compound 2c [PMID: 24900538] [Ligand Id: 8138] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2151321
  • ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
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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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  • protein tyrosine kinase 2/Focal adhesion kinase 1 in Human [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
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  • mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
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  • mitogen-activated protein kinase kinase kinase 9/Mitogen-activated protein kinase kinase kinase 9 in Human [ChEMBL: CHEMBL2872] [GtoPdb: 2084] [UniProtKB: P80192]
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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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  • neurotrophic receptor tyrosine kinase 2/Neurotrophic tyrosine kinase receptor type 2 in Human [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620]
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  • phosphorylase kinase catalytic subunit gamma 2/Phosphorylase kinase gamma subunit 2 in Human [ChEMBL: CHEMBL2349] [GtoPdb: 2147] [UniProtKB: P15735]
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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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  • WNK lysine deficient protein kinase 3/Serine/threonine-protein kinase WNK3 in Human [ChEMBL: CHEMBL6055] [GtoPdb: 2282] [UniProtKB: Q9BYP7]
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  • testis specific serine kinase 2/Testis-specific serine/threonine-protein kinase 2 in Human [ChEMBL: CHEMBL6014] [GtoPdb: 2258] [UniProtKB: Q96PF2]
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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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  • Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
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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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  • IL2 inducible T cell kinase/Tyrosine-protein kinase ITK/TSK in Human [ChEMBL: CHEMBL2959] [GtoPdb: 2046] [UniProtKB: Q08881]
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  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
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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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  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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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 ALK B 7.47 pIC50 34.1 nM IC50 ACS Med Chem Lett (2012) 3: 705-709 [PMID:24900538]
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
GtoPdb - - 8.06 pIC50 8.7 nM IC50 ACS Med Chem Lett (2012) 3: 705-9 [PMID:24900538]
ChEMBL Inhibition of FGFR1 B 8.06 pIC50 8.7 nM IC50 ACS Med Chem Lett (2012) 3: 705-709 [PMID:24900538]
protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
ChEMBL Inhibition of FAK B 7.76 pIC50 17.2 nM IC50 ACS Med Chem Lett (2012) 3: 705-709 [PMID:24900538]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG B 4.49 pIC50 >32000 nM IC50 ACS Med Chem Lett (2012) 3: 705-709 [PMID:24900538]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL Inhibition of SAPK2a B 7.87 pIC50 13.4 nM IC50 ACS Med Chem Lett (2012) 3: 705-709 [PMID:24900538]
mitogen-activated protein kinase kinase kinase 9/Mitogen-activated protein kinase kinase kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2872] [GtoPdb: 2084] [UniProtKB: P80192]
ChEMBL Inhibition of MLK1 B 7.35 pIC50 44.3 nM IC50 ACS Med Chem Lett (2012) 3: 705-709 [PMID:24900538]
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 MuSk B 7 pIC50 <100 nM IC50 ACS Med Chem Lett (2012) 3: 705-709 [PMID:24900538]
neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
