Detailed information for compound 1715632

Basic information

Technical information
  • Name: Unnamed compound
  • MW: 393.446 | Formula: C19H23N9O
  • H donors: 4 H acceptors: 5 LogP: 2.2 Rotable bonds: 6
    Rule of 5 violations (Lipinski): 1
  • SMILES: N[C@H]1CCCC[C@H]1Nc1ncc(c(n1)Nc1cccc(c1)n1nccn1)C(=O)N
  • InChi: 1S/C19H23N9O/c20-15-6-1-2-7-16(15)26-19-22-11-14(17(21)29)18(27-19)25-12-4-3-5-13(10-12)28-23-8-9-24-28/h3-5,8-11,15-16H,1-2,6-7,20H2,(H2,21,29)(H2,22,25,26,27)/t15-,16+/m0/s1
  • InChiKey: TXGKRVFSSHPBAJ-JKSUJKDBSA-N  

Network

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Synonyms

No synonyms found for this compound

Targets

Known targets for this compound

Species Target name Source Bibliographic reference
Homo sapiens zeta-chain (TCR) associated protein kinase 70kDa Starlite/ChEMBL References
Homo sapiens FGR proto-oncogene, Src family tyrosine kinase Starlite/ChEMBL No references
Homo sapiens spleen tyrosine kinase Starlite/ChEMBL References
Homo sapiens fms-related tyrosine kinase 3 Starlite/ChEMBL No references
Homo sapiens protein kinase C, alpha Starlite/ChEMBL References
Homo sapiens mitogen-activated protein kinase kinase kinase 9 Starlite/ChEMBL No references
Homo sapiens p21 protein (Cdc42/Rac)-activated kinase 7 Starlite/ChEMBL No references
Homo sapiens LYN proto-oncogene, Src family tyrosine kinase Starlite/ChEMBL References
Homo sapiens SRC proto-oncogene, non-receptor tyrosine kinase Starlite/ChEMBL No references
Homo sapiens YES proto-oncogene 1, Src family tyrosine kinase Starlite/ChEMBL No references
Homo sapiens LCK proto-oncogene, Src family tyrosine kinase Starlite/ChEMBL No references
Homo sapiens potassium voltage-gated channel, subfamily H (eag-related), member 2 Starlite/ChEMBL References
Homo sapiens Janus kinase 2 Starlite/ChEMBL References

