brigatinib [Ligand Id: 7741] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3545311 (Alunbrig, Ap-26113, AP-26113, AP26113, Brigatinib) |
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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] | ||||||||
| GtoPdb | Wild type ALK | - | 10.05 | pKi | 0.09 | nM | Ki | Proc Natl Acad Sci USA (2011) 108: 7535-40 [PMID:21502504] |
| ChEMBL | Inhibition of ALK phosphorylation in human SUPM2 cells harboring NPM-ALK fusion protein incubated for 1 hrs by immunoblot analysis | B | 7.92 | pIC50 | 12 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of human ALK R1275Q mutant using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 8.18 | pIC50 | 6.6 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of ALK phosphorylation in human DEL cells harboring NPM-ALK fusion protein incubated for 1 hrs by immunoblot analysis | B | 8.18 | pIC50 | 6.6 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of human ALK G1202R mutant using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 8.31 | pIC50 | 4.9 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of human ALK G1202R mutant using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-33P]-ATP assay by radiometric HotSpot assay | B | 8.31 | pIC50 | 4.9 | nM | IC50 | J Med Chem (2020) 63: 10726-10741 [PMID:32432477] |
| ChEMBL | Inhibition of ALK G1202R mutant (unknown origin) | B | 8.31 | pIC50 | 4.9 | nM | IC50 | J Med Chem (2022) 65: 15540-15558 [PMID:36395392] |
| ChEMBL | Inhibition of ALK phosphorylation in human NCI-H2228 cells harboring EML4-ALK variant 3a/3b fusion protein incubated for 1 hrs by immunoblot analysis | B | 8.35 | pIC50 | 4.5 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Binding affinity to ALK G1202R mutant (unknown origin) | B | 8.39 | pIC50 | 4.1 | nM | IC50 | J Med Chem (2021) 64: 9152-9165 [PMID:34138566] |
| ChEMBL | Inhibition of ALK phosphorylation in human NCI-H3122 cells harboring EML4-ALK variant 1 fusion protein incubated for 1 hrs by immunoblot analysis | B | 8.43 | pIC50 | 3.7 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of ALK phosphorylation in human KARPAS-299 cells harboring NPM-ALK fusion protein incubated for 1 hrs by immunoblot analysis | B | 8.49 | pIC50 | 3.2 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of ALK phosphorylation in human L-82 cells harboring NPM-ALK fusion protein incubated for 1 hrs by immunoblot analysis | B | 8.68 | pIC50 | 2.1 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of human ALK L1196M mutant using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 8.77 | pIC50 | 1.7 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of human ALK L1196M mutant using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-33P]-ATP assay by radiometric HotSpot assay | B | 8.77 | pIC50 | 1.7 | nM | IC50 | J Med Chem (2020) 63: 10726-10741 [PMID:32432477] |
| ChEMBL | Inhibition of ALK L1196M mutant (unknown origin) | B | 8.77 | pIC50 | 1.7 | nM | IC50 | J Med Chem (2022) 65: 15540-15558 [PMID:36395392] |
| ChEMBL | Inhibition of ALK phosphorylation in human SU-DHL-1 cells harboring NPM-ALK fusion protein incubated for 1 hrs by immunoblot analysis | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of human ALK F1174L mutant using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 8.85 | pIC50 | 1.4 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Binding affinity to ALK (unknown origin) | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2021) 64: 9152-9165 [PMID:34138566] |
| ChEMBL | Inhibition of human ALK using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of human ALK C1156Y mutant using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| GtoPdb | - | - | 9.43 | pIC50 | 0.37 | nM | IC50 |
Proc Natl Acad Sci USA (2011) 108: 7535-40 [PMID:21502504]; J Med Chem (2016) 59: 4948-64 [PMID:27144831] |
| ChEMBL | Inhibition of human ALK using poly[Glu:Tyr] (4:1) as substrate and [gamma-33P]ATP measured after 1 hr | B | 9.43 | pIC50 | 0.37 | nM | IC50 | J Med Chem (2016) 59: 4948-4964 [PMID:27144831] |
| TEK receptor tyrosine kinase/Angiopoietin-1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763] | ||||||||
| ChEMBL | Inhibition of human TEK using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6 | pIC50 | >1000 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| aurora kinase A/Aurora kinase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] | ||||||||
| ChEMBL | Inhibition of human AURKA using H-LRRASLG as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.84 | pIC50 | 146 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| aurora kinase B/Aurora kinase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4] | ||||||||
| ChEMBL | Inhibition of human AURKB using H-LRRASLG as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6 | pIC50 | >1000 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| aurora kinase C/Aurora kinase C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3935] [GtoPdb: 1938] [UniProtKB: Q9UQB9] | ||||||||
| ChEMBL | Inhibition of human AURKC using H-LRRASLG as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6 | pIC50 | >1000 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| neurotrophic receptor tyrosine kinase 2/BDNF/NT-3 growth factors receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620] | ||||||||
| ChEMBL | Inhibition of human NTRK2 using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6 | pIC50 | >1000 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| calcium/calmodulin dependent protein kinase kinase 2/Calcium/calmodulin-dependent protein kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5284] [GtoPdb: 1957] [UniProtKB: Q96RR4] | ||||||||
| ChEMBL | Inhibition of human CAMKK2 using MBP as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.09 | pIC50 | 82 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| calcium/calmodulin-dependent protein kinase II delta subunit/Calcium/calmodulin-dependent protein kinase type II subunit delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2801] [GtoPdb: 1558] [UniProtKB: Q13557] | ||||||||
