 15 [PMID: 22017539] [Ligand Id: 8636] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1939876 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| MMP13 in Human [GtoPdb: 1637] [UniProtKB: P45452] | ||||||||
| GtoPdb | - | - | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2011) 54: 8174-87 [PMID:22017539] |
| MMP13/Collagenase 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3638350] [GtoPdb: 1637] [UniProtKB: P33435] | ||||||||
| ChEMBL | Biological Assay: The EnzoLyte 520 Generic MMP Assay Kit (AnaSpec Inc.) can detect the activity of several MMPs including MMP-1, 2, 3, 7, 8, 9, 13, and 14. This kit uses a 5-FAM/QXL 520 fluorescence resonance energy transfer (FRET) peptide as an MMP substrate. In the intact FRET peptide, the fluorescence of 5-FAM is quenched by QXL 520. Upon cleavage into two separate fragments by MMPs, the fluorescence of 5-FAM is recovered, and can be monitored at excitation/emission wavelengths=490 nm/520 nm. The assays are performed in a convenient 96-well or 384-well microplate format. | B | 9.1 | pIC50 | 0.8 | nM | IC50 | US-8785489-B2. Heteroaryl substituted indole compounds useful as MMP-13 inhibitors (2014) |
| D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] | ||||||||
| ChEMBL | GPCRScan assay: inhibition of D5 | B | 5 | pKi | 10000 | nM | Ki | Data for DCP probe BI-4394 |
| ChEMBL | GPCRScan assay: inhibition of D5 | B | 5 | pKi | 10000 | nM | Ki | Data for DCP probe BI-4394 |
| MMP1/Matrix metalloproteinase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL332] [GtoPdb: 1628] [UniProtKB: P03956] | ||||||||
| ChEMBL | Inhibition of human recombinant MMP1 after 30 mins by fluorimetry | B | 4.66 | pIC50 | >22000 | nM | IC50 | J Med Chem (2011) 54: 8174-8187 [PMID:22017539] |
| MMP10/Matrix metalloproteinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4270] [GtoPdb: 1634] [UniProtKB: P09238] | ||||||||
| ChEMBL | Inhibition of human recombinant MMP10 after 30 mins by fluorimetry | B | 4.8 | pIC50 | 16000 | nM | IC50 | J Med Chem (2011) 54: 8174-8187 [PMID:22017539] |
| MMP12/Matrix metalloproteinase 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4393] [GtoPdb: 1636] [UniProtKB: P39900] | ||||||||
| ChEMBL | Inhibition of human recombinant MMP12 after 30 mins by fluorimetry | B | 4.66 | pIC50 | >22000 | nM | IC50 | J Med Chem (2011) 54: 8174-8187 [PMID:22017539] |
| MMP13/Matrix metalloproteinase 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL280] [GtoPdb: 1637] [UniProtKB: P45452] | ||||||||
| ChEMBL | Inhibition of human MMP13-mediated degradation of bovine nasal cartilage after 2 hrs by ELISA in the presence of 10% human serum | B | 7.51 | pIC50 | 31 | nM | IC50 | J Med Chem (2011) 54: 8174-8187 [PMID:22017539] |
| ChEMBL | Inhibition of AMPA-activated MMP13-mediated degradation of FITC-labeled type2 collagen after 1.5 hrs by fluorimetry | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2011) 54: 8174-8187 [PMID:22017539] |
| ChEMBL | MMP13 collagen degradation assay | B | 7.96 | pIC50 | 11 | nM | IC50 | Data for DCP probe BI-4394 |
| ChEMBL | Inhibition of MMP13 after 30 mins by fluorimetry in the presence of 1.25% human serum albumin | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2011) 54: 8174-8187 [PMID:22017539] |
| GtoPdb | - | - | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2011) 54: 8174-87 [PMID:22017539] |
| ChEMBL | Inhibition of human MMP13 expressed in Escherichia coli after 30 mins by fluorimetry | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (2011) 54: 8174-8187 [PMID:22017539] |
| ChEMBL | Biochemical assay (FRET) with MMP13 | B | 9 | pIC50 | 1 | nM | IC50 | Data for DCP probe BI-4394 |
| MMP14/Matrix metalloproteinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3869] [GtoPdb: 1638] [UniProtKB: P50281] | ||||||||
| ChEMBL | Inhibition of human recombinant MMP14 after 60 mins by fluorimetry | B | 5.08 | pIC50 | 8300 | nM | IC50 | J Med Chem (2011) 54: 8174-8187 [PMID:22017539] |
| MMP2/Matrix metalloproteinase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL333] [GtoPdb: 1629] [UniProtKB: P08253] | ||||||||
| ChEMBL | Inhibition of human recombinant MMP2 after 30 mins by fluorimetry | B | 4.74 | pIC50 | 18000 | nM | IC50 | J Med Chem (2011) 54: 8174-8187 [PMID:22017539] |
| MMP3/Matrix metalloproteinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL283] [GtoPdb: 1630] [UniProtKB: P08254] | ||||||||
| ChEMBL | Inhibition of human recombinant MMP3 after 30 mins by fluorimetry | B | 4.66 | pIC50 | >22000 | nM | IC50 | J Med Chem (2011) 54: 8174-8187 [PMID:22017539] |
| MMP7/Matrix metalloproteinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4073] [GtoPdb: 1631] [UniProtKB: P09237] | ||||||||
| ChEMBL | Inhibition of human recombinant MMP7 after 30 mins by fluorimetry | B | 4.66 | pIC50 | >22000 | nM | IC50 | J Med Chem (2011) 54: 8174-8187 [PMID:22017539] |
| MMP8/Matrix metalloproteinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4588] [GtoPdb: 1632] [UniProtKB: P22894] | ||||||||
| ChEMBL | Inhibition of human recombinant MMP8 after 30 mins by fluorimetry | B | 4.66 | pIC50 | >22000 | nM | IC50 | J Med Chem (2011) 54: 8174-8187 [PMID:22017539] |
| MMP9/Matrix metalloproteinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL321] [GtoPdb: 1633] [UniProtKB: P14780] | ||||||||
| ChEMBL | Inhibition of human recombinant MMP9 after 30 mins by fluorimetry | B | 5.05 | pIC50 | 8900 | nM | IC50 | J Med Chem (2011) 54: 8174-8187 [PMID:22017539] |
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]