Predicted pathogen targets for this compound

By orthology
Species Potential target Known druggable target/s Ortholog Group
Loa Loa (eye worm) hypothetical protein Get druggable targets OG5_129482 All targets in OG5_129482
Echinococcus granulosus 3'partial|tyrosine protein kinase Fgr Get druggable targets OG5_127750 All targets in OG5_127750
Loa Loa (eye worm) SRC-1 Get druggable targets OG5_127750 All targets in OG5_127750
Echinococcus multilocularis mitogen activated protein kinase kinase kinase Get druggable targets OG5_128497 All targets in OG5_128497
Echinococcus granulosus serine:threonine protein kinase PAK 4 Get druggable targets OG5_131977 All targets in OG5_131977
Echinococcus granulosus tyrosine protein kinase Blk Get druggable targets OG5_127750 All targets in OG5_127750
Schistosoma japonicum IPR000477,RNA-directed DNA polymerase (Reverse transcriptase),domain-containing Get druggable targets OG5_129482 All targets in OG5_129482
Echinococcus granulosus tyrosine protein kinase Fyn Get druggable targets OG5_127750 All targets in OG5_127750
Echinococcus granulosus potassium voltage gated channel subfamily H Get druggable targets OG5_128858 All targets in OG5_128858
Schistosoma japonicum Protein kinase C gamma type, putative Get druggable targets OG5_129482 All targets in OG5_129482
Echinococcus granulosus tyrosine protein kinase Src64B Get druggable targets OG5_127750 All targets in OG5_127750
Echinococcus multilocularis proto oncogene tyrosine protein kinase LCK Get druggable targets OG5_127750 All targets in OG5_127750
Schistosoma japonicum ko:K04910 potassium voltage-gated channel, Eag-related subfamily H, member 7, putative Get druggable targets OG5_128858 All targets in OG5_128858
Echinococcus granulosus mitogen-activated protein kinase kinase kinase 9 Get druggable targets OG5_128497 All targets in OG5_128497
Echinococcus multilocularis Protein kinase C, brain isozyme Get druggable targets OG5_129482 All targets in OG5_129482
Echinococcus multilocularis serine threonine protein kinase Get druggable targets OG5_129482 All targets in OG5_129482
Echinococcus multilocularis tyrosine protein kinase Srms Get druggable targets OG5_127750 All targets in OG5_127750
Loa Loa (eye worm) AGC/PKC/ALPHA protein kinase Get druggable targets OG5_129482 All targets in OG5_129482
Schistosoma japonicum ko:K05703 proto-oncogene tyrosine-protein kinase Fyn, putative Get druggable targets OG5_127750 All targets in OG5_127750
Echinococcus multilocularis tyrosine protein kinase Src42A Get druggable targets OG5_127750 All targets in OG5_127750
Schistosoma japonicum ko:K04910 potassium voltage-gated channel, Eag-related subfamily H, member 7, putative Get druggable targets OG5_128858 All targets in OG5_128858
Echinococcus multilocularis tyrosine protein kinase Src64B Get druggable targets OG5_127750 All targets in OG5_127750
Loa Loa (eye worm) hypothetical protein Get druggable targets OG5_129482 All targets in OG5_129482
Schistosoma mansoni serine/threonine protein kinase Get druggable targets OG5_129482 All targets in OG5_129482
Trichomonas vaginalis voltage and ligand gated potassium channel, putative Get druggable targets OG5_128858 All targets in OG5_128858
Echinococcus granulosus tyrosine protein kinase Fyn Get druggable targets OG5_127750 All targets in OG5_127750
Schistosoma japonicum Calcium-dependent protein kinase C, putative Get druggable targets OG5_129482 All targets in OG5_129482
Echinococcus multilocularis telomerase reverse transcriptase subunit Get druggable targets OG5_129482 All targets in OG5_129482
Echinococcus multilocularis tyrosine protein kinase Fyn Get druggable targets OG5_127750 All targets in OG5_127750
Echinococcus granulosus RNA directed DNA polymerase Get druggable targets OG5_129482 All targets in OG5_129482
Schistosoma mansoni serine/threonine protein kinase Get druggable targets OG5_129482 All targets in OG5_129482
Echinococcus granulosus tyrosine protein kinase Src42A Get druggable targets OG5_127750 All targets in OG5_127750
Schistosoma mansoni tyrosine kinase Get druggable targets OG5_131855 All targets in OG5_131855
Echinococcus multilocularis potassium voltage gated channel subfamily H Get druggable targets OG5_128858 All targets in OG5_128858
Schistosoma japonicum Potassium voltage-gated channel subfamily H member 2, putative Get druggable targets OG5_128858 All targets in OG5_128858
Echinococcus multilocularis tyrosine protein kinase Fyn Get druggable targets OG5_127750 All targets in OG5_127750
Schistosoma japonicum Proto-oncogene tyrosine-protein kinase FGR, putative Get druggable targets OG5_127750 All targets in OG5_127750
Schistosoma japonicum Proto-oncogene tyrosine-protein kinase Yrk, putative Get druggable targets OG5_127750 All targets in OG5_127750
Schistosoma japonicum ko:K05855 spleen tyrosine kinase, putative Get druggable targets OG5_131855 All targets in OG5_131855
Schistosoma japonicum Proto-oncogene tyrosine-protein kinase FYN, putative Get druggable targets OG5_127750 All targets in OG5_127750
Schistosoma mansoni voltage-gated potassium channel Get druggable targets OG5_128858 All targets in OG5_128858
Echinococcus granulosus tyrosine protein kinase Src42A Get druggable targets OG5_127750 All targets in OG5_127750
Echinococcus multilocularis serine:threonine protein kinase PAK 4 Get druggable targets OG5_131977 All targets in OG5_131977
Loa Loa (eye worm) STE/STE20/PAKB protein kinase Get druggable targets OG5_131977 All targets in OG5_131977
Echinococcus multilocularis tyrosine protein kinase lyn tyrosine protein kinase blk Get druggable targets OG5_127750 All targets in OG5_127750
Echinococcus multilocularis RNA directed DNA polymerase Get druggable targets OG5_129482 All targets in OG5_129482
Echinococcus granulosus tyrosine protein kinase shark Get druggable targets OG5_131855 All targets in OG5_131855
Schistosoma japonicum ko:K08253 non-specific protein-tyrosine kinase [EC2.7.10.2], putative Get druggable targets OG5_131855 All targets in OG5_131855
Schistosoma japonicum Protein kinase C alpha type, putative Get druggable targets OG5_129482 All targets in OG5_129482
Echinococcus multilocularis tyrosine protein kinase shark Get druggable targets OG5_131855 All targets in OG5_131855
Schistosoma japonicum ko:K08892 fyn-related kinase, putative Get druggable targets OG5_127750 All targets in OG5_127750
Entamoeba histolytica protein kinase, putative Get druggable targets OG5_127750 All targets in OG5_127750
Echinococcus granulosus tyrosine kinase Get druggable targets OG5_127750 All targets in OG5_127750
Echinococcus multilocularis tyrosine protein kinase HCK Get druggable targets OG5_127750 All targets in OG5_127750
Schistosoma japonicum Protein kinase C alpha type, putative Get druggable targets OG5_129482 All targets in OG5_129482
Schistosoma mansoni tyrosine kinase Get druggable targets OG5_127750 All targets in OG5_127750
Trichomonas vaginalis voltage and ligand gated potassium channel, putative Get druggable targets OG5_128858 All targets in OG5_128858
Loa Loa (eye worm) voltage and ligand gated potassium channel Get druggable targets OG5_128858 All targets in OG5_128858
Schistosoma mansoni voltage-gated potassium channel Get druggable targets OG5_128858 All targets in OG5_128858
Echinococcus multilocularis tyrosine protein kinase Fgr Get druggable targets OG5_127750 All targets in OG5_127750
Schistosoma mansoni tyrosine kinase Get druggable targets OG5_127750 All targets in OG5_127750
Candida albicans protein kinase C similar to S. cerevisiae PKC1 (YBL105C) Get druggable targets OG5_129482 All targets in OG5_129482
Echinococcus multilocularis tyrosine protein kinase Fyn Get druggable targets OG5_127750 All targets in OG5_127750
Echinococcus multilocularis tyrosine protein kinase lyn lyn a protein tyrosine kinase lymphocyte specific protein tyrosine kinase Get druggable targets OG5_127750 All targets in OG5_127750
Loa Loa (eye worm) TK protein kinase Get druggable targets OG5_127750 All targets in OG5_127750
Echinococcus multilocularis tyrosine protein kinase Blk Get druggable targets OG5_127750 All targets in OG5_127750
Echinococcus granulosus tyrosine protein kinase Lyn Get druggable targets OG5_127750 All targets in OG5_127750
Schistosoma japonicum Proto-oncogene tyrosine-protein kinase FYN, putative Get druggable targets OG5_127750 All targets in OG5_127750
Echinococcus granulosus protein kinase C gamma type Get druggable targets OG5_129482 All targets in OG5_129482
Brugia malayi protein-tyrosine kinase Get druggable targets OG5_127750 All targets in OG5_127750
Candida albicans protein kinase C similar to S. cerevisiae PKC1 (YBL105C) Get druggable targets OG5_129482 All targets in OG5_129482
Echinococcus granulosus tyrosine protein kinase HCK Get druggable targets OG5_127750 All targets in OG5_127750
Schistosoma mansoni tyrosine kinase Get druggable targets OG5_131855 All targets in OG5_131855
Brugia malayi Protein kinase c protein 2 Get druggable targets OG5_129482 All targets in OG5_129482
Schistosoma mansoni serine/threonine protein kinase Get druggable targets OG5_128497 All targets in OG5_128497
Loa Loa (eye worm) hypothetical protein Get druggable targets OG5_128858 All targets in OG5_128858
Brugia malayi Voltage-gated potassium channel, HERG (KCNH2)-related. C. elegans unc-103 ortholog Get druggable targets OG5_128858 All targets in OG5_128858
Echinococcus granulosus tyrosine protein kinase Fyn Get druggable targets OG5_127750 All targets in OG5_127750
Brugia malayi serine/threonine-protein kinase PAK 7 Get druggable targets OG5_131977 All targets in OG5_131977
Brugia malayi SRC-1 Get druggable targets OG5_127750 All targets in OG5_127750
Echinococcus granulosus Protein kinase C brain isozyme Get druggable targets OG5_129482 All targets in OG5_129482
Echinococcus granulosus tyrosine kinase|tyrosine protein kinase Fyn Get druggable targets OG5_127750 All targets in OG5_127750
Loa Loa (eye worm) TK protein kinase Get druggable targets OG5_127750 All targets in OG5_127750
Echinococcus multilocularis tyrosine protein kinase Src42A Get druggable targets OG5_127750 All targets in OG5_127750
Echinococcus granulosus proto oncogene tyrosine protein kinase LCK Get druggable targets OG5_127750 All targets in OG5_127750
Echinococcus multilocularis tyrosine protein kinase Fyn Get druggable targets OG5_127750 All targets in OG5_127750

By sequence similarity to non orthologous known druggable targets
No druggable targets predicted by sequence similarity

