Detailed information for compound 1747016

Basic information

Technical information
  • TDR Targets ID: 1747016
  • Name: N-(5-chloro-6-methyl-2-pyridin-2-ylpyrimidin- 4-yl)-N'-[5-(trifluoromethyl)pyridin-2-yl]eth ane-1,2-diamine
  • MW: 408.808 | Formula: C18H16ClF3N6
  • H donors: 2 H acceptors: 4 LogP: 4 Rotable bonds: 7
    Rule of 5 violations (Lipinski): 1
  • SMILES: Cc1nc(nc(c1Cl)NCCNc1ccc(cn1)C(F)(F)F)c1ccccn1
  • InChi: 1S/C18H16ClF3N6/c1-11-15(19)17(28-16(27-11)13-4-2-3-7-23-13)25-9-8-24-14-6-5-12(10-26-14)18(20,21)22/h2-7,10H,8-9H2,1H3,(H,24,26)(H,25,27,28)
  • InChiKey: RKRMHCLBTVBYAU-UHFFFAOYSA-N  


Substructure search Similarity search

Network

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Synonyms

  • N-[5-chloro-6-methyl-2-(2-pyridyl)pyrimidin-4-yl]-N'-[5-(trifluoromethyl)-2-pyridyl]ethane-1,2-diamine
  • N-[5-chloro-6-methyl-2-(2-pyridyl)-4-pyrimidinyl]-N'-[5-(trifluoromethyl)-2-pyridyl]ethane-1,2-diamine
  • [5-chloro-6-methyl-2-(2-pyridyl)pyrimidin-4-yl]-[2-[[5-(trifluoromethyl)-2-pyridyl]amino]ethyl]amine
  • N-(5-chloro-6-methyl-2-pyridin-2-yl-pyrimidin-4-yl)-N'-[5-(trifluoromethyl)pyridin-2-yl]ethane-1,2-diamine
  • Maybridge3_004606
  • RDR 03877
  • IDI1_015993

Targets

Known targets for this compound

Species Target name Source Bibliographic reference
Homo sapiens methionyl aminopeptidase 1 Starlite/ChEMBL References