| ChEMBL | Inhibition of human CAMK2D using KKLNRTLSFAEPG as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.54 | pIC50 | 29 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| calcium/calmodulin-dependent protein kinase II gamma subunit/Calcium/calmodulin-dependent protein kinase type II subunit gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3829] [GtoPdb: 1557] [UniProtKB: Q13555] | ||||||||
| ChEMBL | Inhibition of human CAMK2G using KKLNRTLSFAEPG as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.32 | pIC50 | 48 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| Protein kinase G (PKG) 1/cGMP-dependent protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4273] [GtoPdb: 1492] [UniProtKB: Q13976] | ||||||||
| ChEMBL | Inhibition of human PRKG1 using LRRASLG as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6 | pIC50 | >1000 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| CDC like kinase 1/Dual specificity protein kinase CLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759] | ||||||||
| ChEMBL | Inhibition of human CLK1 using MBP as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.64 | pIC50 | 23 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| CDC like kinase 2/Dual specificity protein kinase CLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760] | ||||||||
| ChEMBL | Inhibition of human CLK2 using MBP as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.62 | pIC50 | 240 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| EPH receptor A1/Ephrin type-A receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5810] [GtoPdb: 1821] [UniProtKB: P21709] | ||||||||
| ChEMBL | Inhibition of human EPHA1 using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6 | pIC50 | >1000 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| EPH receptor A7/Ephrin type-A receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4602] [GtoPdb: 1827] [UniProtKB: Q15375] | ||||||||
| ChEMBL | Inhibition of human EPHA7 using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6 | pIC50 | >1000 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| EPH receptor B1/Ephrin type-B receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5072] [GtoPdb: 1830] [UniProtKB: P54762] | ||||||||
| ChEMBL | Inhibition of human EPHB1 using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6 | pIC50 | >1000 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| epidermal growth factor receptor/Epidermal growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Inhibition of EGFR phosphorylation in EGF-stimulated human NCI-H358 cells preincubated with compound for 2 hrs followed by EGF stimulation for 10 mins by ELISA | B | 5.52 | pIC50 | >3000 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of EGFR phosphorylation in human A-431 cells harboring wild type EGFR incubated for 6 hrs by Western blot analysis | B | 5.54 | pIC50 | 2854 | nM | IC50 | Eur J Med Chem (2023) 261: 115840-115840 [PMID:37783102] |
| ChEMBL | Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using polyE4Y1 as substrate incubated for 5 mins with compound followed by substrate addition measured after 60 mins in presence of 1 mM ATP by ADP-Glo reagent based assay | B | 5.76 | pIC50 | 1718 | nM | IC50 | J Med Chem (2023) 66: 14633-14652 [PMID:37885208] |
| ChEMBL | Inhibition of wild type EGFR (unknown origin) in presence of ATP by FRET assay | B | 5.89 | pIC50 | 1302 | nM | IC50 | Eur J Med Chem (2023) 261: 115840-115840 [PMID:37783102] |
| ChEMBL | Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of EGFR-driven cell viability incubated for 72 hrs by CellTiter 96 aqueous one solution assay | B | 6.31 | pIC50 | 489 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of EGFR L858R mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of EGFR-driven cell viability incubated for 72 hrs by CellTiter 96 aqueous one solution assay | B | 6.4 | pIC50 | 397 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of EGFR 746 to 750 deletion/T790M mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of FLT3-driven cell viability incubated for 72 hrs by CellTiter 96 aqueous one solution assay | B | 6.57 | pIC50 | 272 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of wild type EGFR (unknown origin) measured by ELISA | B | 6.58 | pIC50 | 261.3 | nM | IC50 | ACS Med Chem Lett (2022) 13: 196-202 [PMID:35178175] |
| ChEMBL | Inhibition of recombinant wild type EGFR (unknown origin) | B | 6.58 | pIC50 | 261.3 | nM | IC50 | Eur J Med Chem (2023) 245: 114900-114900 [PMID:36417820] |
| ChEMBL | Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) | B | 6.63 | pIC50 | 235 | nM | IC50 | Eur J Med Chem (2023) 261: 115865-115865 [PMID:37839342] |
| ChEMBL | Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in human NCI-H1975 cells assessed as protein phosphorylation measured after 2 hrs by ELISA | B | 6.69 | pIC50 | 203 | nM | IC50 | J Med Chem (2021) 64: 13704-13718 [PMID:34491761] |
| ChEMBL | Inhibition of EGFR phosphorylation in human PC-9 cells harboring Del19/T790M/C797S mutant incubated for 6 hrs by Western blot analysis | B | 6.73 | pIC50 | 188 | nM | IC50 | Eur J Med Chem (2023) 261: 115840-115840 [PMID:37783102] |
| ChEMBL | Inhibition of wild type EGFR (unknown origin) by ELISA | B | 6.85 | pIC50 | 139.7 | nM | IC50 | J Med Chem (2022) 65: 6840-6858 [PMID:35446588] |
| ChEMBL | Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo kinase assay | B | 6.89 | pIC50 | 130 | nM | IC50 | J Nat Prod (2019) 82: 3065-3073 [PMID:31718182] |
| GtoPdb | - | - | 6.89 | pIC50 | 129 | nM | IC50 | Proc Natl Acad Sci USA (2011) 108: 7535-40 [PMID:21502504] |
| ChEMBL | Inhibition of wild type EGFR (unknown origin) | B | 6.91 | pIC50 | 124 | nM | IC50 | J Med Chem (2023) 66: 6849-6868 [PMID:37141440] |
| ChEMBL | Inhibition of wild-type EGFR (unknown origin) using polyE4Y1 as substrate incubated for 5 mins with compound followed by substrate addition measured after 60 mins in presence of ATP by ADP-Glo reagent based assay | B | 6.96 | pIC50 | 109 | nM | IC50 | J Med Chem (2023) 66: 14633-14652 [PMID:37885208] |
| ChEMBL | Inhibition of EGFR 746 to 750 deletion mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of FLT3-driven cell viability incubated for 72 hrs by CellTiter 96 aqueous one solution assay | B | 7.02 | pIC50 | 95 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of wild type EGFR (unknown origin) | B | 7.13 | pIC50 | 74.8 | nM | IC50 | Bioorg Med Chem Lett (2022) 72: 128729-128729 [PMID:35413415] |
