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

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ChEMBL ligand: CHEMBL1774056
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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 erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607]
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  • muscle associated receptor tyrosine kinase/Muscle, skeletal receptor tyrosine protein kinase in Human [ChEMBL: CHEMBL5684] [GtoPdb: 1847] [UniProtKB: O15146]
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  • neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
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  • protein tyrosine kinase 2 beta/Protein tyrosine kinase 2 beta in Human [ChEMBL: CHEMBL5469] [GtoPdb: 2181] [UniProtKB: Q14289]
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  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
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  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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  • ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
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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: P24864P24941]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]