compound 1d [PMID: 21493067] [Ligand Id: 8123] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1774056
Created with Highcharts 10.3.3ValuesChart context menuCyclin-dependent kinase 2/cyclin E1pKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
  • EPH receptor B2/Ephrin type-B receptor 2 in Human [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323]
Created with Highcharts 10.3.3ValuesChart context menuEphrin type-B receptor 2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
Created with Highcharts 10.3.3ValuesChart context menuEpidermal growth factor receptor erbB1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607]
Created with Highcharts 10.3.3ValuesChart context menuFibroblast growth factor receptor 3pKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuInsulin receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • muscle associated receptor tyrosine kinase/Muscle, skeletal receptor tyrosine protein kinase in Human [ChEMBL: CHEMBL5684] [GtoPdb: 1847] [UniProtKB: O15146]
Created with Highcharts 10.3.3ValuesChart context menuMuscle, skeletal receptor tyrosine protein kinasepKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
  • neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
Created with Highcharts 10.3.3ValuesChart context menuNerve growth factor receptor Trk-ApKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • protein tyrosine kinase 2 beta/Protein tyrosine kinase 2 beta in Human [ChEMBL: CHEMBL5469] [GtoPdb: 2181] [UniProtKB: Q14289]
Created with Highcharts 10.3.3ValuesChart context menuProtein tyrosine kinase 2 betapKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
Created with Highcharts 10.3.3ValuesChart context menuTyrosine-protein kinase JAK2pKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
Created with Highcharts 10.3.3ValuesChart context menuTyrosine-protein kinase JAK3pKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
Created with Highcharts 10.3.3ValuesChart context menuTyrosine-protein kinase LCKpKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
Created with Highcharts 10.3.3ValuesChart context menuTyrosine-protein kinase receptor FLT3pKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
  • ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
Created with Highcharts 10.3.3ValuesChart context menuTyrosine-protein kinase receptor RETpKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864, P24941]
ChEMBL Inhibition of human CDK2/cyclinE B 6.76 pIC50 174 nM IC50 Bioorg Med Chem Lett (2011) 21: 2958-2961 [PMID:21493067]
EPH receptor B2/Ephrin type-B receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323]
ChEMBL Inhibition of human EphB2 B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2958-2961 [PMID:21493067]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of human EGFR B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2958-2961 [PMID:21493067]
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 B 6.94 pIC50 115 nM IC50 Bioorg Med Chem Lett (2011) 21: 2958-2961 [PMID:21493067]
GtoPdb - - 6.94 pIC50 115 nM IC50 Bioorg Med Chem Lett (2011) 21: 2958-61 [PMID:21493067]
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
ChEMBL Inhibition of human InsR B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2011) 21: 2958-2961 [PMID:21493067]
muscle associated receptor tyrosine kinase/Muscle, skeletal receptor tyrosine protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5684] [GtoPdb: 1847] [UniProtKB: O15146]
ChEMBL Inhibition of human MuSk B 6.65 pIC50 224 nM IC50 Bioorg Med Chem Lett (2011) 21: 2958-2961 [PMID:21493067]
GtoPdb - - 6.65 pIC50 224 nM IC50 Bioorg Med Chem Lett (2011) 21: 2958-61 [PMID:21493067]
neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
GtoPdb - - 8.52 pIC50 3 nM IC50 Bioorg Med Chem Lett (2011) 21: 2958-61 [PMID:21493067]
ChEMBL Inhibition of human TRKA B 8.52 pIC50 3 nM IC50 Bioorg Med Chem Lett (2011) 21: 2958-2961 [PMID:21493067]
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 Pyk2 B 6.89 pIC50 129 nM IC50 Bioorg Med Chem Lett (2011) 21: 2958-2961 [PMID:21493067]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL Inhibition of JAK2 after 60 min B 8.52 pIC50 <3 nM IC50 Bioorg Med Chem Lett (2011) 21: 2958-2961 [PMID:21493067]
GtoPdb - - 9 pIC50 <1 nM IC50 Bioorg Med Chem Lett (2011) 21: 2958-61 [PMID:21493067]
ChEMBL Inhibition of human JAK2 B 9 pIC50 <1 nM IC50 Bioorg Med Chem Lett (2011) 21: 2958-2961 [PMID:21493067]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
GtoPdb - - 7.82 pIC50 15 nM IC50 Bioorg Med Chem Lett (2011) 21: 2958-61 [PMID:21493067]
ChEMBL Inhibition of human JAK3 B 7.82 pIC50 15 nM IC50 Bioorg Med Chem Lett (2011) 21: 2958-2961 [PMID:21493067]
ChEMBL Inhibition of JAK3 after 60 min B 8.15 pIC50 7 nM IC50 Bioorg Med Chem Lett (2011) 21: 2958-2961 [PMID:21493067]
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 B 6.67 pIC50 215 nM IC50 Bioorg Med Chem Lett (2011) 21: 2958-2961 [PMID:21493067]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Inhibition of human FLT3 D835Y mutant B 7.09 pIC50 82 nM IC50 Bioorg Med Chem Lett (2011) 21: 2958-2961 [PMID:21493067]
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
GtoPdb - - 7.72 pIC50 19 nM IC50 Bioorg Med Chem Lett (2011) 21: 2958-61 [PMID:21493067]
ChEMBL Inhibition of human RET B 7.72 pIC50 19 nM IC50 Bioorg Med Chem Lett (2011) 21: 2958-2961 [PMID:21493067]

ChEMBL data shown on this page come from version 35:

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]