NVP-TAE 226 [Ligand Id: 9382] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL458997 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73] | ||||||||
| ChEMBL | Inhibition of ALK by cell based assay | B | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 463-466 [PMID:21074994] |
| ChEMBL | Inhibition of ALK | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 463-466 [PMID:21074994] |
| mitogen-activated protein kinase 9/c-Jun N-terminal kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4179] [GtoPdb: 1497] [UniProtKB: P45984] | ||||||||
| ChEMBL | Inhibition of JNK2 (unknown origin) using biotinylated ATF2 by HTRF method | B | 7.38 | pIC50 | 42 | nM | IC50 | Medchemcomm (2012) 3: 238-243 |
| mitogen-activated protein kinase 10/c-Jun N-terminal kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2637] [GtoPdb: 1498] [UniProtKB: P53779] | ||||||||
| ChEMBL | Inhibition of JNK3 (unknown origin) using biotinylated ATF2 by HTRF method | B | 7.92 | pIC50 | 12 | nM | IC50 | Medchemcomm (2012) 3: 238-243 |
| epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Inhibition of GST-tagged recombinant HER1 (unknown origin) expressed in baculovirus expression system incubated for 15-45 mins in presence of [gamma32P]-ATP by radiometric assay | B | 6.26 | pIC50 | 550 | nM | IC50 | J Med Chem (2020) 63: 12707-12724 [PMID:33119295] |
| fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] | ||||||||
| ChEMBL | Inhibition of GST-tagged recombinant FGFR1 (unknown origin) expressed in baculovirus expression system incubated for 15-45 mins in presence of [gamma32P]-ATP by radiometric assay | B | 6.12 | pIC50 | 750 | nM | IC50 | J Med Chem (2020) 63: 12707-12724 [PMID:33119295] |
| protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397] | ||||||||
| ChEMBL | Inhibition of FAK (unknown origin) by FRET-based Z'-Lyte assay | B | 5.28 | pIC50 | 5200 | nM | IC50 | Eur J Med Chem (2021) 222: 113569-113569 [PMID:34111829] |
| ChEMBL | Inhibition of human recombinant full length FAK incubated for 40 mins in presence of Mg/ATP mix by [gamma p33]-ATP based scintillation counting method | B | 7.44 | pIC50 | 36 | nM | IC50 | Bioorg Med Chem Lett (2021) 54: 128433-128433 [PMID:34757216] |
| ChEMBL | Inhibition of FAK (unknown origin) | B | 8.08 | pIC50 | 8.3 | nM | IC50 | Eur J Med Chem (2023) 250: 115192-115192 [PMID:36801517] |
| ChEMBL | Inhibition of pre-activated recombinant full length FAK (unknown origin) using ULight labeled poly(Glu/Tyr) as substrate after 1.6 hrs by TR-FRET assay | B | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 4552-4556 [PMID:23845217] |
| ChEMBL | Inhibition of FAK (unknown origin) using ULight-poly GT as substrate after 1.6 hrs by TR-FRET assay | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2015) 58: 237-251 [PMID:25180654] |
| ChEMBL | Inhibition of FAK (unknown origin) using Ulight-poly(Glu:Tyr)(4:1) as substrate after 1.6 hrs by TR-FRET assay | B | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1727-1730 [PMID:28284808] |
| ChEMBL | Inhibition of N-terminal DYKDDDD-tagged truncated FAK (376 to 1052 residues) (unknown origin) expressed in Sf21 insect cells using TK as substrate in presence of ATP measured after 50 mins by HTRF assay | B | 8.16 | pIC50 | 6.9 | nM | IC50 | Eur J Med Chem (2022) 237: 114373-114373 [PMID:35486993] |
| ChEMBL | Inhibition of human recombinant N-terminal His-tagged FAK (393 to 698 residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) peptide substrate incubated for 60 mins by ADP-Glo assay | B | 8.17 | pIC50 | 6.79 | nM | IC50 | Eur J Med Chem (2019) 172: 154-162 [PMID:30978560] |
| ChEMBL | Inhibition of recombinant human N-terminal His-tagged FAK (393 to 698 residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) peptide as substrate measured after 60 mins by ADP-Glo kinase assay | B | 8.17 | pIC50 | 6.79 | nM | IC50 | Bioorg Med Chem (2017) 25: 3989-3996 [PMID:28576633] |
| ChEMBL | Inhibition of recombinant human N-terminal His-tagged FAK cytoplasmic domain (393 to 698 residues) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation after 60 mins by ADP-Glo kinase assay | B | 8.17 | pIC50 | 6.79 | nM | IC50 | Bioorg Med Chem (2017) 25: 6313-6321 [PMID:29102081] |
| ChEMBL | Inhibition of N-terminal GST-fused human truncated FAK (376 to 1052 residues) expressed in baculovirus expression system using tyrosine kinase peptide as substrate measured after 50 mins in presence of ATP by homogenous time resolved flourescence assay | B | 8.2 | pIC50 | 6.3 | nM | IC50 | Eur J Med Chem (2020) 188: 112024-112024 [PMID:31923858] |
| ChEMBL | Inhibition of FAK (unknown origin) incubated for 50 mins in presence of substrate/ATP by HTRF assay | B | 8.2 | pIC50 | 6.3 | nM | IC50 | RSC Med Chem (2023) 14: 2301-2314 [PMID:37974962] |