| ChEMBL | Inhibition of recombinant EGFR Del19/T790M/C797S mutant (unknown origin) preincubated for 10 mins followed by substrate and ATP addition and measured after 60 mins by ADP-glo based luminescence assay | B | 7.17 | pIC50 | 67.2 | nM | IC50 | Eur J Med Chem (2023) 261: 115865-115865 [PMID:37839342] |
| ChEMBL | Inhibition of human EGFR using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.17 | pIC50 | 67 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of EGFR del19/T790M/C797S triple mutant (unknown origin) in presence of ATP by FRET assay | B | 7.26 | pIC50 | 55.3 | nM | IC50 | Eur J Med Chem (2023) 261: 115840-115840 [PMID:37783102] |
| ChEMBL | Inhibition of EGFR (unknown origin) incubated for 10 mins in presence of ATP by ADP-Glo based luminometer analysis | B | 7.27 | pIC50 | 53.1 | nM | IC50 | Nat Commun (2017) 8: 14768-14768 [PMID:28287083] |
| ChEMBL | Inhibition of wild type EGFR (unknown origin) using TK as substrate incubated for 120 mins in presence of ATP by HTRF assay | B | 7.28 | pIC50 | 53 | nM | IC50 | Bioorg Med Chem (2023) 90: 117338-117338 [PMID:37269687] |
| ChEMBL | Inhibition of wild type EGFR (unknown origin) using TK as substrate incubated for 120 mins in the presence of ATP by HTRF assay | B | 7.28 | pIC50 | 53 | nM | IC50 | Bioorg Med Chem (2022) 70: 116907-116907 [PMID:35810715] |
| ChEMBL | Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) | B | 7.28 | pIC50 | 52.93 | nM | IC50 | Bioorg Med Chem Lett (2024) 101: 129648-129648 [PMID:38331226] |
| ChEMBL | Inhibition of recombinant human EGFR T790M/L858R double mutant using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISA | B | 7.29 | pIC50 | 50.9 | nM | IC50 | ACS Med Chem Lett (2018) 9: 1123-1127 [PMID:30429956] |
| ChEMBL | Inhibition of EGFR Del19/T790M/C797S mutant (unknown origin) | B | 7.36 | pIC50 | 44 | nM | IC50 | Eur J Med Chem (2023) 261: 115865-115865 [PMID:37839342] |
| ChEMBL | Inhibition of recombinant wild type EGFR L858R/T790M/C797S triple mutant (unknown origin) using polyE4Y1 as substrate incubated for 5 mins with compound followed by substrate addition measured after 60 mins in presence of ATP by ADP-Glo reagent based assay | B | 7.42 | pIC50 | 38.3 | nM | IC50 | Eur J Med Chem (2023) 245: 114900-114900 [PMID:36417820] |
| ChEMBL | Inhibition of recombinant human C-terminal His-tagged/N-terminal GST-tagged EGFR (668 to 1210 residues) T790M/L858R/C797S mutant using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISA | B | 7.42 | pIC50 | 38.3 | nM | IC50 | ACS Med Chem Lett (2018) 9: 1123-1127 [PMID:30429956] |
| ChEMBL | Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) measured by ELISA | B | 7.42 | pIC50 | 38.3 | nM | IC50 | ACS Med Chem Lett (2022) 13: 196-202 [PMID:35178175] |
| ChEMBL | Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) | B | 7.42 | pIC50 | 38 | nM | IC50 | J Med Chem (2024) 67: 14702-14722 [PMID:39143914] |
| ChEMBL | Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) by ELISA | B | 7.42 | pIC50 | 37.6 | nM | IC50 | J Med Chem (2022) 65: 6840-6858 [PMID:35446588] |
| ChEMBL | Inhibition of human EGFR L858R/T790M double mutant using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.54 | pIC50 | 29 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of EGFR L858R mutant (unknown origin) | B | 7.55 | pIC50 | 28.3 | nM | IC50 | Bioorg Med Chem Lett (2022) 72: 128729-128729 [PMID:35413415] |
| ChEMBL | Inhibition of Wild type EGFR (unknown origin) | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2021) 64: 13704-13718 [PMID:34491761] |
| ChEMBL | Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) in presence of ATP by FRET assay | B | 7.68 | pIC50 | 20.8 | nM | IC50 | Eur J Med Chem (2023) 261: 115840-115840 [PMID:37783102] |
| ChEMBL | Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using fluoresceine-labelled poly-GT peptide as substrate incubated for 1 hr by TR-FRET assay | B | 7.73 | pIC50 | 18.5 | nM | IC50 | Eur J Med Chem (2021) 225: 113786-113786 [PMID:34464874] |
| ChEMBL | Inhibition of EGFR L858R/T790M mutant (unknown origin) by ELISA | B | 7.76 | pIC50 | 17.2 | nM | IC50 | J Med Chem (2022) 65: 6840-6858 [PMID:35446588] |
| ChEMBL | Inhibition of EGFR L858R mutant (unknown origin) using polyE4Y1 as substrate incubated for 5 mins with compound followed by substrate addition measured after 60 mins in presence of ATP by ADP-Glo reagent based assay | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (2023) 66: 14633-14652 [PMID:37885208] |
| ChEMBL | Inhibition of EGFR L858R mutant (unknown origin) | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2023) 66: 6849-6868 [PMID:37141440] |
| ChEMBL | Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using fluoresceine-labelled poly-GT peptide as substrate preincubated with enzyme for 3 hrs followed by substrate and ATP addition by TR-FRET assay | B | 7.9 | pIC50 | 12.5 | nM | IC50 | Eur J Med Chem (2021) 225: 113786-113786 [PMID:34464874] |
| ChEMBL | Inhibition of EGFR Del19 mutant (unknown origin) | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2023) 66: 6849-6868 [PMID:37141440] |
| ChEMBL | Inhibition of EGFR L858R/C797S mutant (unknown origin) using TK-substrate preincubated with enzyme for 30 mins followed by substrate and ATP addition for 20 mins by HTRF assay | B | 7.96 | pIC50 | 11 | nM | IC50 | ACS Med Chem Lett (2023) 14: 591-598 [PMID:37197473] |
| ChEMBL | Inhibition of EGFR del19 mutant (unknown origin) | B | 7.98 | pIC50 | 10.5 | nM | IC50 | Bioorg Med Chem Lett (2022) 72: 128729-128729 [PMID:35413415] |
| ChEMBL | Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) expressed in Bac-to-Bac baculovirus expression system measured after 2 hrs by ELISA method | B | 8.1 | pIC50 | 8 | nM | IC50 | Eur J Med Chem (2022) 244: 114856-114856 [PMID:36279692] |
| ChEMBL | Inhibition of EGFR C797S/T790M/Del19 mutant (unknown origin) | B | 8.12 | pIC50 | 7.63 | nM | IC50 | Eur J Med Chem (2024) 275: 116590-116590 [PMID:38908104] |