Predicted pathogen targets for this compound

By orthology
Species Potential target Known druggable target/s Ortholog Group
Toxoplasma gondii methionine aminopeptidase, type i, putative Get druggable targets OG5_126721 All targets in OG5_126721
Plasmodium yoelii methionine aminopeptidase, type I, putative Get druggable targets OG5_126721 All targets in OG5_126721
Toxoplasma gondii methionine aminopeptidase Get druggable targets OG5_126721 All targets in OG5_126721
Leishmania mexicana methionine aminopeptidase Get druggable targets OG5_126721 All targets in OG5_126721
Treponema pallidum methionine aminopeptidase (map) Get druggable targets OG5_126721 All targets in OG5_126721
Schistosoma mansoni methionyl aminopeptidase 1 (M24 family) Get druggable targets OG5_126721 All targets in OG5_126721
Echinococcus granulosus methionyl aminopeptidase 1 M24 family Get druggable targets OG5_126721 All targets in OG5_126721
Trypanosoma brucei methionine aminopeptidase, putative Get druggable targets OG5_126721 All targets in OG5_126721
Schistosoma japonicum ko:K01265 methionyl aminopeptidase [EC3.4.11.18], putative Get druggable targets OG5_126721 All targets in OG5_126721
Trypanosoma brucei metallo- peptidase, Clan MG, Family M24 Get druggable targets OG5_126721 All targets in OG5_126721
Candida albicans methionine aminopeptidase Get druggable targets OG5_126721 All targets in OG5_126721
Plasmodium knowlesi methionine aminopeptidase 1b, putative Get druggable targets OG5_126721 All targets in OG5_126721
Neospora caninum methionine aminopeptidase, putative Get druggable targets OG5_126721 All targets in OG5_126721
Plasmodium berghei methionine aminopeptidase 1b, putative Get druggable targets OG5_126721 All targets in OG5_126721
Brugia malayi Methionine aminopeptidase protein type I Get druggable targets OG5_126721 All targets in OG5_126721
Mycobacterium ulcerans methionine aminopeptidase Get druggable targets OG5_126721 All targets in OG5_126721
Leishmania braziliensis methionine aminopeptidase, putative,metallo-peptidase, Clan MG, Family M24 Get druggable targets OG5_126721 All targets in OG5_126721
Babesia bovis methionine aminopeptidase, putative Get druggable targets OG5_126721 All targets in OG5_126721
Mycobacterium leprae PROBABLE METHIONINE AMINOPEPTIDASE MAPB (MAP) (PEPTIDASE M) Get druggable targets OG5_126721 All targets in OG5_126721
Echinococcus multilocularis methionyl aminopeptidase 1 (M24 family) Get druggable targets OG5_126721 All targets in OG5_126721
Leishmania major methionine aminopeptidase, putative,metallo-peptidase, Clan MG, Family M24 Get druggable targets OG5_126721 All targets in OG5_126721
Schistosoma japonicum ko:K01265 methionyl aminopeptidase [EC3.4.11.18], putative Get druggable targets OG5_126721 All targets in OG5_126721
Candida albicans methionine aminopeptidase Get druggable targets OG5_126721 All targets in OG5_126721
Schistosoma mansoni methionyl aminopeptidase 1 (M24 family) Get druggable targets OG5_126721 All targets in OG5_126721
Neospora caninum methionine aminopeptidase, putative Get druggable targets OG5_126721 All targets in OG5_126721
Cryptosporidium parvum methionine aminopeptidase with MYND finger at N-terminus Get druggable targets OG5_126721 All targets in OG5_126721
Mycobacterium tuberculosis Methionine aminopeptidase MapA (map) (peptidase M) (MetAP) Get druggable targets OG5_126721 All targets in OG5_126721
Trypanosoma cruzi metallo- peptidase, Clan MG, Family M24 Get druggable targets OG5_126721 All targets in OG5_126721
Trypanosoma brucei methionine aminopeptidase, type I, putative Get druggable targets OG5_126721 All targets in OG5_126721
Plasmodium vivax methionine aminopeptidase 1b, putative Get druggable targets OG5_126721 All targets in OG5_126721
Toxoplasma gondii methionine aminopeptidase Get druggable targets OG5_126721 All targets in OG5_126721
Neospora caninum methionine aminopeptidase, putative Get druggable targets OG5_126721 All targets in OG5_126721
Loa Loa (eye worm) methionine aminopeptidase type I Get druggable targets OG5_126721 All targets in OG5_126721
Mycobacterium tuberculosis Methionine aminopeptidase MapB (map) (peptidase M) Get druggable targets OG5_126721 All targets in OG5_126721
Plasmodium knowlesi methionine aminopeptidase 1a, putative Get druggable targets OG5_126721 All targets in OG5_126721
Echinococcus multilocularis methionyl aminopeptidase 1 (M24 family) Get druggable targets OG5_126721 All targets in OG5_126721
Trypanosoma brucei gambiense methionine aminopeptidase, putative,metallo- peptidase, Clan MG, Family M24 Get druggable targets OG5_126721 All targets in OG5_126721
Leishmania infantum methionine aminopeptidase, putative,metallo-peptidase, Clan MG, Family M24 Get druggable targets OG5_126721 All targets in OG5_126721
Mycobacterium leprae PROBABLE METHIONINE AMINOPEPTIDASE MAPA (MAP) (PEPTIDASE M) (MetAP) Get druggable targets OG5_126721 All targets in OG5_126721
Schistosoma japonicum Methionine aminopeptidase 1, putative Get druggable targets OG5_126721 All targets in OG5_126721
Wolbachia endosymbiont of Brugia malayi methionine aminopeptidase Get druggable targets OG5_126721 All targets in OG5_126721
Plasmodium falciparum methionine aminopeptidase 1a, putative Get druggable targets OG5_126721 All targets in OG5_126721
Mycobacterium ulcerans methionine aminopeptidase MapB Get druggable targets OG5_126721 All targets in OG5_126721
Babesia bovis methionine aminopeptidase, putative Get druggable targets OG5_126721 All targets in OG5_126721
Chlamydia trachomatis methionine aminopeptidase Get druggable targets OG5_126721 All targets in OG5_126721
Trypanosoma cruzi metallo- peptidase, Clan MG, Family M24 Get druggable targets OG5_126721 All targets in OG5_126721
Plasmodium vivax methionine aminopeptidase 1a, putative Get druggable targets OG5_126721 All targets in OG5_126721
Plasmodium yoelii methionine aminopeptidase, type I Get druggable targets OG5_126721 All targets in OG5_126721
Trypanosoma congolense metallo- peptidase, Clan MG, Family M24 Get druggable targets OG5_126721 All targets in OG5_126721
Theileria parva methionine aminopeptidase, type I, putative Get druggable targets OG5_126721 All targets in OG5_126721
Plasmodium berghei methionine aminopeptidase 1a, putative Get druggable targets OG5_126721 All targets in OG5_126721
Cryptosporidium hominis methionine aminopeptidase 1 (MetAP 1) (MAP 1) (Peptidase M 1) Get druggable targets OG5_126721 All targets in OG5_126721
Leishmania donovani metallo- peptidase, Clan MG, Family M24 Get druggable targets OG5_126721 All targets in OG5_126721
Plasmodium falciparum methionine aminopeptidase 1b, putative Get druggable targets OG5_126721 All targets in OG5_126721
Theileria parva methionine aminopeptidase, type I, putative Get druggable targets OG5_126721 All targets in OG5_126721
By sequence similarity to non orthologous known druggable targets
Species Potential target Known druggable target Length Alignment span Identity
Toxoplasma gondii methionine aminopeptidase 2, putative methionyl aminopeptidase 1 386 aa 313 aa 20.4 %
Obtained from network model