Obtained from network model

Ranking Plot


Putative Targets List


Species Potential target Raw Global Species
Schistosoma mansoni run and tbc1 domain containing 0.0022 0.0069 0.0069
Brugia malayi STAT protein, DNA binding domain containing protein 0.0041 0.0411 0.1095
Loa Loa (eye worm) thyroid receptor interactor 0.0022 0.0069 0.017
Echinococcus multilocularis endophilin A3 0.0022 0.0069 0.0069
Echinococcus granulosus c src tyrosine kinase 0.0076 0.1055 0.1055
Trichomonas vaginalis conserved hypothetical protein 0.0022 0.0069 0.1461
Entamoeba histolytica unconventional myosin IB 0.0022 0.0069 0.0333
Schistosoma mansoni cell polarity protein 0.0022 0.0069 0.0069
Echinococcus granulosus tyrosine protein kinase HCK 0.0119 0.1831 0.1831
Entamoeba histolytica protein kinase, putative 0.0042 0.0429 0.2304
Brugia malayi Protein kinase domain containing protein 0.0054 0.0651 0.1746
Echinococcus multilocularis growth factor receptor bound protein 2 0.0063 0.0815 0.0815
Brugia malayi SH2 domain containing protein 0.0041 0.0411 0.1095
Trichomonas vaginalis conserved hypothetical protein 0.0022 0.0069 0.1461
Echinococcus multilocularis basement membrane specific heparan sulfate 0.0019 0.0007 0.0007
Brugia malayi SH2 domain containing protein 0.0054 0.0651 0.1746
Trypanosoma brucei conserved protein 0.0022 0.0069 0.5
Echinococcus multilocularis PAK box P21 Rho binding 0.0019 0.0009 0.0009
Schistosoma mansoni tensin 0.0041 0.0411 0.0411
Echinococcus multilocularis breast cancer anti estrogen resistance protein 0.0022 0.0069 0.0069
Entamoeba histolytica hypothetical protein, conserved 0.0022 0.0069 0.0333
Echinococcus multilocularis hematopoietic lineage cell specific protein 0.0022 0.0069 0.0069
Echinococcus granulosus phosphatidylinositol 3 kinase regulatory subunit 0.0041 0.0411 0.0411
Schistosoma mansoni hypothetical protein 0.0019 0.0009 0.0009
Schistosoma mansoni sh3-containing grb2-like protein 1 (endophilin II) 0.0022 0.0069 0.0069
Echinococcus granulosus tyrosine kinase 0.016 0.2577 0.2577
Schistosoma mansoni Dab2-interacting protein-like 0.0022 0.0069 0.0069
Giardia lamblia Kinase, STE STE20 0.002 0.0026 0.5
Onchocerca volvulus 0.0054 0.0651 1
Onchocerca volvulus 0.0041 0.0411 0.587
Loa Loa (eye worm) hypothetical protein 0.0022 0.0069 0.017
Echinococcus multilocularis protein kinase c epsilon type 0.002 0.0028 0.0028
Loa Loa (eye worm) p53BP2 0.0022 0.0069 0.017
Loa Loa (eye worm) STE/STE20/PAKB protein kinase 0.0221 0.3699 1
Echinococcus multilocularis raf serine:threonine protein kinase 0.002 0.0039 0.0039
Echinococcus multilocularis tensin 0.0041 0.0411 0.0411
Echinococcus multilocularis slit robo rho gtpase activating protein 1 0.0022 0.0069 0.0069
Echinococcus granulosus protein kinase c epsilon type 0.002 0.0028 0.0028
Schistosoma mansoni hypothetical protein 0.0041 0.0411 0.0411
Trichomonas vaginalis STE family protein kinase 0.002 0.0026 0.0424
Echinococcus granulosus twitchin 0.002 0.0024 0.0024
Schistosoma mansoni sorting nexin 0.0022 0.0069 0.0069
Echinococcus multilocularis proto oncogene tyrosine protein kinase LCK 0.0182 0.2981 0.2981
Echinococcus granulosus neurotracting:lsamp:neurotrimin:obcam 0.0019 0.0007 0.0007
Trichomonas vaginalis p67phox protein, putative 0.0022 0.0069 0.1461
Entamoeba histolytica protein kinase, putative 0.0119 0.1831 1
Echinococcus granulosus tyrosine kinase 0.0054 0.0651 0.0651
Brugia malayi Tyrosine-protein kinase abl-1 0.0076 0.1055 0.2841
Echinococcus multilocularis tyrosine protein kinase Fyn 0.0182 0.2981 0.2981
Loa Loa (eye worm) TK/FER protein kinase 0.0054 0.0651 0.1746
Loa Loa (eye worm) P21-Rho-binding domain-containing protein 0.0019 0.0009 0.0005
Echinococcus multilocularis tyrosine protein kinase lyn tyrosine protein kinase blk 0.0182 0.2981 0.2981
Brugia malayi Src substrate cortactin 0.0022 0.0069 0.017
Brugia malayi Variant SH3 domain containing protein 0.0022 0.0069 0.017
Echinococcus multilocularis N chimaerin 0.0048 0.0544 0.0544
Loa Loa (eye worm) variant SH3 domain-containing protein 0.0063 0.0815 0.2189
Schistosoma mansoni shc transforming protein 0.0041 0.0411 0.0411
Loa Loa (eye worm) TK/FER protein kinase 0.0054 0.0651 0.1746
Schistosoma mansoni serine/threonine protein kinase 0.002 0.0039 0.0039
Echinococcus multilocularis serine:threonine protein kinase PAK 3 0.002 0.0026 0.0026
Echinococcus granulosus serine:threonine protein kinase PAK 3 0.002 0.0026 0.0026
Schistosoma mansoni protein kinase 0.0019 0.0009 0.0009
Echinococcus multilocularis suppressor of cytokine signaling 7 0.0041 0.0411 0.0411
Brugia malayi cytokine inducible SH2-containing protein 5 0.0041 0.0411 0.1095
Echinococcus granulosus neural Wiskott Aldrich syndrome protein 0.0019 0.0009 0.0009
Echinococcus multilocularis Immunoglobulin 0.0019 0.0007 0.0007
Schistosoma mansoni SH2A 0.0041 0.0411 0.0411
Schistosoma mansoni signal transduction protein lnk-related 0.0041 0.0411 0.0411
Brugia malayi Myosin tail family protein 0.0022 0.0069 0.017
Schistosoma mansoni hypothetical protein 0.0019 0.0009 0.0009
Loa Loa (eye worm) SH2 domain-containing protein 0.0041 0.0411 0.1095
Echinococcus multilocularis SH2 motif 0.0041 0.0411 0.0411
Brugia malayi RhoGAP domain containing protein 0.0048 0.0544 0.1456
Echinococcus multilocularis transfer RNA-Ala 0.0022 0.0069 0.0069
Onchocerca volvulus 0.0041 0.0411 0.587
Loa Loa (eye worm) SH2 domain-containing protein 0.0041 0.0411 0.1095
Echinococcus granulosus rho guanine nucleotide exchange factor 7 0.0022 0.0069 0.0069
