INCB3619 [Ligand Id: 8679] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL434567 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ADAM10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5028] [GtoPdb: 1658] [UniProtKB: O14672] | ||||||||
| ChEMBL | Inhibition of ADAM10 | B | 7.23 | pIC50 | 59 | nM | IC50 | J Med Chem (2007) 50: 603-606 [PMID:17256836] |
| ChEMBL | Inhibition of ADAM10 | B | 7.66 | pIC50 | 22 | nM | IC50 | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| ChEMBL | Inhibition of human ADAM10 | B | 7.66 | pIC50 | 22 | nM | IC50 | J Med Chem (2015) 58: 5808-5824 [PMID:26192023] |
| ADAM17 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3706] [GtoPdb: 1662] [UniProtKB: P78536] | ||||||||
| ChEMBL | Inhibition of ADAM17 in human A549 cells assessed as potentiation of gefitinib-mediated inhibition of cell viability by measuring gefitinib IC50 at 10 uM after 96 hrs by CellTiter-Glo assay (Rvb = 8 microM) | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2015) 58: 5808-5824 [PMID:26192023] |
| ChEMBL | Inhibition of TACE | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| ADAM17 in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3332] [UniProtKB: O77636] | ||||||||
| ChEMBL | Inhibition of porcine spleen ADAM17 | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2015) 58: 5808-5824 [PMID:26192023] |
| ADAM9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5982] [GtoPdb: 1657] [UniProtKB: Q13443] | ||||||||
| ChEMBL | Inhibition of ADAM9 | B | 5.3 | pIC50 | >5000 | nM | IC50 | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| ADAM33/Disintegrin and metalloproteinase domain-containing protein 33 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6121] [GtoPdb: 1673] [UniProtKB: Q9BZ11] | ||||||||
| ChEMBL | Inhibition of ADAM33 | B | 5.99 | pIC50 | 1026 | nM | IC50 | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| GtoPdb | - | - | 5.99 | pIC50 | 1026 | nM | IC50 | Bioorg Med Chem (2008) 16: 8781-94 [PMID:18790648] |
| ADAM8/Disintegrin and metalloproteinase domain-containing protein 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5665] [GtoPdb: 1656] [UniProtKB: P78325] | ||||||||
| GtoPdb | - | - | 6 | pIC50 | 1000 | nM | IC50 | Bioorg Med Chem (2008) 16: 8781-94 [PMID:18790648] |
| ChEMBL | Inhibition of ADAM8 | B | 6 | pIC50 | 1000 | nM | IC50 | 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 | 5.3 | pIC50 | >5000 | nM | IC50 | J Med Chem (2007) 50: 603-606 [PMID:17256836] |
| ChEMBL | Inhibition of MMP1 | B | 5.3 | pIC50 | >5000 | nM | IC50 | 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] | ||||||||
| ChEMBL | Inhibition of MMP12 | B | 7.77 | pIC50 | 17 | nM | IC50 | 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 | 6.11 | pIC50 | 772 | nM | IC50 | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| ChEMBL | Inhibition of human MT1-MMP | B | 6.11 | pIC50 | 772 | nM | IC50 | J Med Chem (2015) 58: 5808-5824 [PMID:26192023] |
| MMP2/Matrix metalloproteinase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL333] [GtoPdb: 1629] [UniProtKB: P08253] | ||||||||
| ChEMBL | Inhibition of MMP2 | B | 7.41 | pIC50 | 39 | nM | IC50 | J Med Chem (2007) 50: 603-606 [PMID:17256836] |
| ChEMBL | Inhibition of MMP2 | B | 7.46 | pIC50 | 35 | nM | IC50 | 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 | 5.4 | pIC50 | 4000 | nM | IC50 | J Med Chem (2007) 50: 603-606 [PMID:17256836] |
| ChEMBL | Inhibition of MMP3 | B | 5.45 | pIC50 | 3560 | nM | IC50 | 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 | 5.3 | pIC50 | >5000 | nM | IC50 | 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 | 6.37 | pIC50 | 428 | nM | IC50 | J Med Chem (2007) 50: 603-606 [PMID:17256836] |
| ChEMBL | Inhibition of MMP9 | B | 6.52 | pIC50 | 304 | nM | IC50 | Bioorg Med Chem (2008) 16: 8781-8794 [PMID:18790648] |
| erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626] | ||||||||
| ChEMBL | Inhibition of Her2 sheddase activity in BT474 cell line | F | 7.17 | pIC50 | 68 | nM | IC50 | J Med Chem (2007) 50: 603-606 [PMID:17256836] |
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]