| ChEMBL | Inhibition of EGFR 19 del/T790M/C797S mutant (unknown origin) by ELISA | B | 8.18 | pIC50 | 6.6 | nM | IC50 | J Med Chem (2022) 65: 6840-6858 [PMID:35446588] |
| ChEMBL | Inhibition of EGFR C797S/T790M/L858R mutant (unknown origin) | B | 8.23 | pIC50 | 5.95 | nM | IC50 | Eur J Med Chem (2024) 275: 116590-116590 [PMID:38908104] |
| ChEMBL | Inhibition of EGFR C797S/T790M/L858R mutant (unknown origin) incubated for 10 mins in presence of ATP by ADP-Glo based luminometer analysis | B | 8.25 | pIC50 | 5.57 | nM | IC50 | Nat Commun (2017) 8: 14768-14768 [PMID:28287083] |
| ChEMBL | Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using polyE4Y1 as substrate incubated for 5 mins with compound followed by substrate addition measured after 60 mins in presence of ATP by ADP-Glo reagent based assay | B | 8.27 | pIC50 | 5.4 | nM | IC50 | J Med Chem (2023) 66: 14633-14652 [PMID:37885208] |
| ChEMBL | Inhibition of EGFR L858R/T790M double mutant (unknown origin) using polyE4Y1 as substrate incubated for 5 mins with compound followed by substrate addition measured after 60 mins in presence of ATP by ADP-Glo reagent based assay | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2023) 66: 14633-14652 [PMID:37885208] |
| ChEMBL | Inhibition of EGFR dTCb mutant (unknown origin) | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2023) 66: 6849-6868 [PMID:37141440] |
| ChEMBL | Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) | B | 8.31 | pIC50 | 4.9 | nM | IC50 | Bioorg Med Chem Lett (2022) 72: 128729-128729 [PMID:35413415] |
| ChEMBL | Inhibition of EGFR LTb mutant (unknown origin) | B | 8.35 | pIC50 | 4.5 | nM | IC50 | J Med Chem (2023) 66: 6849-6868 [PMID:37141440] |
| ChEMBL | Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) preincubated for 10 mins followed by ATP and substrate addition and measured after 60 mins by plate reader analysis | B | 8.36 | pIC50 | 4.4 | nM | IC50 | J Med Chem (2023) 66: 6849-6868 [PMID:37141440] |
| ChEMBL | Inhibition of EGFR LTCb mutant (unknown origin) | B | 8.36 | pIC50 | 4.4 | nM | IC50 | J Med Chem (2023) 66: 6849-6868 [PMID:37141440] |
| ChEMBL | Inhibition of EGFR Del19/T790M/C797S triple mutant (unknown origin) using polyE4Y1 as substrate incubated for 5 mins with compound followed by substrate addition measured after 60 mins in presence of ATP by ADP-Glo reagent based assay | B | 8.36 | pIC50 | 4.4 | nM | IC50 | J Med Chem (2023) 66: 14633-14652 [PMID:37885208] |
| ChEMBL | Inhibition of EGFR del19/T790M/C797S mutant (unknown origin) | B | 8.41 | pIC50 | 3.9 | nM | IC50 | Bioorg Med Chem Lett (2022) 72: 128729-128729 [PMID:35413415] |
| ChEMBL | Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using TK as substrate incubated for 120 mins in presence of ATP by HTRF assay | B | 8.47 | pIC50 | 3.38 | nM | IC50 | Bioorg Med Chem (2023) 90: 117338-117338 [PMID:37269687] |
| ChEMBL | Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using TK as substrate incubated for 120 mins in the presence of ATP by HTRF assay | B | 8.47 | pIC50 | 3.38 | nM | IC50 | Bioorg Med Chem (2022) 70: 116907-116907 [PMID:35810715] |
| ChEMBL | Inhibition of human C-terminal His-tagged and N-terminal GST-tagged EGFR L858R/T790M/C797S triple mutant ( 668 to 1210 amino acids) expressed in baculovirus infected Sf9 insect cells using Poly(Glu,Tyr) 4:1 as substrate after 60 mins by ELISA | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2019) 62: 7302-7308 [PMID:31298540] |
| ChEMBL | Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) by ELISA | B | 8.6 | pIC50 | 2.5 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127327-127327 [PMID:32631532] |
| ChEMBL | Kinase Inhibitory Activity Assay: The inhibitory activity on a C797S-containing epidermal growth factor receptor (EGFR) kinase and an MET kinase was measured for compound 1 obtained in the above Example, and the results are shown in Table 1 below. The kinase inhibitory activity was measured by the following method:1. Each kinase was incubated with 8 mM MOPS (pH 7.0), 0.2 mM EDTA, 250 μM KKKGQEEEYVFIE (SEQ ID NO: 1), 1 mM sodium orthovanadate, 5 mM sodium-6-glycerophosphate, 10 mM magnesium acetate, and [η-33P]-ATP.2. The compound to be evaluated (DMSO solution) and Mg/ATP were added to proceed the reaction.3. After about 40 minutes at room temperature, the reaction was stopped by the addition of 10 μL of 0.5% phosphoric acid.4. 10 μL of 0.5% reaction solution was spotted onto a P30 filtermat.5. Washed 4 times for about 4 minutes in 0.425% phosphoric acid. Washed once in methanol, and then dried and analyzed by scintillation counting to measure IC50 value. | B | 8.7 | pIC50 | 2 | nM | IC50 | US-11248003-B2. Pyrimidine derivative having effect of inhibiting cancer cell growth and pharmaceutical composition containing same (2022) |
| ChEMBL | Inhibition of wild type EGFR (unknown origin) using TK-substrate preincubated with enzyme for 30 mins followed by substrate and ATP addition for 25 mins by HTRF assay | B | 8.8 | pIC50 | 1.6 | nM | IC50 | ACS Med Chem Lett (2023) 14: 591-598 [PMID:37197473] |
| ChEMBL | Inhibition of human EGFR L858R mutant using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of EGFR 19D/T790M/C797S mutant (unknown origin) by ELISA | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127327-127327 [PMID:32631532] |
| ChEMBL | Inhibition of EGFR L858R/T790M mutant (unknown origin) by ELISA | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127327-127327 [PMID:32631532] |
| ChEMBL | Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) using TK-substrate preincubated with enzyme for 30 mins followed by substrate and ATP addition for 10 mins by HTRF assay | B | 8.89 | pIC50 | 1.3 | nM | IC50 | ACS Med Chem Lett (2023) 14: 591-598 [PMID:37197473] |
| ChEMBL | Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M/C797S mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo kinase assay | B | 9 | pIC50 | 1 | nM | IC50 | J Nat Prod (2019) 82: 3065-3073 [PMID:31718182] |
| ChEMBL | Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo kinase assay | B | 9 | pIC50 | 1 | nM | IC50 | J Nat Prod (2019) 82: 3065-3073 [PMID:31718182] |