ChEMBL Amplified Luminescent Proximity Assay: To measure JAK2 kinase activity, a commercially available purified enzyme may be used. The enzyme may be a C-terminal His6-tagged, recombinant, human JAK2, amino acids 808-end, (Genbank Accession number NM 004972) expressed by baculovirus in Sf21 cells (Upstate Biotechnology MA). After incubation of the kinase with a biotinylated substrate and adenosine triphosphate (ATP) for 60 minutes at room temperature, the kinase reaction may be stopped by the addition of 30 mM ethylenediaminetetraacetic acid (EDTA). The reaction may be performed in 384 well microtitre plates and the reaction products may be detected with the addition of streptavidin coated Donor Beads and phosphotyrosine-specific antibodies coated Acceptor Beads using the EnVision Multilabel Plate Reader after an overnight incubation at room temperature. B 8.52 pIC50 3 nM IC50 US-8486966-B2. 9-(pyrazol-3-yl)-9H-purine-2-amine and 3-(pyrazol-3-yl) -3H-imidazo[4,5-B] pyridin-5-amine derivatives and their use for the treatment of cancer (2013)
GtoPdb - - 8.85 pIC50 1.4 nM IC50 ACS Med Chem Lett (2012) 3: 705-9 [PMID:24900538]
ChEMBL Inhibition of TrkA B 8.85 pIC50 1.4 nM IC50 ACS Med Chem Lett (2012) 3: 705-709 [PMID:24900538]
neurotrophic receptor tyrosine kinase 2/Neurotrophic tyrosine kinase receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620]
ChEMBL Inhibition of TrkB B 7 pIC50 <100 nM IC50 ACS Med Chem Lett (2012) 3: 705-709 [PMID:24900538]
phosphorylase kinase catalytic subunit gamma 2/Phosphorylase kinase gamma subunit 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2349] [GtoPdb: 2147] [UniProtKB: P15735]
GtoPdb - - 8.21 pIC50 6.1 nM IC50 ACS Med Chem Lett (2012) 3: 705-9 [PMID:24900538]
ChEMBL Inhibition of PhKg2 B 8.21 pIC50 6.1 nM IC50 ACS Med Chem Lett (2012) 3: 705-709 [PMID:24900538]
salt inducible kinase 1/Serine/threonine-protein kinase SIK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6082] [GtoPdb: 2197] [UniProtKB: P57059]
ChEMBL Inhibition of SIK B 8.26 pIC50 5.5 nM IC50 ACS Med Chem Lett (2012) 3: 705-709 [PMID:24900538]
GtoPdb - - 8.26 pIC50 5.5 nM IC50 ACS Med Chem Lett (2012) 3: 705-9 [PMID:24900538]
WNK lysine deficient protein kinase 3/Serine/threonine-protein kinase WNK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6055] [GtoPdb: 2282] [UniProtKB: Q9BYP7]
GtoPdb - - 7 pIC50 99.8 nM IC50 ACS Med Chem Lett (2012) 3: 705-9 [PMID:24900538]
ChEMBL Inhibition of WNK3 B 7 pIC50 99.8 nM IC50 ACS Med Chem Lett (2012) 3: 705-709 [PMID:24900538]
testis specific serine kinase 2/Testis-specific serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6014] [GtoPdb: 2258] [UniProtKB: Q96PF2]
GtoPdb - - 7.51 pIC50 30.6 nM IC50 ACS Med Chem Lett (2012) 3: 705-9 [PMID:24900538]
ChEMBL Inhibition of TSSK2 B 7.51 pIC50 30.6 nM IC50 ACS Med Chem Lett (2012) 3: 705-709 [PMID:24900538]
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
GtoPdb - - 8.92 pIC50 1.2 nM IC50 ACS Med Chem Lett (2012) 3: 705-9 [PMID:24900538]
ChEMBL Inhibition of Abl B 8.92 pIC50 1.2 nM IC50 ACS Med Chem Lett (2012) 3: 705-709 [PMID:24900538]
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
ChEMBL Inhibition of BTK B 8.46 pIC50 3.5 nM IC50 ACS Med Chem Lett (2012) 3: 705-709 [PMID:24900538]
GtoPdb - - 8.46 pIC50 3.5 nM IC50 ACS Med Chem Lett (2012) 3: 705-9 [PMID:24900538]
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 Fgr B 8.66 pIC50 2.2 nM IC50 ACS Med Chem Lett (2012) 3: 705-709 [PMID:24900538]
GtoPdb - - 8.66 pIC50 2.2 nM IC50 ACS Med Chem Lett (2012) 3: 705-9 [PMID:24900538]
IL2 inducible T cell kinase/Tyrosine-protein kinase ITK/TSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2959] [GtoPdb: 2046] [UniProtKB: Q08881]
ChEMBL Inhibition of Itk B 7.14 pIC50 72.2 nM IC50 ACS Med Chem Lett (2012) 3: 705-709 [PMID:24900538]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL Inhibition of JAK2 B 7.17 pIC50 68.3 nM IC50 ACS Med Chem Lett (2012) 3: 705-709 [PMID:24900538]
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 Lck B 7 pIC50 <100 nM IC50 ACS Med Chem Lett (2012) 3: 705-709 [PMID:24900538]
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 Flt3 B 8.68 pIC50 2.1 nM IC50 ACS Med Chem Lett (2012) 3: 705-709 [PMID:24900538]
GtoPdb - - 8.68 pIC50 2.1 nM IC50 ACS Med Chem Lett (2012) 3: 705-9 [PMID:24900538]
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL Inhibition of Ret B 7 pIC50 <100 nM IC50 ACS Med Chem Lett (2012) 3: 705-709 [PMID:24900538]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Inhibition of cSrc B 7.74 pIC50 18.2 nM IC50 ACS Med Chem Lett (2012) 3: 705-709 [PMID:24900538]
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 FLT4 B 7.19 pIC50 64 nM IC50 ACS Med Chem Lett (2012) 3: 705-709 [PMID:24900538]

ChEMBL data shown on this page come from version 32:

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]