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] |
| ChEMBL | Inhibition of human ADAM10 using (7-methoxycour-marin-4-yl)-acetyl-Pro-Leu-Ala-Gln-Ala-Val-(3-[2,4-dinitrophenyl]- L -2, 3-diaminopropionyl)-Arg-Ser-Ser-Ser-Arg-NH2 as a substrate | B | 7.66 | pIC50 | 22 | nM | IC50 | Eur J Med Chem (2021) 226: 113877-113877 [PMID:34624823] |
| 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] |
| ChEMBL | Inhibition of porcine ADAM17 using (7-methoxycour-marin-4-yl)-acetyl-Pro-Leu-Ala-Gln-Ala-Val-(3-[2,4-dinitrophenyl]- L -2, 3-diaminopropionyl)-Arg-Ser-Ser-Ser-Arg-NH2 as a substrate | B | 7.85 | pIC50 | 14 | nM | IC50 | Eur J Med Chem (2021) 226: 113877-113877 [PMID:34624823] |
| 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 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]