| ChEMBL | Inhibition of EGFR Del19/T790M/C797S triple mutant (unknown origin) using TK as substrate incubated for 120 mins in presence of ATP by HTRF assay | B | 9.09 | pIC50 | 0.82 | nM | IC50 | Bioorg Med Chem (2023) 90: 117338-117338 [PMID:37269687] |
| ChEMBL | Inhibition of EGFR del18/T790M/C797S triple mutant (unknown origin) using TK as substrate incubated for 120 mins in the presence of ATP by HTRF assay | B | 9.09 | pIC50 | 0.82 | nM | IC50 | Bioorg Med Chem (2022) 70: 116907-116907 [PMID:35810715] |
| ChEMBL | Inhibition of EGFR del19/T790M mutant (unknown origin) | B | 9.15 | pIC50 | 0.7 | nM | IC50 | Bioorg Med Chem Lett (2022) 72: 128729-128729 [PMID:35413415] |
| 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 human FGFR1 using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.89 | pIC50 | 128 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of human FGFR1 V561M mutant using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.39 | pIC50 | 41 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802] | ||||||||
| ChEMBL | Inhibition of human FGFR2 using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.64 | pIC50 | 228 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of human FGFR2 N549H using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.69 | pIC50 | 203 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607] | ||||||||
| ChEMBL | Inhibition of human FGFR3 using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.45 | pIC50 | 358 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455] | ||||||||
| ChEMBL | Inhibition of human FGFR4 using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.74 | pIC50 | 181 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397] | ||||||||
| ChEMBL | Inhibition of human FAK using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 8.41 | pIC50 | 3.9 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581] | ||||||||
| ChEMBL | Inhibition of human MET using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6 | pIC50 | >1000 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Kinase Inhibitory Activity Assay: The inhibitory activity on a C797S-containing epidermal growth factor receptor (EGFR) kinase and an MET kinase was measured for compound 1 obtained in the above Example, and the results are shown in Table 1 below. The kinase inhibitory activity was measured by the following method:1. Each kinase was incubated with 8 mM MOPS (pH 7.0), 0.2 mM EDTA, 250 μM KKKGQEEEYVFIE (SEQ ID NO: 1), 1 mM sodium orthovanadate, 5 mM sodium-6-glycerophosphate, 10 mM magnesium acetate, and [η-33P]-ATP.2. The compound to be evaluated (DMSO solution) and Mg/ATP were added to proceed the reaction.3. After about 40 minutes at room temperature, the reaction was stopped by the addition of 10 μL of 0.5% phosphoric acid.4. 10 μL of 0.5% reaction solution was spotted onto a P30 filtermat.5. Washed 4 times for about 4 minutes in 0.425% phosphoric acid. Washed once in methanol, and then dried and analyzed by scintillation counting to measure IC50 value. | B | 7.15 | pIC50 | 70 | nM | IC50 | US-11248003-B2. Pyrimidine derivative having effect of inhibiting cancer cell growth and pharmaceutical composition containing same (2022) |
| Insulin-like growth factor I receptor/Insulin-like growth factor 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069] | ||||||||
| ChEMBL | Inhibition of IGF-1R phosphorylation in IGF-1 stimulated human HepG2 cells preincubated with compound for 30 mins followed by IGF-1 stimulation for 10 mins by Immunoblot analysis | B | 6.83 | pIC50 | 148 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of human IGF1R using KKKSPGEYVNIEFG as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.14 | pIC50 | 73 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of human IGF1R using KKKSPGEYVNIEFG as substrate and [gamma-33P]ATP measured after 1 hr | B | 7.6 | pIC50 | 24.9 | nM | IC50 | J Med Chem (2016) 59: 4948-4964 [PMID:27144831] |
| GtoPdb | - | - | 7.61 | pIC50 | 24.6 | nM | IC50 | J Med Chem (2016) 59: 4948-64 [PMID:27144831] |
| Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
| ChEMBL | Inhibition of INSR phosphorylation in insulin-stimulated human H4-II-E cells preincubated with compound for 30 mins followed by insulin stimulation and measured after 10 mins by immunoblot analysis | B | 5.03 | pIC50 | 9331 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of human InsR using myelin basic protein as substrate and [gamma-33P]ATP measured after 1 hr | B | 6.71 | pIC50 | 196 | nM | IC50 | J Med Chem (2016) 59: 4948-4964 [PMID:27144831] |
| GtoPdb | - | - | 6.71 | pIC50 | 196 | nM | IC50 | J Med Chem (2016) 59: 4948-64 [PMID:27144831] |
| ChEMBL | Inhibition of human INSR using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.8 | pIC50 | 160 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| Insulin receptor-related receptor/Insulin receptor-related protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5483] [GtoPdb: 1802] [UniProtKB: P14616] | ||||||||
| ChEMBL | Inhibition of human INSRR using MBP as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.35 | pIC50 | 45 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| leucine rich repeat kinase 2/Leucine-rich repeat serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075104] [GtoPdb: 2059] [UniProtKB: Q5S007] | ||||||||
| ChEMBL | Inhibition of human LRRK2 using RLGRDKYKTLRQIRQ as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.29 | pIC50 | 51 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| leukocyte receptor tyrosine kinase/Leukocyte tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5627] [GtoPdb: 1838] [UniProtKB: P29376] | ||||||||
| ChEMBL | Inhibition of human LTK using EAIYAAPFAKKK as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.85 | pIC50 | 14 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| colony stimulating factor 1 receptor/Macrophage colony-stimulating factor 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333] | ||||||||
| ChEMBL | Inhibition of human FMS using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.45 | pIC50 | 358 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5] | ||||||||