| ChEMBL | Inhibition of recombinant N-terminal GST-tagged human FAK (327 to 1052 residues) expressed in baculovirus expression system using TK as substrate incubated for 50 mins in presence of ATP and measured after 1 hr by HTRF assay | B | 8.21 | pIC50 | 6.2 | nM | IC50 | Eur J Med Chem (2019) 183: 111716-111716 [PMID:31550660] |
| ChEMBL | Inhibition of recombinant human N-terminal His-tagged FAK (393 to 698 residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate measured after 1 hr by ADP-glo luminescence assay | B | 8.24 | pIC50 | 5.8 | nM | IC50 | J Med Chem (2020) 63: 12707-12724 [PMID:33119295] |
| ChEMBL | Inhibition of FAK (unknown origin) | B | 8.26 | pIC50 | 5.5 | nM | IC50 | Med Chem Res (2013) null: 1-22 |
| ChEMBL | Inhibition of FAK (unknown origin) | B | 8.26 | pIC50 | 5.5 | nM | IC50 | RSC Med Chem (2023) 14: 2301-2314 [PMID:37974962] |
| ChEMBL | Inhibition of FAK (unknown origin) | B | 8.26 | pIC50 | 5.5 | nM | IC50 | Eur J Med Chem (2019) 177: 32-46 [PMID:31129452] |
| ChEMBL | Inhibition of Focal adhesion kinase (unknown origin) | B | 8.26 | pIC50 | 5.5 | nM | IC50 | ACS Med Chem Lett (2021) 12: 30-38 [PMID:33488961] |
| ChEMBL | Inhibition of recombinant FAK domain (unknown origin) | B | 8.26 | pIC50 | 5.5 | nM | IC50 | Eur J Med Chem (2022) 237: 114373-114373 [PMID:35486993] |
| GtoPdb | - | - | 8.26 | pIC50 | 5.5 | nM | IC50 |
Mol Carcinog (2007) 46: 488-96 [PMID:17219439]; Mol Cancer Ther (2007) 6: 1357-67 [PMID:17431114] |
| ChEMBL | Inhibition of GST-tagged recombinant FAK (unknown origin) expressed in baculovirus expression system incubated for 15-45 mins in presence of [gamma32P]-ATP by radiometric assay | B | 8.27 | pIC50 | 5.4 | nM | IC50 | J Med Chem (2020) 63: 12707-12724 [PMID:33119295] |
| ChEMBL | Inhibition of recombinant human FAK (393 to 698 residues) using poly (4:1 Glu, Tyr) peptide as substrate incubated for 60 mins in presence of ATP by ADP-Glo reagent based luminescent assay | B | 8.35 | pIC50 | 4.5 | nM | IC50 | Eur J Med Chem (2022) 241: 114607-114607 [PMID:35872546] |
| Insulin-like growth factor I receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069] | ||||||||
| ChEMBL | Inhibition of IGF1R (unknown origin) | B | 6.8 | pIC50 | 160 | nM | IC50 | ACS Med Chem Lett (2021) 12: 30-38 [PMID:33488961] |
| GtoPdb | In vitro kinase assay with recombinant kinase domains and peptide substrates. | - | 6.85 | pIC50 | ~140 | nM | IC50 | Mol Cancer Ther (2007) 6: 1357-67 [PMID:17431114] |
| ChEMBL | Inhibition of GST-tagged recombinant IGFR1 (unknown origin) expressed in baculovirus expression system incubated for 15-45 mins in presence of [gamma32P]-ATP by radiometric assay | B | 7.09 | pIC50 | 81 | nM | IC50 | J Med Chem (2020) 63: 12707-12724 [PMID:33119295] |
| Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
| ChEMBL | Inhibition of GST-tagged recombinant INSR (unknown origin) expressed in baculovirus expression system incubated for 15-45 mins in presence of [gamma32P]-ATP by radiometric assay | B | 7.37 | pIC50 | 43 | nM | IC50 | J Med Chem (2020) 63: 12707-12724 [PMID:33119295] |
| ChEMBL | Inhibition of recombinant insulin receptor (unknown origin) | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2015) 58: 237-251 [PMID:25180654] |
| GtoPdb | In vitro kinase assay with recombinant kinase domains and peptide substrates. | - | 7.59 | pIC50 | 26 | nM | IC50 | Mol Cancer Ther (2007) 6: 1357-67 [PMID:17431114] |
| ChEMBL | Inhibition of insulin receptor | B | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 463-466 [PMID:21074994] |
| 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 GST-tagged recombinant PDGFRbeta (unknown origin) expressed in baculovirus expression system incubated for 15-45 mins in presence of [gamma32P]-ATP by radiometric assay | B | 5.59 | pIC50 | 2600 | nM | IC50 | J Med Chem (2020) 63: 12707-12724 [PMID:33119295] |
| 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 GST-tagged recombinant HER2 (unknown origin) expressed in baculovirus expression system incubated for 15-45 mins in presence of [gamma32P]-ATP by radiometric assay | B | 6.15 | pIC50 | 710 | nM | IC50 | J Med Chem (2020) 63: 12707-12724 [PMID:33119295] |
| aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] | ||||||||
| ChEMBL | Inhibition of human AURKA | B | 8.4 | pIC50 | 4 | nM | IC50 | Eur J Med Chem (2016) 124: 896-905 [PMID:27668758] |
| protein tyrosine kinase 2 beta in Human [GtoPdb: 2181] [UniProtKB: Q14289] | ||||||||
| GtoPdb | - | - | 8.7 | pIC50 | 2 | nM | IC50 | Mol Cancer Ther (2007) 6: 1357-67 [PMID:17431114] |
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]