Schistosoma mansoni voltage-gated potassium channel 0.0049 0.0552 0.0552
Loa Loa (eye worm) TK/FER protein kinase 0.0054 0.0651 0.1746
Echinococcus granulosus tyrosine protein phosphatase non receptor type 0.0041 0.0411 0.0411
Echinococcus multilocularis potassium voltage gated channel subfamily H 0.0045 0.0477 0.0477
Loa Loa (eye worm) variant SH3 domain-containing protein 0.0042 0.0439 0.117
Entamoeba histolytica protein kinase, putative 0.002 0.0026 0.0097
Echinococcus multilocularis tyrosine protein kinase lyn lyn a protein tyrosine kinase lymphocyte specific protein tyrosine kinase 0.0182 0.2981 0.2981
Echinococcus multilocularis phosphatidylinositol 3 kinase regulatory subunit 0.0041 0.0411 0.0411
Loa Loa (eye worm) hypothetical protein 0.0022 0.0069 0.017
Echinococcus granulosus roundabout 2 0.0019 0.0007 0.0007
Brugia malayi Variant SH3 domain containing protein 0.0048 0.0544 0.1456
Schistosoma mansoni formin binding protein and related proteins 0.0022 0.0069 0.0069
Echinococcus granulosus fch and double sh3 domains protein 2 0.0022 0.0069 0.0069
Loa Loa (eye worm) TK/FER protein kinase 0.0054 0.0651 0.1746
Onchocerca volvulus 0.0041 0.0411 0.587
Loa Loa (eye worm) hypothetical protein 0.0041 0.0411 0.1095
Schistosoma mansoni growth factor receptor-bound protein 0.0066 0.0873 0.0873
Loa Loa (eye worm) hypothetical protein 0.0041 0.0411 0.1095
Brugia malayi Variant SH3 domain containing protein 0.0022 0.0069 0.017
Brugia malayi Protein kinase domain containing protein 0.0054 0.0651 0.1746
Loa Loa (eye worm) protein kinase C and casein kinase substrate in neurons protein 2 0.0022 0.0069 0.017
Echinococcus multilocularis tyrosine protein kinase Abl 0.0076 0.1055 0.1055
Echinococcus multilocularis epidermal growth factor receptor kinase 0.0022 0.0069 0.0069
Echinococcus multilocularis tyrosine protein kinase Blk 0.016 0.2577 0.2577
Echinococcus multilocularis PAK box P21 Rho binding 0.002 0.0026 0.0026
Entamoeba histolytica hypothetical protein 0.0022 0.0069 0.0333
Loa Loa (eye worm) hypothetical protein 0.0041 0.0411 0.1095
Onchocerca volvulus Suppressor of cytokine signaling at 36E homolog 0.0041 0.0411 0.587
Loa Loa (eye worm) hypothetical protein 0.0041 0.0411 0.1095
Entamoeba histolytica hypothetical protein 0.0022 0.0069 0.0333
Loa Loa (eye worm) hypothetical protein 0.0054 0.0651 0.1746
Schistosoma mansoni dreadlocks/dock 0.0022 0.0069 0.0069
Echinococcus granulosus tyrosine protein kinase Fps85D 0.0054 0.0651 0.0651
Echinococcus multilocularis tyrosine protein kinase Src42A 0.0182 0.2981 0.2981
Echinococcus granulosus SHC transforming protein 3 0.0041 0.0411 0.0411
Schistosoma mansoni hypothetical protein 0.0041 0.0411 0.0411
Schistosoma mansoni vesicular amine transporter 0.0022 0.006 0.006
Echinococcus granulosus SH2 domain containing adapter protein F 0.0041 0.0411 0.0411
Echinococcus multilocularis tyrosine protein phosphatase non receptor type 0.0041 0.0411 0.0411
Echinococcus granulosus SH2 domain containing protein 7 0.0041 0.0411 0.0411
Schistosoma mansoni chimerin-related rho-gtpase-activating protein 0.0048 0.0544 0.0544
Schistosoma mansoni protein kinase 0.002 0.0026 0.0026
Schistosoma mansoni tyrosine kinase 0.0182 0.2981 0.2981
Echinococcus granulosus defective proboscis extension response 0.0019 0.0007 0.0007
Echinococcus multilocularis tyrosine protein kinase ABL1 0.0054 0.0651 0.0651
Echinococcus granulosus 3'partial|tyrosine protein kinase Fgr 0.0182 0.2981 0.2981
Echinococcus granulosus slit robo rho gtpase activating protein 1 0.0022 0.0069 0.0069
Echinococcus granulosus tyrosine protein kinase Src42A 0.015 0.2395 0.2395
Brugia malayi Protein kinase domain containing protein 0.0054 0.0651 0.1746
Loa Loa (eye worm) TK protein kinase 0.0119 0.1831 0.4942
Echinococcus granulosus tyrosine protein kinase Fyn 0.0182 0.2981 0.2981
Brugia malayi Peripheral plasma membrane protein CASK 0.0022 0.0069 0.017
Trichomonas vaginalis neutrophil cytosolic factor 2, neutrophil NADPH oxidase factor, putative 0.0022 0.0069 0.1461
Loa Loa (eye worm) hypothetical protein 0.0041 0.0411 0.1095
Echinococcus granulosus RNA directed DNA polymerase 0.0048 0.0533 0.0533
Echinococcus granulosus expressed protein 0.0022 0.0069 0.0069
Brugia malayi serine/threonine-protein kinase PAK 7 0.0221 0.3699 1
Brugia malayi protein-tyrosine kinase 0.0022 0.0069 0.017
Schistosoma mansoni tyrosine kinase 0.0526 0.9254 0.9254
Trichomonas vaginalis voltage and ligand gated potassium channel, putative 0.0042 0.0424 1
Trichomonas vaginalis STE family protein kinase 0.002 0.0026 0.0424
Schistosoma mansoni protein tyrosine phosphatase n11 (shp2) 0.0041 0.0411 0.0411
Schistosoma mansoni suppressor of cytokine signaling 0.0041 0.0411 0.0411
Loa Loa (eye worm) hypothetical protein 0.0022 0.0069 0.017
Echinococcus multilocularis roundabout 2 0.0019 0.0007 0.0007
Entamoeba histolytica protein kinase, putative 0.002 0.0026 0.0097
Echinococcus multilocularis 0.0041 0.0411 0.0411
Loa Loa (eye worm) RhoGAP domain-containing protein 0.0048 0.0544 0.1456
Entamoeba histolytica hypothetical protein 0.0022 0.0069 0.0333
Brugia malayi SH2 domain containing protein 0.0041 0.0411 0.1095
Schistosoma mansoni tyrosine kinase 0.0182 0.2981 0.2981
Echinococcus granulosus signal transduction protein lnk realted 0.0041 0.0411 0.0411
Schistosoma mansoni tyrosine kinase 0.0076 0.1055 0.1055
Entamoeba histolytica p21-activated kinase 0.002 0.0026 0.0097
Loa Loa (eye worm) hypothetical protein 0.0041 0.0411 0.1095
Entamoeba histolytica BAR/SH3 domain containing protein 0.0022 0.0069 0.0333