| ChEMBL | Inhibition of human MNK1 T385D mutant using MBP as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.06 | pIC50 | 88 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| microtubule affinity regulating kinase 3/MAP/microtubule affinity-regulating kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5600] [GtoPdb: 2099] [UniProtKB: P27448] | ||||||||
| ChEMBL | Inhibition of human MARK3 using KKKVSRSGLYRSPSMPENLNRPR as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.9 | pIC50 | 127 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| KIT proto-oncogene, receptor tyrosine kinase/Mast/stem cell growth factor receptor Kit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721] | ||||||||
| ChEMBL | Inhibition of human KIT V560G mutant using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.71 | pIC50 | 195 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of human KIT D816H mutant using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.95 | pIC50 | 111 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of human KIT D816V mutant using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.08 | pIC50 | 83 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680] | ||||||||
| ChEMBL | Inhibition of human MELK using KKLNRTLSFAEPG as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.05 | pIC50 | 895 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| mitogen-activated protein kinase kinase kinase 9/Mitogen-activated protein kinase kinase kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2872] [GtoPdb: 2084] [UniProtKB: P80192] | ||||||||
| ChEMBL | Inhibition of human MAP3K9 using casein as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.66 | pIC50 | 218 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| NUAK family kinase 1/NUAK family SNF1-like kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5784] [GtoPdb: 2129] [UniProtKB: O60285] | ||||||||
| ChEMBL | Inhibition of NUAK1 (unknown origin) | B | 7.33 | pIC50 | 47 | nM | IC50 | J Med Chem (2021) 64: 2-25 [PMID:33356242] |
| ChEMBL | Inhibition of human NUAK1 using KKKVSRSGLYRSPSMPENLNRPR as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.33 | pIC50 | 47 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| phosphorylase kinase catalytic subunit gamma 2/Phosphorylase b kinase gamma catalytic chain, liver/testis isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2349] [GtoPdb: 2147] [UniProtKB: P15735] | ||||||||
| ChEMBL | Inhibition of human PHKg2 using KKLNRTLSFAEPG as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.97 | pIC50 | 108 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| protein tyrosine kinase 2 beta/Protein-tyrosine kinase 2-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5469] [GtoPdb: 2181] [UniProtKB: Q14289] | ||||||||
| ChEMBL | Inhibition of human PTK2B using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.62 | pIC50 | 24 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| protein tyrosine kinase 6/Protein-tyrosine kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4601] [GtoPdb: 2182] [UniProtKB: Q13882] | ||||||||
| ChEMBL | Inhibition of human PTK6 using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 8.39 | pIC50 | 4.1 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ret proto-oncogene/Proto-oncogene tyrosine-protein kinase receptor Ret in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] | ||||||||
| ChEMBL | Inhibition of human RET using RRRRRRRRRRRVYSTDYYRLFNPS as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.19 | pIC50 | 65 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of human RET V804L mutant using RRRRRRRRRRRVYSTDYYRLFNPS as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.57 | pIC50 | 27 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of human RET V804M mutant using RRRRRRRRRRRVYSTDYYRLFNPS as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.66 | pIC50 | 22 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| c-ros oncogene 1, receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase ROS in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5568] [GtoPdb: 1840] [UniProtKB: P08922] | ||||||||
| ChEMBL | Inhibition of human ROS1 using KKKSPGEYVNIEFG as substrate and [gamma-33P]ATP measured after 1 hr | B | 8.72 | pIC50 | 1.9 | nM | IC50 | J Med Chem (2016) 59: 4948-4964 [PMID:27144831] |
| ChEMBL | Inhibition of human ROS1 using KKKSPGEYVNIEFG as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 8.72 | pIC50 | 1.9 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| SRC proto-oncogene, non-receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase Src in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931] | ||||||||
| ChEMBL | Inhibition of human SRC T341M mutant using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.8 | pIC50 | 160 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| ChEMBL | Inhibition of FLT3-ITD F691I mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of FLT3-driven cell viability incubated for 72 hrs by CellTiter 96 aqueous one solution assay | B | 5.94 | pIC50 | 1155 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of FLT3-ITD F691L mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of FLT3-driven cell viability incubated for 72 hrs by CellTiter 96 aqueous one solution assay | B | 6.58 | pIC50 | 263 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of FLT3-ITD D835Y mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of FLT3-driven cell viability incubated for 72 hrs by CellTiter 96 aqueous one solution assay | B | 6.68 | pIC50 | 211 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of FLT3-ITD mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of FLT3-driven cell viability incubated for 72 hrs by CellTiter 96 aqueous one solution assay | B | 6.8 | pIC50 | 158 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of human FLT3 using EAIYAAPFAKKK as substrate and [gamma-33P]ATP measured after 1 hr | B | 8.68 | pIC50 | 2.1 | nM | IC50 | J Med Chem (2016) 59: 4948-4964 [PMID:27144831] |
| ChEMBL | Inhibition of human FLT3 using EAIYAAPFAKKK as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 8.68 | pIC50 | 2.1 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of human FLT3 D835Y mutant using EAIYAAPFAKKK as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| erb-b2 receptor tyrosine kinase 2/Receptor tyrosine-protein kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626] | ||||||||