Ranking Plot

Putative Targets List

Species Potential target Raw Global Species
Echinococcus granulosus tm gpcr rhodopsin 0.0081 1 1
Leishmania major methionine aminopeptidase, putative,metallo-peptidase, Clan MG, Family M24 0.0054 0.4297 0.5
Brugia malayi follicle stimulating hormone receptor 0.0081 1 1
Schistosoma mansoni rhodopsin-like orphan GPCR 0.0081 1 1
Schistosoma mansoni alpha-1 adrenergic receptor 0.0081 1 1
Echinococcus granulosus rhodopsin orphan GPCR 0.0081 1 1
Brugia malayi G-protein coupled receptor 0.0081 1 1
Schistosoma mansoni amine GPCR 0.0081 1 1
Brugia malayi RE15519p 0.0081 1 1
Echinococcus granulosus somatostatin receptor 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Schistosoma mansoni biogenic amine (dopamine) receptor 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Onchocerca volvulus 0.0081 1 0.5
Schistosoma mansoni peptide (FMRFamide/somatostatin)-like receptor 0.0081 1 1
Echinococcus granulosus neuropeptides capa receptor 0.0081 1 1
Trypanosoma cruzi metallo- peptidase, Clan MG, Family M24 0.0054 0.4297 0.5
Echinococcus multilocularis allatostatin A receptor 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Brugia malayi G-protein-linked acetylcholine receptor protein 2, putative 0.0081 1 1
Schistosoma mansoni peptide (FMRFamide/somatostatin)-like receptor 0.0081 1 1
Brugia malayi putative neuropeptide receptor 0.0081 1 1
Echinococcus multilocularis dro:myosuppressin receptor 0.0081 1 1
Mycobacterium leprae PROBABLE METHIONINE AMINOPEPTIDASE MAPB (MAP) (PEPTIDASE M) 0.0034 0 0.5
Echinococcus granulosus rhodopsin orphan GPCR 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Echinococcus granulosus g protein coupled receptor 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Echinococcus multilocularis rhodopsin orphan GPCR 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Brugia malayi AKH receptor 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Onchocerca volvulus 0.0081 1 0.5
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Echinococcus multilocularis g protein linked acetylcholine receptor gar 2a 0.0081 1 1
Echinococcus multilocularis orexin receptor type 2 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Schistosoma mansoni thyrotropin-releasing hormone receptor 0.0081 1 1
Onchocerca volvulus 0.0081 1 0.5
Schistosoma mansoni rhodopsin-like orphan GPCR 0.0081 1 1
Brugia malayi G protein-coupled receptor 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Echinococcus multilocularis g protein linked acetylcholine receptor gar 2a 0.0081 1 1
Brugia malayi G protein-coupled receptor F59B2.13 0.0081 1 1
Brugia malayi neuropeptide F receptor 0.0081 1 1
Brugia malayi Dopamine receptor protein 1, putative (partial) 0.0081 1 1
Loa Loa (eye worm) TYRA-2 protein 0.0081 1 1
Echinococcus multilocularis tm gpcr rhodopsin gpcr rhodopsin superfamily 0.0081 1 1
Echinococcus granulosus pyroglutamylated rfamide peptide receptor 0.0081 1 1
Echinococcus multilocularis 7TM GPCR, rhodopsin 0.0081 1 1
Echinococcus granulosus g protein linked acetylcholine receptor gar 2a 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Echinococcus granulosus neuropeptide s receptor 0.0081 1 1
Onchocerca volvulus 0.0081 1 0.5
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Echinococcus granulosus 7tm_1 domain containing protein 0.0081 1 1
Schistosoma mansoni amine GPCR 0.0081 1 1
Schistosoma mansoni growth hormone secretagogue receptor 0.0081 1 1
Echinococcus multilocularis methionyl aminopeptidase 1 (M24 family) 0.0054 0.4297 0.4297
Brugia malayi Dopamine receptor protein 2 0.0081 1 1
Plasmodium falciparum methionine aminopeptidase 1b, putative 0.0054 0.4297 1
Wolbachia endosymbiont of Brugia malayi methionine aminopeptidase 0.0034 0 0.5
Loa Loa (eye worm) melatonin receptor type 1A 0.0081 1 1