Schistosoma mansoni tyrosine kinase 0.0032 0.0249 0.0249
Schistosoma mansoni serine/threonine protein kinase 0.0068 0.0896 0.0896
Echinococcus granulosus tyrosine kinase|tyrosine protein kinase Fyn 0.016 0.2577 0.2577
Schistosoma mansoni growth factor receptor-bound protein 0.0063 0.0815 0.0815
Schistosoma mansoni C-fyn 0.0022 0.0069 0.0069
Echinococcus granulosus tyrosine protein kinase Srms 0.0054 0.0651 0.0651
Schistosoma mansoni apoptosis stimulating of P53 0.0022 0.0069 0.0069
Schistosoma mansoni serine/threonine protein kinase 0.002 0.0028 0.0028
Brugia malayi Variant SH3 domain containing protein 0.0022 0.0069 0.017
Trypanosoma cruzi hypothetical protein, conserved 0.0025 0.0127 1
Entamoeba histolytica hypothetical protein 0.0022 0.0069 0.0333
Loa Loa (eye worm) TK protein kinase 0.016 0.2577 0.6962
Brugia malayi WH1 domain containing protein 0.0019 0.0009 0.0005
Loa Loa (eye worm) hypothetical protein 0.0022 0.0069 0.017
Echinococcus granulosus tyrosine protein kinase Src64B 0.0182 0.2981 0.2981
Schistosoma mansoni chimerin-related rho-gtpase-activating protein 0.0048 0.0544 0.0544
Echinococcus granulosus p21 activated protein kinase 1 Dpak1 0.002 0.0026 0.0026
Schistosoma mansoni tensin-related 0.0041 0.0411 0.0411
Entamoeba histolytica hypothetical protein, conserved 0.0022 0.0069 0.0333
Echinococcus granulosus raf serine:threonine protein kinase 0.002 0.0039 0.0039
Schistosoma mansoni wiskott-aldrich syndrome protein 0.0019 0.0009 0.0009
Entamoeba histolytica hypothetical protein 0.0022 0.0069 0.0333
Echinococcus granulosus suppressor of cytokine signaling 6 0.0041 0.0411 0.0411
Loa Loa (eye worm) TK/FER protein kinase 0.0054 0.0651 0.1746
Schistosoma mansoni protein kinase 0.002 0.0026 0.0026
Echinococcus granulosus SH2 motif 0.0041 0.0411 0.0411
Echinococcus multilocularis telomerase reverse transcriptase subunit 0.0048 0.0533 0.0533
Schistosoma mansoni defective proboscis extension response (dpr)-related 0.0019 0.0007 0.0007
Loa Loa (eye worm) hypothetical protein 0.0041 0.0411 0.1095
Echinococcus multilocularis c src tyrosine kinase 0.0076 0.1055 0.1055
Echinococcus multilocularis tyrosine kinase 0.0054 0.0651 0.0651
Brugia malayi Fes/CIP4 homology domain containing protein 0.0022 0.0069 0.017
Loa Loa (eye worm) hypothetical protein 0.0063 0.0815 0.2189
Echinococcus multilocularis tyrosine protein kinase Fyn 0.0182 0.2981 0.2981
Schistosoma mansoni tensin-related 0.0041 0.0411 0.0411
Loa Loa (eye worm) hypothetical protein 0.0039 0.037 0.0984
Loa Loa (eye worm) hypothetical protein 0.0041 0.0411 0.1095
Brugia malayi Variant SH3 domain containing protein 0.0025 0.0127 0.0327
Echinococcus granulosus PAK box P21 Rho binding 0.0019 0.0009 0.0009
Echinococcus multilocularis SH2 motif 0.0041 0.0411 0.0411
Loa Loa (eye worm) guanylate kinase 0.0022 0.0069 0.017
Brugia malayi Variant SH3 domain containing protein 0.0063 0.0815 0.2189
Trichomonas vaginalis conserved hypothetical protein 0.0022 0.0069 0.1461
Loa Loa (eye worm) hypothetical protein 0.0022 0.0069 0.017
Echinococcus granulosus serine:threonine protein kinase PAK 4 0.0202 0.3356 0.3356
Echinococcus multilocularis p21 activated protein kinase 1 Dpak1 0.002 0.0026 0.0026
Schistosoma mansoni tyrosine kinase 0.0057 0.071 0.071
Brugia malayi Protein kinase domain containing protein 0.0054 0.0651 0.1746
Echinococcus multilocularis Immunoglobulin 0.0019 0.0007 0.0007
Echinococcus granulosus src region 0.0022 0.0069 0.0069
Loa Loa (eye worm) protein-tyrosine kinase 0.0022 0.0069 0.017
Echinococcus multilocularis Protein kinase C, brain isozyme 0.0068 0.0896 0.0896
Schistosoma mansoni suppressor of cytokine signaling 0.0041 0.0411 0.0411
Echinococcus granulosus endophilin A3 0.0022 0.0069 0.0069
Brugia malayi SH2 domain containing protein 0.0054 0.0651 0.1746
Brugia malayi Protein kinase domain 0.002 0.0026 0.0053
Entamoeba histolytica SH2 domain containing protein 0.0041 0.0411 0.2208
Schistosoma mansoni serine/threonine protein kinase 0.0162 0.2624 0.2624
Loa Loa (eye worm) hypothetical protein 0.0041 0.0411 0.1095
Loa Loa (eye worm) TK/KIN16 protein kinase 0.0032 0.0247 0.0651
Echinococcus multilocularis serine:threonine protein kinase PAK 4 0.0202 0.3356 0.3356
Echinococcus granulosus growth factor receptor bound protein 2 0.0066 0.0873 0.0873
Brugia malayi Voltage-gated potassium channel, HERG (KCNH2)-related. C. elegans unc-103 ortholog 0.0045 0.0477 0.1275
Echinococcus multilocularis SH2 domain containing protein 7 0.0041 0.0411 0.0411
Onchocerca volvulus Suppressor of cytokine signaling 7 homolog 0.0041 0.0411 0.587
Loa Loa (eye worm) hypothetical protein 0.0022 0.0069 0.017
Brugia malayi P21-Rho-binding domain containing protein 0.0019 0.0009 0.0005
Schistosoma mansoni nck2/grb4 0.0063 0.0815 0.0815
Echinococcus multilocularis tyrosine protein kinase Src64B 0.0182 0.2981 0.2981
Brugia malayi Immunoglobulin I-set domain containing protein 0.0032 0.0247 0.0651
Loa Loa (eye worm) hypothetical protein 0.0022 0.0069 0.017
Loa Loa (eye worm) hypothetical protein 0.0048 0.0533 0.1426
Loa Loa (eye worm) variant SH3 domain-containing protein 0.0022 0.0069 0.017
Echinococcus multilocularis tyrosine protein kinase Fyn 0.0182 0.2981 0.2981
Echinococcus multilocularis suppressor of cytokine signaling 6 0.0041 0.0411 0.0411
Brugia malayi Protein-tyrosine phosphatase containing protein 0.0041 0.0411 0.1095
Echinococcus granulosus Immunoglobulin 0.0019 0.0007 0.0007
Echinococcus granulosus tensin C1 domain containing phosphatase 0.0041 0.0411 0.0411