| ChEMBL | Inhibition of human ERBB2 using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.38 | pIC50 | 42 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| erb-b2 receptor tyrosine kinase 4/Receptor tyrosine-protein kinase erbB-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3009] [GtoPdb: 1799] [UniProtKB: Q15303] | ||||||||
| ChEMBL | Inhibition of human ERBB4 using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.57 | pIC50 | 27 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418] | ||||||||
| ChEMBL | Inhibition of human RPS6KA1 using KKLNRTLSVA as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.52 | pIC50 | 30 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ribosomal protein S6 kinase A2/Ribosomal protein S6 kinase alpha-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3906] [GtoPdb: 1529] [UniProtKB: Q15349] | ||||||||
| ChEMBL | Inhibition of human RPS6kA2 using KKLNRTLSVA as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.89 | pIC50 | 13 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812] | ||||||||
| ChEMBL | Inhibition of human RPS6kA3 using KKLNRTLSVA as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.59 | pIC50 | 26 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ribosomal protein S6 kinase A6/Ribosomal protein S6 kinase alpha-6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4924] [GtoPdb: 1530] [UniProtKB: Q9UK32] | ||||||||
| ChEMBL | Inhibition of human RPS6KA6 using KKLNRTLSVA as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.38 | pIC50 | 42 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| serine/threonine kinase 10/Serine/threonine-protein kinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3981] [GtoPdb: 2211] [UniProtKB: O94804] | ||||||||
| ChEMBL | Inhibition of human STK10 using RLGRDKYKTLRQIRQ as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.91 | pIC50 | 123 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| serine/threonine kinase 4/Serine/threonine-protein kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4598] [GtoPdb: 2225] [UniProtKB: Q13043] | ||||||||
| ChEMBL | Inhibition of human STK4 using KKSRGDYMTMQIG as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6 | pIC50 | >1000 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| BR serine/threonine kinase 1/Serine/threonine-protein kinase BRSK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5650] [GtoPdb: 1946] [UniProtKB: Q8TDC3] | ||||||||
| ChEMBL | Inhibition of human BRSK1 using KKKVSRSGLYRSPSMPENLNRPR as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.47 | pIC50 | 338 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| BR serine/threonine kinase 2/Serine/threonine-protein kinase BRSK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4574] [GtoPdb: 1947] [UniProtKB: Q8IWQ3] | ||||||||
| ChEMBL | Inhibition of human BRSK2 using KKLNRTLSFAEPG as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.9 | pIC50 | 125 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757] | ||||||||
| ChEMBL | Inhibition of human CHEK1 using KKKVSRSGLYRSPSMPENLNRPR as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.52 | pIC50 | 30 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| checkpoint kinase 2/Serine/threonine-protein kinase Chk2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2527] [GtoPdb: 1988] [UniProtKB: O96017] | ||||||||
| ChEMBL | Inhibition of human CHEK2 using KKKVSRSGLYRSPSMPENLNRPR as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 8.19 | pIC50 | 6.5 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of human CHEK2 I157T mutant using KKKVSRSGLYRSPSMPENLNRPR as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 8.25 | pIC50 | 5.6 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| protein kinase D1/Serine/threonine-protein kinase D1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3863] [GtoPdb: 1489] [UniProtKB: Q15139] | ||||||||
| ChEMBL | Inhibition of human PRKD1 using KKLNRTLSVA as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.71 | pIC50 | 197 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| protein kinase D2/Serine/threonine-protein kinase D2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4900] [GtoPdb: 2173] [UniProtKB: Q9BZL6] | ||||||||
| ChEMBL | Inhibition of human PRKD2 using KKLNRTLSVA as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.55 | pIC50 | 285 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| protein kinase D3/Serine/threonine-protein kinase D3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2595] [GtoPdb: 2174] [UniProtKB: O94806] | ||||||||
| ChEMBL | Inhibition of human PRKD3 using KKLNRTLSVA as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.02 | pIC50 | 95 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| microtubule affinity regulating kinase 1/Serine/threonine-protein kinase MARK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5940] [GtoPdb: 2097] [UniProtKB: Q9P0L2] | ||||||||
| ChEMBL | Inhibition of human MARK1 using KKKVSRSGLYRSPSMPENLNRPR as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.9 | pIC50 | 127 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| microtubule affinity regulating kinase 2/Serine/threonine-protein kinase MARK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3831] [GtoPdb: 2098] [UniProtKB: Q7KZI7] | ||||||||
| ChEMBL | Inhibition of human Par-1Balpha using KKKVSRSGLYRSPSMPENLNRPR as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.03 | pIC50 | 93 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| NIMA related kinase 9/Serine/threonine-protein kinase Nek9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5257] [GtoPdb: 2124] [UniProtKB: Q8TD19] | ||||||||
| ChEMBL | Inhibition of human NEK9 using MBP as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6 | pIC50 | >1000 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350] | ||||||||
| ChEMBL | Inhibition of human PLK1 using casein as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.21 | pIC50 | 611 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| salt inducible kinase 2/Serine/threonine-protein kinase SIK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5699] [GtoPdb: 2198] [UniProtKB: Q9H0K1] | ||||||||