Trypanosoma brucei metallo- peptidase, Clan MG, Family M24 0.0054 0.4297 0.5
Onchocerca volvulus 0.0081 1 0.5
Schistosoma mansoni neuropeptide receptor 0.0081 1 1
Loa Loa (eye worm) neuropeptide F receptor 0.0081 1 1
Brugia malayi ORL1-like opioid receptor 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Echinococcus multilocularis neuropeptide receptor 0.0081 1 1
Brugia malayi neuropeptide F receptor 0.0081 1 1
Brugia malayi GnHR receptor homolog 0.0081 1 1
Echinococcus granulosus thyrotropin releasing hormone receptor 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Echinococcus multilocularis rhodopsin orphan GPCR 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Echinococcus granulosus fmrfamide receptor 0.0081 1 1
Echinococcus multilocularis tachykinin peptides receptor 99D 0.0081 1 1
Onchocerca volvulus 0.0081 1 0.5
Echinococcus multilocularis biogenic amine (5HT) receptor 0.0081 1 1
Echinococcus multilocularis g protein coupled receptor 0.0081 1 1
Mycobacterium ulcerans methionine aminopeptidase 0.0034 0 0.5
Schistosoma mansoni rhodopsin-like orphan GPCR 0.0081 1 1
Echinococcus multilocularis g protein coupled receptor 0.0081 1 1
Echinococcus granulosus tm gpcr rhodopsin 0.0081 1 1
Brugia malayi hypothetical protein 0.0081 1 1
Toxoplasma gondii methionine aminopeptidase 0.0054 0.4297 1
Brugia malayi hypothetical protein 0.0081 1 1
Schistosoma mansoni histamine h1 receptor 0.0081 1 1
Brugia malayi larval opioid receptor 0.0081 1 1
Echinococcus granulosus hypothetical protein 0.0081 1 1
Schistosoma mansoni rhodopsin-like orphan GPCR 0.0081 1 1
Schistosoma mansoni biogenic amine (dopamine) receptor 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Onchocerca volvulus Dopamine\/Ecdysteroid receptor homolog 0.0081 1 0.5
Onchocerca volvulus 0.0081 1 0.5
Echinococcus granulosus neuropeptide FF receptor 2 0.0081 1 1
Brugia malayi Serotonin receptor 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Echinococcus multilocularis somatostatin receptor 0.0081 1 1
Schistosoma mansoni neuropeptide F-like receptor 0.0081 1 1
Echinococcus granulosus rhodopsin orphan GPCR 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Onchocerca volvulus 0.0081 1 0.5
Echinococcus granulosus G protein coupled 5 hydroxytryptamine receptor 0.0081 1 1
Schistosoma mansoni neuropeptide receptor 0.0081 1 1
Brugia malayi G-protein coupled receptor 0.0081 1 1
Echinococcus granulosus serotonin receptor 0.0081 1 1
Brugia malayi Dopamine receptor protein 1 0.0081 1 1
Brugia malayi gonadotropin-releasing hormone receptor 2 0.0081 1 1
Trypanosoma brucei methionine aminopeptidase, putative 0.0054 0.4297 0.5
Schistosoma mansoni peptide (allatostatin)-like receptor 0.0081 1 1
Schistosoma mansoni hypothetical protein 0.0081 1 1
Echinococcus granulosus tm gpcr rhodopsin 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Onchocerca volvulus 0.0081 1 0.5
Brugia malayi sulfakinin receptor protein 0.0081 1 1
Echinococcus granulosus biogenic amine 5HT receptor 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Schistosoma mansoni rhodopsin-like orphan GPCR 0.0081 1 1
Schistosoma mansoni biogenic amine receptor 0.0081 1 1
Echinococcus multilocularis thyrotropin releasing hormone receptor 0.0081 1 1
Echinococcus granulosus G protein coupled receptor 139 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Echinococcus multilocularis G protein coupled 5 hydroxytryptamine receptor 0.0081 1 1
Echinococcus multilocularis fmrfamide receptor 0.0081 1 1
Schistosoma mansoni muscarinic acetylcholine (GAR) receptor 0.0081 1 1
Schistosoma mansoni hypothetical protein 0.0081 1 1
Plasmodium vivax methionine aminopeptidase 1b, putative 0.0054 0.4297 1
Echinococcus multilocularis G protein coupled receptor 139 0.0081 1 1
Brugia malayi hypothetical protein 0.0081 1 1
Echinococcus multilocularis neuropeptides capa receptor 0.0081 1 1