Onchocerca volvulus 0.0023 0.0087 0.0302
Echinococcus granulosus arf GAP with SH3 domain ANK repeat and PH 0.0022 0.0069 0.0069
Echinococcus multilocularis SH2 domain containing adapter protein F 0.0041 0.0411 0.0411
Entamoeba histolytica protein kinase, putative 0.002 0.0026 0.0097
Schistosoma mansoni serine/threonine protein kinase 0.0068 0.0896 0.0896
Trypanosoma cruzi hypothetical protein, conserved 0.0025 0.0127 1
Schistosoma mansoni sorbin 0.0022 0.0069 0.0069
Echinococcus multilocularis suppressor of cytokine signaling 7 0.0041 0.0411 0.0411
Entamoeba histolytica BAR/SH3 domain containing protein 0.0022 0.0069 0.0333
Entamoeba histolytica hypothetical protein 0.0022 0.0069 0.0333
Entamoeba histolytica protein kinase, putative 0.0022 0.0069 0.0333
Trichomonas vaginalis voltage and ligand gated potassium channel, putative 0.0042 0.0424 1
Echinococcus granulosus tyrosine protein kinase Lyn 0.0183 0.2999 0.2999
Echinococcus multilocularis tyrosine protein kinase Fps85D 0.0054 0.0651 0.0651
Echinococcus granulosus suppressor of cytokine signaling 7 0.0041 0.0411 0.0411
Loa Loa (eye worm) SRC-1 0.0182 0.2981 0.8056
Onchocerca volvulus 0.0041 0.0411 0.587
Echinococcus multilocularis neuroglian 0.0019 0.0007 0.0007
Brugia malayi Sex muscle abnormal protein 5 0.0063 0.0815 0.2189
Echinococcus multilocularis guanine nucleotide exchange factor VAV2 0.0048 0.0544 0.0544
Echinococcus granulosus epidermal growth factor receptor kinase 0.0022 0.0069 0.0069
Schistosoma mansoni development and differentiation-enhancing factor ddef 0.0022 0.0069 0.0069
Onchocerca volvulus 0.0041 0.0411 0.587
Schistosoma mansoni voltage-gated potassium channel 0.0049 0.0552 0.0552
Echinococcus granulosus SH2 motif 0.0041 0.0411 0.0411
Loa Loa (eye worm) TK/FER protein kinase 0.0054 0.0651 0.1746
Loa Loa (eye worm) TK/FER protein kinase 0.0054 0.0651 0.1746
Schistosoma mansoni dynamin-associated protein 0.0025 0.0127 0.0127
Loa Loa (eye worm) hypothetical protein 0.0041 0.0411 0.1095
Echinococcus multilocularis NCK adaptor protein 0.0066 0.0873 0.0873
Echinococcus multilocularis serine:threonine protein kinase PAK 3 0.002 0.0026 0.0026
Brugia malayi Variant SH3 domain containing protein 0.0022 0.0069 0.017
Brugia malayi hypothetical protein 0.0054 0.0651 0.1746
Schistosoma mansoni proto-oncogene tyrosine-protein kinase src 0.0076 0.1055 0.1055
Echinococcus granulosus tyrosine protein kinase Fyn 0.0182 0.2981 0.2981
Echinococcus multilocularis expressed protein 0.0022 0.0069 0.0069
Echinococcus multilocularis tyrosine protein kinase Fyn 0.016 0.2577 0.2577
Trichomonas vaginalis conserved hypothetical protein 0.0022 0.0069 0.1461
Echinococcus multilocularis tyrosine protein kinase Srms 0.016 0.2577 0.2577
Echinococcus granulosus tyrosine protein kinase Src42A 0.0182 0.2981 0.2981
Echinococcus granulosus tyrosine protein phosphatase non receptor type 0.0041 0.0411 0.0411
Loa Loa (eye worm) TK/FER protein kinase 0.0054 0.0651 0.1746
Schistosoma mansoni hypothetical protein 0.0022 0.0069 0.0069
Loa Loa (eye worm) hypothetical protein 0.0041 0.0411 0.1095
Echinococcus granulosus proto oncogene tyrosine protein kinase LCK 0.0182 0.2981 0.2981
Loa Loa (eye worm) TK/FER protein kinase 0.0054 0.0651 0.1746
Loa Loa (eye worm) STAT protein 0.0041 0.0411 0.1095
Echinococcus multilocularis fch and double sh3 domains protein 2 0.0022 0.0069 0.0069
Schistosoma mansoni tyrosine kinase 0.0076 0.1055 0.1055
Echinococcus granulosus 3'partial|serine:threonine protein kinase PAK 2 0.0019 0.0009 0.0009
Echinococcus granulosus protein kinase C gamma type 0.006 0.0763 0.0763
Schistosoma mansoni GTPase activating protein 0.0041 0.0411 0.0411
Echinococcus granulosus hematopoietic lineage cell specific protein 0.0022 0.0069 0.0069
Onchocerca volvulus 0.0054 0.0651 1
Echinococcus granulosus neuroglian 0.0019 0.0007 0.0007
Echinococcus multilocularis Spectrin alpha actinin 0.0022 0.0069 0.0069
Entamoeba histolytica SH2-protein kinase domain containing protein 0.0042 0.0429 0.2304
Entamoeba histolytica hypothetical protein 0.0022 0.0069 0.0333
Leishmania major hypothetical protein, conserved 0.0025 0.0127 0.5
Echinococcus granulosus intersectin 2 0.0027 0.0155 0.0155
Loa Loa (eye worm) sex muscle abnormal protein 5 0.0063 0.0815 0.2189
Brugia malayi SH2 domain containing protein 0.0041 0.0411 0.1095
Loa Loa (eye worm) SH2 domain-containing protein 0.0041 0.0411 0.1095
Schistosoma mansoni cell adhesion molecule 0.0019 0.0007 0.0007
Loa Loa (eye worm) hypothetical protein 0.0022 0.0069 0.017
Onchocerca volvulus 0.0054 0.0651 1
Echinococcus multilocularis tyrosine protein kinase Fgr 0.0182 0.2981 0.2981
Onchocerca volvulus 0.0041 0.0411 0.587
Loa Loa (eye worm) cytokine inducible SH2-containing protein 5 0.0041 0.0411 0.1095
Schistosoma mansoni tensin 0.0041 0.0411 0.0411
Echinococcus granulosus guanine nucleotide exchange factor VAV2 0.0048 0.0544 0.0544
Schistosoma mansoni tyrosine-protein kinase zap-70 0.0041 0.0411 0.0411
Brugia malayi protein kinase C II. 0.002 0.0028 0.0057
Echinococcus granulosus tyrosine protein kinase Fyn 0.0182 0.2981 0.2981
Entamoeba histolytica hypothetical protein 0.0022 0.0069 0.0333
Echinococcus multilocularis neural Wiskott Aldrich syndrome protein 0.0019 0.0009 0.0009
Brugia malayi Tensin 0.0041 0.0411 0.1095
Loa Loa (eye worm) TK/ABL protein kinase 0.0054 0.0651 0.1746
Echinococcus granulosus Protein kinase C brain isozyme 0.0068 0.0896 0.0896
Brugia malayi P21-Rho-binding domain containing protein 0.0019 0.0009 0.0005
Schistosoma mansoni tyrosine kinase 0.0567 1 1
