compound 19a [PMID: 24359159] [Ligand Id: 6977] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3116050
  • ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
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  • casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II alpha in Human [ChEMBL: CHEMBL3629] [GtoPdb: 1549] [UniProtKB: P68400]
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  • casein kinase 2, alpha prime polypeptide subunit/Casein kinase II alpha (prime) in Human [ChEMBL: CHEMBL4070] [GtoPdb: 1550] [UniProtKB: P19784]
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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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  • neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
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  • tyrosine kinase 2/Non-receptor tyrosine-protein kinase TYK2 in Mouse [ChEMBL: CHEMBL2321619] [GtoPdb: 2269] [UniProtKB: Q9R117]
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  • protein kinase C zeta/Protein kinase C zeta in Human [ChEMBL: CHEMBL3438] [GtoPdb: 1491] [UniProtKB: Q05513]
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  • aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
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  • salt inducible kinase 1/Serine/threonine-protein kinase SIK1 in Human [ChEMBL: CHEMBL6082] [GtoPdb: 2197] [UniProtKB: P57059]
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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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  • FGR proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FGR in Human [ChEMBL: CHEMBL4454] [GtoPdb: 2024] [UniProtKB: P09769]
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  • Janus kinase 1/Tyrosine-protein kinase JAK1 in Human [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
  • Janus kinase 1/Tyrosine-protein kinase JAK1 in Mouse [ChEMBL: CHEMBL2968] [GtoPdb: 2047] [UniProtKB: P52332]
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  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Mouse [ChEMBL: CHEMBL1649049] [GtoPdb: 2048] [UniProtKB: Q62120]
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  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Mouse [ChEMBL: CHEMBL5250] [GtoPdb: 2049] [UniProtKB: Q62137]
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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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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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  • fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
ChEMBL Inhibition of human ALK B 7.3 pIC50 50 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3629] [GtoPdb: 1549] [UniProtKB: P68400]
ChEMBL Inhibition of human recombinant 6 X His-tagged full length CK2alpha expressed in insect sf21 cells using CK2tide as substrate after 20 mins by fluorescence assay B 4.52 pIC50 >30000 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
casein kinase 2, alpha prime polypeptide subunit/Casein kinase II alpha (prime) in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4070] [GtoPdb: 1550] [UniProtKB: P19784]
ChEMBL Inhibition of human CK2alpha2 B 8.57 pIC50 2.7 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
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 B 7.3 pIC50 50 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
LIM domain kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3836] [GtoPdb: 2054] [UniProtKB: P53667]
ChEMBL Inhibition of human LIMK1 B 7.2 pIC50 63 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
ChEMBL Inhibition of human TrkA B 7.46 pIC50 35 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
tyrosine kinase 2/Non-receptor tyrosine-protein kinase TYK2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321619] [GtoPdb: 2269] [UniProtKB: Q9R117]
ChEMBL Inhibition of Tyk2 in mouse BA/F3 cells expressing TEL-Tyk2 assessed as inhibition of STAT5 phosphorylation by Western blotting analysis B 6.62 pIC50 240 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
protein kinase C zeta/Protein kinase C zeta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3438] [GtoPdb: 1491] [UniProtKB: Q05513]
ChEMBL Inhibition of human PKCzeta B 6.7 pIC50 200 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL Inhibition of human aurora A kinase B 7.24 pIC50 58 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
salt inducible kinase 1/Serine/threonine-protein kinase SIK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6082] [GtoPdb: 2197] [UniProtKB: P57059]
ChEMBL Inhibition of human SIK B 6.72 pIC50 190 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
ChEMBL Inhibition of human Abl B 7.6 pIC50 25 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
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 B 7.48 pIC50 33 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
GtoPdb - - 8.52 pIC50 <3 nM IC50 J Med Chem (2014) 57: 144-58 [PMID:24359159]
ChEMBL Inhibition of Jak1 (unknown origin) B 8.52 pIC50 <3 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
ChEMBL Inhibition of human JAK2 B 8.7 pIC50 <2 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
Janus kinase 1/Tyrosine-protein kinase JAK1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2968] [GtoPdb: 2047] [UniProtKB: P52332]
ChEMBL Inhibition of Jak1 in mouse BA/F3 cells expressing TEL-Jak1 assessed as inhibition of STAT5 phosphorylation by Western blotting analysis B 6.59 pIC50 260 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL Inhibition of Jak2 V617F mutant in human SET2 cells assessed as inhibition of STAT5 phosphorylation after 24 hrs by Western blotting analysis B 7.27 pIC50 54 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
ChEMBL Inhibition of Jak2 V617F mutant in human SET2 cells assessed as inhibition of STAT5 phosphorylation after 1 hr by Western blotting analysis B 7.52 pIC50 30 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
ChEMBL Inhibition of Jak2 V617F mutant in human UKE1 cells assessed as inhibition of STAT5 phosphorylation after 24 hrs by Western blotting analysis B 8.3 pIC50 5 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
GtoPdb - - 8.52 pIC50 <3 nM IC50 J Med Chem (2014) 57: 144-58 [PMID:24359159]
ChEMBL Inhibition of Jak2 (unknown origin) B 8.52 pIC50 <3 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
ChEMBL Inhibition of Jak2 V617F mutant in human UKE1 cells assessed as inhibition of STAT5 phosphorylation after 1 hr by Western blotting analysis B 8.7 pIC50 2 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1649049] [GtoPdb: 2048] [UniProtKB: Q62120]
ChEMBL Inhibition of Jak2 in mouse BA/F3 cells expressing TEL-Jak2 assessed as inhibition of STAT5 phosphorylation by Western blotting analysis B 7.92 pIC50 12 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
ChEMBL Inhibition of Jak3 (unknown origin) B 6.66 pIC50 220 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
GtoPdb - - 6.66 pIC50 220 nM IC50 J Med Chem (2014) 57: 144-58 [PMID:24359159]
ChEMBL Inhibition of human JAK3 B 7.46 pIC50 35 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5250] [GtoPdb: 2049] [UniProtKB: Q62137]
ChEMBL Inhibition of Jak3 in mouse BA/F3 cells expressing TEL-Jak3 assessed as inhibition of STAT5 phosphorylation by Western blotting analysis B 5.7 pIC50 2000 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
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 B 7.35 pIC50 45 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL Inhibition of human Ret B 7.34 pIC50 46 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
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 KDR B 7.66 pIC50 22 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]
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 B 7.4 pIC50 40 nM IC50 J Med Chem (2014) 57: 144-158 [PMID:24359159]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]