Brugia malayi hypothetical protein 0.0081 1 1
Loa Loa (eye worm) neuropeptide F receptor 0.0081 1 1
Loa Loa (eye worm) gonadotropin-releasing hormone receptor 2 0.0081 1 1
Loa Loa (eye worm) follicle stimulating hormone receptor 0.0081 1 1
Echinococcus granulosus rhodopsin orphan GPCR 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Onchocerca volvulus 0.0081 1 0.5
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Loa Loa (eye worm) G-protein-linked acetylcholine receptor protein 2 0.0081 1 1
Echinococcus multilocularis tm gpcr rhodopsin gpcr rhodopsin superfamily 0.0081 1 1
Brugia malayi hypothetical protein 0.0081 1 1
Brugia malayi putative neuropeptide receptor NPR1 0.0081 1 1
Mycobacterium leprae PROBABLE METHIONINE AMINOPEPTIDASE MAPA (MAP) (PEPTIDASE M) (MetAP) 0.0034 0 0.5
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Trypanosoma cruzi metallo- peptidase, Clan MG, Family M24 0.0054 0.4297 0.5
Schistosoma mansoni biogenic amine (5HT) receptor 0.0081 1 1
Schistosoma mansoni biogenic amine (dopamine) receptor 0.0081 1 1
Schistosoma mansoni opsin-like receptor 0.0081 1 1
Echinococcus multilocularis neuropeptides capa receptor 0.0081 1 1
Echinococcus multilocularis rhodopsin orphan GPCR 0.0081 1 1
Onchocerca volvulus 0.0081 1 0.5
Trypanosoma brucei methionine aminopeptidase, type I, putative 0.0054 0.4297 0.5
Schistosoma mansoni hypothetical protein 0.0081 1 1
Echinococcus multilocularis rhodopsin orphan GPCR 0.0081 1 1
Echinococcus multilocularis pyroglutamylated rfamide peptide receptor 0.0081 1 1
Loa Loa (eye worm) unidentified vitellogenin-linked transcript protein 6 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Echinococcus granulosus g protein coupled receptor 0.0081 1 1
Schistosoma mansoni biogenic amine (octopamine/dopamine) receptor 0.0081 1 1
Schistosoma mansoni neuropeptide receptor 0.0081 1 1
Echinococcus granulosus 7TM GPCR rhodopsin 0.0081 1 1
Schistosoma mansoni peptide (FMRFamide/neurokinin-3)-like receptor 0.0081 1 1
Echinococcus granulosus peptide allatostatin:somatostatin 0.0081 1 1
Echinococcus granulosus neuropeptide receptor 0.0081 1 1
Echinococcus multilocularis rhodopsin orphan GPCR 0.0081 1 1
Schistosoma mansoni rhodopsin-like orphan GPCR 0.0081 1 1
Onchocerca volvulus 0.0081 1 0.5
Brugia malayi Serotonin/octopamine receptor family protein 7 0.0081 1 1
Onchocerca volvulus 0.0081 1 0.5
Loa Loa (eye worm) G-protein coupled receptor 0.0081 1 1
Loa Loa (eye worm) G-protein coupled receptor 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Brugia malayi Unidentified vitellogenin-linked transcript protein 6, putative 0.0081 1 1
Echinococcus multilocularis growth hormone secretagogue receptor type 1 0.0081 1 1
Schistosoma mansoni neuropeptide f receptor 76f 0.0081 1 1
Echinococcus granulosus tachykinin peptides receptor 99D 0.0081 1 1
Schistosoma mansoni rhodopsin-like orphan GPCR 0.0081 1 1
Echinococcus granulosus g-protein coupled receptor 0.0081 1 1
Mycobacterium tuberculosis Methionine aminopeptidase MapA (map) (peptidase M) (MetAP) 0.0034 0 0.5
Echinococcus granulosus neuropeptide receptor A26 0.0081 1 1
Echinococcus multilocularis peptide (allatostatin:somatostatin) 0.0081 1 1
Echinococcus granulosus g protein linked acetylcholine receptor gar 2a 0.0081 1 1
Echinococcus granulosus rhodopsin orphan GPCR 0.0081 1 1
Schistosoma mansoni ancient conserved domain protein 2 (cyclin m2) 0.0081 1 1
Chlamydia trachomatis methionine aminopeptidase 0.0034 0 0.5
Onchocerca volvulus Neuropeptide F receptor homolog 0.0081 1 0.5
Echinococcus granulosus rhodopsin orphan GPCR 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Schistosoma mansoni adenoreceptor 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Echinococcus granulosus sex peptide receptor 0.0081 1 1
Schistosoma mansoni hypothetical protein 0.0081 1 1