Echinococcus granulosus nostrin 0.0022 0.0069 0.0069
Trichomonas vaginalis conserved hypothetical protein 0.0022 0.0069 0.1461
Brugia malayi tRNA modification GTPase TrmE family protein 0.0041 0.0411 0.1095
Echinococcus multilocularis tyrosine protein kinase shark 0.0567 1 1
Loa Loa (eye worm) TK/FER protein kinase 0.0054 0.0651 0.1746
Brugia malayi Protein kinase c protein 2 0.0057 0.0712 0.1909
Loa Loa (eye worm) hypothetical protein 0.0041 0.0411 0.1095
Echinococcus multilocularis SH2 motif 0.0041 0.0411 0.0411
Onchocerca volvulus 0.0025 0.0127 0.1001
Schistosoma mansoni eps8-related protein 0.0022 0.0069 0.0069
Echinococcus multilocularis nostrin 0.0022 0.0069 0.0069
Schistosoma mansoni nephrin 0.0019 0.0007 0.0007
Echinococcus multilocularis signal transduction protein lnk realted 0.0041 0.0411 0.0411
Echinococcus multilocularis SHC transforming protein 3 0.0041 0.0411 0.0411
Loa Loa (eye worm) voltage and ligand gated potassium channel 0.0045 0.0477 0.1275
Echinococcus multilocularis tyrosine protein phosphatase non receptor type 0.0041 0.0411 0.0411
Schistosoma mansoni hypothetical protein 0.0022 0.0069 0.0069
Brugia malayi Variant SH3 domain containing protein 0.0042 0.0439 0.117
Schistosoma mansoni signal transducing adapter molecule (stam) 0.0022 0.0069 0.0069
Echinococcus granulosus serine:threonine protein kinase PAK 3 0.002 0.0026 0.0026
Entamoeba histolytica protein kinase, putative 0.002 0.0026 0.0097
Onchocerca volvulus 0.0054 0.0651 1
Loa Loa (eye worm) hypothetical protein 0.0041 0.0411 0.1095
Echinococcus multilocularis tensin 0.0041 0.0411 0.0411
Loa Loa (eye worm) AGC/PKC/ETA protein kinase 0.002 0.0028 0.0057
Echinococcus multilocularis arf GAP with SH3 domain, ANK repeat and PH 0.0022 0.0069 0.0069
Brugia malayi SH2 domain containing protein 0.0041 0.0411 0.1095
Brugia malayi SH2 domain containing protein 0.0041 0.0411 0.1095
Loa Loa (eye worm) hypothetical protein 0.0041 0.0411 0.1095
Brugia malayi SH2 domain containing protein 0.0041 0.0411 0.1095
Echinococcus granulosus N chimaerin 0.0048 0.0544 0.0544
Echinococcus granulosus potassium voltage gated channel subfamily H 0.0045 0.0477 0.0477
Trichomonas vaginalis conserved hypothetical protein 0.0022 0.0069 0.1461
Echinococcus granulosus hypothetical protein 0.0041 0.0411 0.0411
Brugia malayi Variant SH3 domain containing protein 0.0022 0.0069 0.017
Schistosoma mansoni Neurotrimin precursor (hNT) 0.0019 0.0007 0.0007
Loa Loa (eye worm) hypothetical protein 0.0019 0.0009 0.0005
Loa Loa (eye worm) AGC/PKC/ALPHA protein kinase 0.005 0.0579 0.1549
Echinococcus granulosus mitogen-activated protein kinase kinase kinase 9 0.0124 0.1934 0.1934
Onchocerca volvulus 0.0054 0.0651 1
Schistosoma mansoni adapter molecule crk 0.0063 0.0815 0.0815
Echinococcus multilocularis tyrosine protein kinase Btk29A 0.0076 0.1055 0.1055
Brugia malayi SRC-1 0.0182 0.2981 0.8056
Brugia malayi protein-tyrosine kinase 0.016 0.2577 0.6962
Echinococcus multilocularis RNA directed DNA polymerase 0.0048 0.0533 0.0533
Schistosoma mansoni hypothetical protein 0.0019 0.0009 0.0009
Echinococcus granulosus Spectrin alpha actinin 0.0022 0.0069 0.0069
Schistosoma mansoni vav2 0.0048 0.0544 0.0544
Trichomonas vaginalis STE family protein kinase 0.002 0.0026 0.0424
Echinococcus granulosus tensin 0.0041 0.0411 0.0411
Entamoeba histolytica SH2-protein kinase domain containing protein 0.0054 0.0651 0.3527
Loa Loa (eye worm) hypothetical protein 0.0025 0.0127 0.0327
Trichomonas vaginalis STE family protein kinase 0.002 0.0026 0.0424
Echinococcus multilocularis intersectin 2 0.0027 0.0155 0.0155
Loa Loa (eye worm) hypothetical protein 0.0055 0.0666 0.1787
Trichomonas vaginalis STE family protein kinase 0.002 0.0026 0.0424
Echinococcus granulosus breast cancer anti estrogen resistance protein 0.0022 0.0069 0.0069
Schistosoma mansoni slit-robo rho gtpase activating protein 0.0022 0.0069 0.0069
Schistosoma mansoni proto-oncogene tyrosine-protein kinase abl1 0.0063 0.0815 0.0815
Brugia malayi SH2 domain containing protein 0.0041 0.0411 0.1095
Echinococcus multilocularis rho guanine nucleotide exchange factor 7 0.0022 0.0069 0.0069
Schistosoma mansoni protein kinase 0.002 0.0026 0.0026
Loa Loa (eye worm) protein-tyrosine phosphatase 0.0041 0.0411 0.1095
Echinococcus granulosus tyrosine protein kinase Blk 0.016 0.2577 0.2577
Brugia malayi SH3 domain containing protein 0.0022 0.0069 0.017
Trichomonas vaginalis conserved hypothetical protein 0.0022 0.0069 0.1461
Brugia malayi hypothetical protein 0.0041 0.0411 0.1095
Onchocerca volvulus 0.0054 0.0651 1
Echinococcus multilocularis mitogen activated protein kinase kinase kinase 0.0124 0.1934 0.1934
Echinococcus multilocularis tyrosine protein kinase Src42A 0.015 0.2395 0.2395
Brugia malayi Guanylate kinase family protein 0.0022 0.0069 0.017
Schistosoma mansoni tensin 0.0041 0.0411 0.0411
Echinococcus granulosus tyrosine protein kinase Btk29A 0.0076 0.1055 0.1055
Echinococcus granulosus NCK adaptor protein 0.0063 0.0815 0.0815
Echinococcus multilocularis tyrosine protein kinase HCK 0.0119 0.1831 0.1831
Echinococcus granulosus tyrosine protein kinase ABL1 0.0054 0.0651 0.0651
Echinococcus granulosus expressed conserved protein 0.0041 0.0411 0.0411
Brugia malayi Variant SH3 domain containing protein 0.0063 0.0815 0.2189
Brugia malayi Spectrin alpha chain 0.0022 0.0069 0.017
Echinococcus multilocularis serine threonine protein kinase 0.006 0.0763 0.0763
Brugia malayi Protein kinase domain containing protein 0.0054 0.0651 0.1746

