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 34:

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]