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| ChEMBL ligand: CHEMBL3764045 (Pamufetinib, Tas-115) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581] | ||||||||
| GtoPdb | - | - | 7.41 | pKi | 39 | nM | Ki | Mol Cancer Ther (2013) 12: 2685-96 [PMID:24140932] |
| ChEMBL | Inhibition of recombinant N-terminal GST-tagged human Met using FLPeptide 2 as substrate after 90 mins by mobility shift assay | B | 7.49 | pIC50 | 32 | nM | IC50 | Eur J Med Chem (2016) 108: 495-504 [PMID:26717201] |
| ChEMBL | Inhibition of N-terminal GST-tagged human recombinant c-MET (956 to 1390 residues) expressed in Baculovirus infected Sf9 cell expression system by ELISA analysis | B | 7.49 | pIC50 | 32 | nM | IC50 | RSC Med Chem (2024) 15: 2553-2569 [PMID:39026631] |
| ChEMBL | Inhibition of c-Met (unknown origin) by mobility shift assay | B | 7.49 | pIC50 | 32 | nM | IC50 | Eur J Med Chem (2023) 261: 115796-115796 [PMID:37708796] |
| platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234] | ||||||||
| ChEMBL | Inhibition of wild type human PDGFRalpha transfected with CHO cells by ADP-Glo assay | B | 9.09 | pIC50 | 0.81 | nM | IC50 | Eur J Med Chem (2023) 260: 115762-115762 [PMID:37683364] |
| platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619] | ||||||||
| ChEMBL | Inhibition of PDGFRbeta (unknown origin) by DiscoverX KINOMEscan assay | B | 8.15 | pIC50 | 7.06 | nM | IC50 | Eur J Med Chem (2023) 260: 115762-115762 [PMID:37683364] |
| AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530] | ||||||||
| ChEMBL | Inhibition of AXL (unknown origin) by FRET assay | B | 7.82 | pIC50 | 15 | nM | IC50 | Eur J Med Chem (2023) 261: 115796-115796 [PMID:37708796] |
| kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
| GtoPdb | - | - | 7.92 | pKi | 12 | nM | Ki | Mol Cancer Ther (2013) 12: 2685-96 [PMID:24140932] |
| ChEMBL | Inhibition of recombinant N-terminal 6His-tagged VEGFR-2 (unknown origin) using FL-Peptide 22 as substrate after 90 mins by mobility shift assay | B | 7.52 | pIC50 | 30 | nM | IC50 | Eur J Med Chem (2016) 108: 495-504 [PMID:26717201] |
| ChEMBL | Inhibition of human recombinant VEGFR2 (805 to 1356 residues) in presence of ATP by ELISA analysis | B | 7.52 | pIC50 | 30 | nM | IC50 | RSC Med Chem (2024) 15: 2553-2569 [PMID:39026631] |
| ChEMBL | Inhibition of VEGFR-2 (unknown origin) by ELISA method | B | 7.52 | pIC50 | 30 | nM | IC50 | Eur J Med Chem (2023) 261: 115796-115796 [PMID:37708796] |
ChEMBL data shown on this page come from version 36:
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]