Echinococcus granulosus orexin receptor type 2 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Schistosoma mansoni amine GPCR 0.0081 1 1
Schistosoma mansoni neuropeptide receptor 0.0081 1 1
Echinococcus granulosus dro:myosuppressin receptor 0.0081 1 1
Echinococcus multilocularis serotonin receptor 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Echinococcus multilocularis tm gpcr rhodopsin gpcr rhodopsin superfamily 0.0081 1 1
Echinococcus multilocularis neuropeptide Y receptor 0.0081 1 1
Schistosoma mansoni biogenic amine receptor 0.0081 1 1
Echinococcus multilocularis neuropeptide receptor A26 0.0081 1 1
Echinococcus granulosus neuropeptide receptor 0.0081 1 1
Echinococcus multilocularis rhodopsin orphan GPCR 0.0081 1 1
Echinococcus granulosus neuropeptide Y receptor 0.0081 1 1
Onchocerca volvulus 0.0081 1 0.5
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Loa Loa (eye worm) 5-hydroxytryptamine 2C receptor 0.0081 1 1
Echinococcus multilocularis rhodopsin orphan GPCR 0.0081 1 1
Mycobacterium tuberculosis Methionine aminopeptidase MapB (map) (peptidase M) 0.0034 0 0.5
Schistosoma mansoni histamine-responsive GPCR (AAF21638) 0.0081 1 1
Echinococcus multilocularis rhodopsin orphan GPCR 0.0081 1 1
Schistosoma mansoni neuropeptide F-like receptor 0.0081 1 1
Echinococcus granulosus neuropeptide Y receptor 0.0081 1 1
Brugia malayi hypothetical protein 0.0081 1 1
Echinococcus multilocularis neuropeptide FF receptor 2 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Echinococcus multilocularis g protein coupled receptor 0.0081 1 1
Brugia malayi Melatonin receptor type 1A 0.0081 1 1
Mycobacterium ulcerans methionine aminopeptidase MapB 0.0034 0 0.5
Echinococcus multilocularis neuropeptide Y receptor 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Schistosoma mansoni opsin-like receptor 0.0081 1 1
Schistosoma mansoni myosin xvIII 0.0081 1 1
Echinococcus granulosus neuropeptides capa receptor 0.0081 1 1
Echinococcus granulosus allatostatin A receptor 0.0081 1 1
Echinococcus multilocularis G-protein coupled receptor, putative 0.0081 1 1
Echinococcus granulosus alpha 1A adrenergic receptor 0.0081 1 1
Echinococcus multilocularis alpha 1A adrenergic receptor 0.0081 1 1
Brugia malayi hypothetical protein 0.0081 1 1
Schistosoma mansoni amine GPCR 0.0081 1 1
Echinococcus multilocularis neuropeptide s receptor 0.0081 1 1
Brugia malayi Serotonin receptor 0.0081 1 1
Schistosoma mansoni opsin-like receptor 0.0081 1 1
Echinococcus multilocularis g-protein coupled receptor 0.0081 1 1
Schistosoma mansoni biogenic amine receptor 0.0081 1 1
Brugia malayi Tachykinin-like peptides receptor 99D 0.0081 1 1
Schistosoma mansoni amine GPCR 0.0081 1 1
Brugia malayi Dopamine receptor 0.0081 1 1
Echinococcus granulosus g protein coupled receptor 0.0081 1 1
Echinococcus multilocularis sex peptide receptor 0.0081 1 1
Echinococcus multilocularis neuropeptide receptor 0.0081 1 1
Echinococcus multilocularis serotonin receptor 0.0081 1 1
Onchocerca volvulus 0.0081 1 0.5
Schistosoma mansoni rhodopsin-like orphan GPCR 0.0081 1 1
Onchocerca volvulus 0.0081 1 0.5
Onchocerca volvulus 0.0081 1 0.5
Treponema pallidum methionine aminopeptidase (map) 0.0034 0 0.5
Echinococcus granulosus biogenic amine 5HT receptor 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Loa Loa (eye worm) hypothetical protein 0.0081 1 1
Echinococcus granulosus rhodopsin orphan GPCR 0.0081 1 1
Schistosoma mansoni biogenic amine (5HT) receptor 0.0081 1 1
Echinococcus multilocularis fmrfamide receptor 0.0081 1 1
Brugia malayi hypothetical protein 0.0081 1 1
Schistosoma mansoni rhodopsin-like orphan GPCR 0.0081 1 1
Brugia malayi hypothetical protein 0.0081 1 1
Schistosoma mansoni peptide (allatostatin/somatostatin)-like receptor 0.0081 1 1
Echinococcus granulosus growth hormone secretagogue receptor type 1 0.0081 1 1