Activities

Activity type Activity value Assay description Source Reference
Fu (ADMET) = 1.4 % Fraction unbound in human plasma ChEMBL. 23350847
IC50 (binding) = 1 nM Inhibition of human recombinant spleen tyrosine kinase (360 to 635 amino acid residues) after 10 mins by scintillation counting analysis ChEMBL. 23151054
IC50 (binding) = 1 nM Inhibition of human recombinant truncated SYK (360 to 365 amino acid residues) using N-terminally biotinylated EPEGDYEEVLE peptide as substrate assessed as inhibition of [33P]-ATP incorporation incubated for 10 mins prior to substrate addition measured after 15 mins by scintillation counting ChEMBL. 23350847
IC50 (binding) = 1 nM Millipore Kinase Panel Assay BINDINGDB. No reference
IC50 (binding) = 6 nM BindingDB_Patents: Inhibition Assay. SYK tyrosine phosphorylation activity is measured using the LANCE Technology developed by Perkin Elmer Life and Analytical Sciences (Boston, Mass.). LANCE refers to homogeneous time resolved fluorometry applications using techniques such as time-resolved fluorescence resonance energy transfer assay (TR-FRET) (see generally for procedures in Perkin Elmer Application Note How to Optimize a Tyrosine Kinase Assay Using Time Resolved Fluorescence-Based LANCE Detection, wwww.perkinelmer.com/lifesciences). The assay principle involves detection of a phosphorylated substrate using energy transfer from a phosphospecific europium-labeled antibody to streptavidin-allophycocyanin as an acceptor.To test the ability of candidate molecules to inhibit SYK tyrosine phosphorylation activity, molecules are reconstituted in 30% DMSO and serially diluted 1:3 with the final dilution containing DMSO in the absence of the candidate molecule. The final DMSO concentration in the assay is 3%. ChEMBL. No reference
IC50 (binding) = 6 nM BindingDB_Patents: Inhibition Assay. SYK tyrosine phosphorylation activity is measured using the LANCE Technology developed by Perkin Elmer Life and Analytical Sciences (Boston, Mass.). LANCE refers to homogeneous time resolved fluorometry applications using techniques such as time-resolved fluorescence resonance energy transfer assay (TR-FRET) (see generally for procedures in Perkin Elmer Application Note How to Optimize a Tyrosine Kinase Assay Using Time Resolved Fluorescence-Based LANCE Detection, wwww.perkinelmer.com/lifesciences). The assay principle involves detection of a phosphorylated substrate using energy transfer from a phosphospecific europium-labeled antibody to streptavidin-allophycocyanin as an acceptor.To test the ability of candidate molecules to inhibit SYK tyrosine phosphorylation activity, molecules are reconstituted in 30% DMSO and serially diluted 1:3 with the final dilution containing DMSO in the absence of the candidate molecule. The final DMSO concentration in the assay is 3%. ChEMBL. No reference
IC50 (binding) = 13 nM Inhibition of Syk (unknown origin) using 4 uM peptide assessed as product formation after 60 mins incubation by microfluidic mobility shift assay ChEMBL. 24726806
IC50 (binding) = 13 nM Inhibition of Syk (unknown origin) using 5-Fluo-Ahx-GAPDYENLQELNKK-Amide as substrate after 60 mins by microfluidic mobility shift assay ChEMBL. 25633741
IC50 (binding) = 13 nM Inhibition of Syk (unknown origin) using 5-Fluo-Ahx-GAPDYENLQELNKK-Amide as substrate after 60 mins by microfluidic mobility shift assay ChEMBL. 26320624
IC50 (binding) = 60 nM Inhibition of ZAP70 (unknown origin) ChEMBL. 24726806
IC50 (binding) = 68 nM Inhibition of human ZAP70 ChEMBL. 25633741
IC50 (binding) = 81 nM Millipore Kinase Panel Assay BINDINGDB. No reference
IC50 (binding) = 90 nM Inhibition of human PKCalpha ChEMBL. 25633741
IC50 (binding) = 123 nM Millipore Kinase Panel Assay BINDINGDB. No reference
IC50 (binding) = 139 nM Millipore Kinase Panel Assay BINDINGDB. No reference
IC50 (binding) = 166 nM BindingDB_Patents: Millipore Kinase Panel Assay. Employing the Milipore panel of purified kinases EXAMPLE 87 (IC50=1 nM) inhibited 98% of purified Syk kinase activity at 50 nM. IC50 values were determined for those kinases that were inhibited by >80% at 300 nM in the Millipore kinase panel. ChEMBL. No reference
IC50 (binding) = 178 nM Inhibition of Syk in anti IgM-stimulated human Ramos cells assessed as BLNK phosphorylation by cellular assay ChEMBL. 24726806
IC50 (binding) = 178 nM Inhibition of Syk in anti-igM stimulated human Ramos B cells assessed as phospho-BLNK level preincubated for 30 mins followed by anti-IgM stimulation measured after 15 mins by flow cytometric analysis ChEMBL. 25633741
IC50 (binding) = 178 nM Inhibition of Syk in anti-igM stimulated human Ramos B cells assessed as phospho-BLNK level preincubated for 30 mins followed by anti-IgM stimulation measured after 15 mins by flow cytometric analysis ChEMBL. 26320624
IC50 (binding) = 199 nM Millipore Kinase Panel Assay BINDINGDB. No reference
IC50 (binding) = 238 nM Inhibition of Lyn (unknown origin) ChEMBL. 24726806
IC50 (binding) = 244 nM Millipore Kinase Panel Assay BINDINGDB. No reference
IC50 (binding) = 300 nM Millipore Kinase Panel Assay BINDINGDB. No reference
IC50 (binding) = 952 nM Inhibition of Syk in human whole blood assessed as inhibition of P-SLP76 in CD14+ monocytes by flow cytometry ChEMBL. 24726806
IC50 (binding) = 952 nM Inhibition of Syk in anti-CD32 stimulated CD14+ human monocytes assessed as phospho-SLP76 level preincubated for 30 mins followed by anti-CD32 stimulation measured after 5 mins by flow cytometric analysis ChEMBL. 25633741
IC50 (binding) = 952 nM Inhibition of Syk in anti-CD32 stimulated CD14+ human monocytes in presence of 90% human blood assessed as phospho-SLP76 level preincubated for 30 mins followed by anti-CD32 stimulation measured after 5 mins by flow cytometric analysis ChEMBL. 26320624
IC50 (binding) = 1750 nM Inhibition of JAK2 (unknown origin) ChEMBL. 24726806
IC50 (binding) = 1805 nM Inhibition of ZAP70 in anti-CD3 stimulated human Jurkat T cells assessed as SLP76 phosphorylation at Y128 preincubated for 30 mins followed by anti-CD3 stimulation measured after 2 mins by FACS analysis ChEMBL. 25633741
IC50 (binding) = 8600 nM Inhibition of human ERG by Q-patch assay ChEMBL. 24726806
IC50 (binding) = 8600 nM Inhibition of human ERG expressed in CHO cells by automated Qpatch clamp assay ChEMBL. 25633741
IC50 (binding) = 0.223 uM Inhibition of SYK in human Ramos cells ChEMBL. 23350847
IC50 (functional) = 0.223 uM Cytotoxicity against human Ramos cells ChEMBL. 23151054
IC50 (binding) = 0.54 uM Inhibition of SYK in human whole blood ChEMBL. 23350847
IC50 (binding) = 9.1 uM Inhibition of human ERG channel ChEMBL. 23350847
IC50 (binding) = 10 uM Inhibition of human ERG by manual patch clamp assay ChEMBL. 25633741
IC50 (ADMET) > 25 uM Inhibition of CYP3A4 (unknown origin) ChEMBL. 23350847
Inhibition (binding) = 42 % Inhibition of human ERG at 10 uM by manual patch clamp assay relative to control ChEMBL. 25633741
Inhibition (binding) = 72 % Inhibition of human ERG at 30 uM by manual patch clamp assay relative to control ChEMBL. 25633741

Phenotypes

Whole-cell/tissue/organism interactions

Species name Source Reference Is orphan
Homo sapiens ChEMBL23 23151054

Many chemical entities in TDR Targets come from high-throughput screenings with whole cells or tissue samples, and not all assayed compounds have been tested against a single a single target protein, probably because they get ruled out during screening process. Even if these compounds may have not been of interest in the original screening, they may come as interesting leads for other screening assays. Furthermore, we may be able to propose drug-target associations using chemical similarities and network patterns.

Annotated phenotypes:

We have no manually annotated phenotypes for this drug. What does this mean? / Care to help?
In TDR Targets, information about phenotypes that are caused by drugs, or by genetic manipulation of cells (e.g. gene knockouts or knockdowns) is manually curated from the literature. These descriptions help to describe the potential of the target for drug development. If no information is available for this gene or if the information is incomplete, this may mean that i) the papers containing this information either appeared after the curation effort for this organism was carried out or they were inadvertently missed by curators; or that ii) the curation effort for this organism has not yet started.
 
In any case, if you have information about papers containing relevant validation data for this target, please log in using your TDR Targets username and password and send them to us using the corresponding form in this page (only visible to registered users) or contact us.

External resources for this compound

Bibliographic References

5 literature references were collected for this gene.

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