| ChEMBL | Inhibition of human SIK2 using AMARAASAAALARRR as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.33 | pIC50 | 466 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| TAO kinase 1/Serine/threonine-protein kinase TAO1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5261] [GtoPdb: 2233] [UniProtKB: Q7L7X3] | ||||||||
| ChEMBL | Inhibition of human TAOK1 using MBP as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.31 | pIC50 | 493 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| testis specific serine kinase 1B/Testis-specific serine/threonine-protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6003] [GtoPdb: 2257] [UniProtKB: Q9BXA7] | ||||||||
| ChEMBL | Inhibition of human TSSK1 using KKKVSRSGLYRSPSMPENLNRPR as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 8.36 | pIC50 | 4.4 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| testis specific serine kinase 2/Testis-specific serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6014] [GtoPdb: 2258] [UniProtKB: Q96PF2] | ||||||||
| ChEMBL | Inhibition of human TSSK2 using KKKVSRSGLYRSPSMPENLNRPR as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.86 | pIC50 | 138 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519] | ||||||||
| ChEMBL | Inhibition of human ABL1 using EAIYAAPFAKKK as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.3 | pIC50 | 500 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of human ABL1 T315I mutant using EAIYAAPFAKKK as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.62 | pIC50 | 242 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| ChEMBL | Inhibition of human ABL1 Q252H mutant using EAIYAAPFAKKK as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.77 | pIC50 | 171 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| BLK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Blk in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2250] [GtoPdb: 1940] [UniProtKB: P51451] | ||||||||
| ChEMBL | Inhibition of human BLK using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.87 | pIC50 | 136 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187] | ||||||||
| ChEMBL | Inhibition of human BTK using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.17 | pIC50 | 674 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| C-terminal Src kinase/Tyrosine-protein kinase CSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2634] [GtoPdb: 1994] [UniProtKB: P41240] | ||||||||
| ChEMBL | Inhibition of human CSK using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.48 | pIC50 | 329 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| FER tyrosine kinase/Tyrosine-protein kinase Fer in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3982] [GtoPdb: 2022] [UniProtKB: P16591] | ||||||||
| ChEMBL | Inhibition of human FER using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 8.89 | pIC50 | 1.3 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| FES proto-oncogene, tyrosine kinase/Tyrosine-protein kinase Fes/Fps in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5455] [GtoPdb: 2023] [UniProtKB: P07332] | ||||||||
| ChEMBL | Inhibition of human FES using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 8.46 | pIC50 | 3.5 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| FGR proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fgr in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4454] [GtoPdb: 2024] [UniProtKB: P09769] | ||||||||
| ChEMBL | Inhibition of human FGR using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.31 | pIC50 | 492 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| fyn related Src family tyrosine kinase/Tyrosine-protein kinase FRK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4223] [GtoPdb: 2025] [UniProtKB: P42685] | ||||||||
| ChEMBL | Inhibition of human FRK using RLGRDKYKTLRQIRQ as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.28 | pIC50 | 52 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241] | ||||||||
| ChEMBL | Inhibition of human FYN using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.7 | pIC50 | 198 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631] | ||||||||
| ChEMBL | Inhibition of human HCK using KVEKIGEGTYGVVYK as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.7 | pIC50 | 198 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
| ChEMBL | Inhibition of human JAK2 using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.81 | pIC50 | 154 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lck in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239] | ||||||||
| ChEMBL | Inhibition of human LCK using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.29 | pIC50 | 512 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948] | ||||||||
| ChEMBL | Inhibition of human LYN using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.62 | pIC50 | 241 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| MER proto-oncogene, tyrosine kinase/Tyrosine-protein kinase Mer in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866] | ||||||||
| ChEMBL | Inhibition of human MERTK using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6 | pIC50 | >1000 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| YES proto-oncogene 1, Src family tyrosine kinase/Tyrosine-protein kinase Yes in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073] [GtoPdb: 2284] [UniProtKB: P07947] | ||||||||
| ChEMBL | Inhibition of human YES1 using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.72 | pIC50 | 19 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
| ChEMBL | Inhibition of human VEGFR2 using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 6.09 | pIC50 | 816 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
| fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916] | ||||||||
| ChEMBL | Inhibition of human FLT4 using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay | B | 7.24 | pIC50 | 58 | nM | IC50 | Clin Cancer Res (2016) 22: 5527-5538 [PMID:27780853] |
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]