Activities

Activity type Activity value Assay description Source Reference
Activity (functional) > 90 % Antiproliferative activity against HUVEC at 20 uM after 30 hrs by [3H]-thymidine incorporation assay relative to control ChEMBL. 23634668
EC50 (binding) = 0.28 uM Inhibition of human methionine aminopeptidase 1 in presence of Co2+ ChEMBL. 23634668
EC50 (functional) = 4.3 uM Antiproliferative activity against HUVEC after 30 hrs by [3H]-thymidine incorporation assay ChEMBL. 23634668
EC50 (binding) > 100 uM Inhibition of human methionine aminopeptidase 1 in presence of Zn2+ ChEMBL. 23634668
EC50 (binding) > 200 uM Inhibition of human methionine aminopeptidase 1 in presence of Mn2+ ChEMBL. 23634668
IC50 (binding) = 2 uM Inhibition of human recombinant full-length cytosolic METAP1 expressed in Escherichia coli BL21(DE3) using Met-Pro-p-nitroanilide as substrate after 20 mins by spectrophotometric analysis in presence of Bacillus coagulans GST-tagged proline iminopeptidase ChEMBL. 23507151
IC50 (binding) > 100 uM Inhibition of human recombinant GST-6XHis-tagged full-length cytosolic METAP2 expressed in cabbage looper BTI-TN-5B1-4 cells using Met-Pro-p-nitroanilide as substrate after 20 mins by spectrophotometric analysis in presence of Bacillus coagulans GST-tagged proline iminopeptidase ChEMBL. 23507151
Inhibition (binding) > 30 % Inhibition of human methionine aminopeptidase 1 at 100 uM relative to control ChEMBL. 23634668

Phenotypes

Whole-cell/tissue/organism interactions

Species name Source Reference Is orphan
Homo sapiens ChEMBL23 23634668

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

2 literature references were collected for this gene.

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