allitinib [Ligand Id: 9912] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1947204 (ALL-3, Allitinib, Als 1306, Ast 1306, Ast-1306, Ast1306)
  • TEK receptor tyrosine kinase/Angiopoietin-1 receptor in Human [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
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  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • EPH receptor A2/Ephrin type-A receptor 2 in Human [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317]
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  • EPH receptor B2/Ephrin type-B receptor 2 in Human [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323]
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  • epidermal growth factor receptor/Epidermal growth factor receptor in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
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  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
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  • MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
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  • Insulin-like growth factor I receptor/Insulin-like growth factor 1 receptor in Human [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
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  • macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912]
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  • KIT proto-oncogene, receptor tyrosine kinase/Mast/stem cell growth factor receptor Kit in Human [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
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  • platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
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  • platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
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  • protein kinase C beta/Protein kinase C beta type in Human [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
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  • SRC proto-oncogene, non-receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase Src in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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  • AKT serine/threonine kinase 1/RAC-alpha serine/threonine-protein kinase in Human [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
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  • erb-b2 receptor tyrosine kinase 2/Receptor tyrosine-protein kinase erbB-2 in Human [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
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  • erb-b2 receptor tyrosine kinase 4/Receptor tyrosine-protein kinase erbB-4 in Human [ChEMBL: CHEMBL3009] [GtoPdb: 1799] [UniProtKB: Q15303]
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  • ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase beta-1 in Human [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443]
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  • Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-2 in Human [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9]
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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL1 in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
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  • spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405]
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  • fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
TEK receptor tyrosine kinase/Angiopoietin-1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
ChEMBL Inhibition of N-terminal GST-tagged recombinant human Tie2 (771 to end residues) cytoplasmic domain expressed in baculovirus infected sf21 insect cells using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 5 pIC50 >10000 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
aurora kinase A/Aurora kinase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL Inhibition of N-terminal GST-tagged recombinant human full length AURA expressed in baculovirus infected sf21 insect cells using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 5 pIC50 >10000 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibition of recombinant human full length CDK2 expressed in baculovirus infected sf21 insect cells using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 5 pIC50 >10000 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
EPH receptor A2/Ephrin type-A receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317]
ChEMBL Inhibition of EphA2 (unknown origin) expressed in Bac-to-Bac baculovirus expression system using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 5 pIC50 >10000 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
EPH receptor B2/Ephrin type-B receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323]
ChEMBL Inhibition of EphB2 (unknown origin) expressed in Bac-to-Bac baculovirus expression system using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 5 pIC50 >10000 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
epidermal growth factor receptor/Epidermal growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of EGFR T790M/L858R double mutant (unknown origin) using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 7.92 pIC50 12 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
GtoPdb - - 9.3 pIC50 0.5 nM IC50 PLoS ONE (2011) 6: e21487 [PMID:21789172]
ChEMBL Inhibition of EGFR (unknown origin) expressed in Bac-to-Bac baculovirus expression system using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 9.3 pIC50 0.5 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
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 FGFR1 (unknown origin) expressed in Bac-to-Bac baculovirus expression system using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 5 pIC50 >10000 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
ChEMBL Inhibition of N-terminal GST-tagged recombinant human full length GSK3b expressed in baculovirus infected sf21 insect cells using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 5 pIC50 >10000 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
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 c-Met (unknown origin) expressed in Bac-to-Bac baculovirus expression system using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 5 pIC50 >10000 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
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 IGF1R (unknown origin) expressed in Bac-to-Bac baculovirus expression system using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 5 pIC50 >10000 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912]
ChEMBL Inhibition of RON (unknown origin) expressed in Bac-to-Bac baculovirus expression system using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 5 pIC50 >10000 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
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 c-Kit (unknown origin) expressed in Bac-to-Bac baculovirus expression system using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 5 pIC50 >10000 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
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 PDGFRalpha (unknown origin) expressed in Bac-to-Bac baculovirus expression system using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 5 pIC50 >10000 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
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) using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 5 pIC50 >10000 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
protein kinase C beta/Protein kinase C beta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771]
ChEMBL Inhibition of N-terminal GST-tagged recombinant human full length PKCb2 expressed in baculovirus infected sf21 insect cells using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 5 pIC50 >10000 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
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 c-Src (unknown origin) expressed in Bac-to-Bac baculovirus expression system using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 5 pIC50 >10000 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
AKT serine/threonine kinase 1/RAC-alpha serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
ChEMBL Inhibition of N-terminal GST-tagged recombinant human AKT1 (104 to end residues) catalytic domain expressed in baculovirus infected sf21 insect cells using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 5 pIC50 >10000 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
erb-b2 receptor tyrosine kinase 2/Receptor tyrosine-protein kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
GtoPdb - - 8.52 pIC50 3 nM IC50 PLoS ONE (2011) 6: e21487 [PMID:21789172]
ChEMBL Inhibition of ErbB2 (unknown origin) expressed in Bac-to-Bac baculovirus expression system using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 8.52 pIC50 3 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
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 ErbB4 (unknown origin) using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 9.1 pIC50 0.8 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
GtoPdb - - 9.1 pIC50 0.8 nM IC50 PLoS ONE (2011) 6: e21487 [PMID:21789172]
ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase beta-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443]
ChEMBL Inhibition of N-terminal GST-tagged recombinant human p70S6K1 (1 to 421 residues) catalytic domain expressed in baculovirus infected sf21 insect cells co-expressing N-terminal GST-tagged PDK1 using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 5 pIC50 >10000 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9]
ChEMBL Inhibition of N-terminal GST-tagged recombinant human full length PIM2 expressed in baculovirus infected sf21 insect cells using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 5 pIC50 >10000 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
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 c-Abl (unknown origin) using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 5 pIC50 >10000 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL Inhibition of N-terminal His-tagged recombinant human JAK2 (826 to end residues) catalytic domain expressed in baculovirus infected sf21 insect cells using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 5 pIC50 >10000 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405]
ChEMBL Inhibition of N-terminal GST-tagged recombinant human full length SYK expressed in baculovirus infected sf21 insect cells using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 5 pIC50 >10000 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
ChEMBL Inhibition of Flt-1 (unknown origin) using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 5 pIC50 >10000 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]
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 KDR (unknown origin) expressed in Bac-to-Bac baculovirus expression system using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISA B 5 pIC50 >10000 nM IC50 PLoS One (2011) 6: 21487-21487 [PMID:21789172]

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]