Detailed information for compound 270689

Basic information

Technical information
  • Name: Unnamed compound
  • MW: 605.609 | Formula: C26H22F3N5O5S2
  • H donors: 4 H acceptors: 6 LogP: 4.25 Rotable bonds: 8
    Rule of 5 violations (Lipinski): 2
  • SMILES: OC(=O)C(F)(F)F.Cc1sc(c(n1)c1cccc(c1)C(=N)N)C(=O)Nc1ccc(cc1)c1ccccc1S(=O)(=O)N
  • InChi: 1S/C24H21N5O3S2.C2HF3O2/c1-14-28-21(16-5-4-6-17(13-16)23(25)26)22(33-14)24(30)29-18-11-9-15(10-12-18)19-7-2-3-8-20(19)34(27,31)32;3-2(4,5)1(6)7/h2-13H,1H3,(H3,25,26)(H,29,30)(H2,27,31,32);(H,6,7)
  • InChiKey: MJPRHOCGAAJSMO-UHFFFAOYSA-N  


Substructure search Similarity search

Network

Hover on a compound node to display the structore

Synonyms

No synonyms found for this compound

Targets

Known targets for this compound

Species Target name Source Bibliographic reference
Homo sapiens protease, serine, 2 (trypsin 2) References
Homo sapiens protease, serine, 3 Starlite/ChEMBL References
Oryctolagus cuniculus Coagulation factor X Starlite/ChEMBL References
Homo sapiens coagulation factor X Starlite/ChEMBL References
Homo sapiens coagulation factor II (thrombin) Starlite/ChEMBL References
Homo sapiens protease, serine, 1 (trypsin 1) References

Predicted pathogen targets for this compound

By orthology
Species Potential target Known druggable target/s Ortholog Group
Onchocerca volvulus Get druggable targets OG5_126639 All targets in OG5_126639
Schistosoma japonicum ko:K09639 transmembrane protease, serine 8, putative Get druggable targets OG5_126639 All targets in OG5_126639
Loa Loa (eye worm) hypothetical protein Get druggable targets OG5_126639 All targets in OG5_126639
Brugia malayi Trypsin family protein Get druggable targets OG5_126639 All targets in OG5_126639
Schistosoma japonicum ko:K09639 transmembrane protease, serine 8, putative Get druggable targets OG5_126639 All targets in OG5_126639
Schistosoma mansoni subfamily S1A unassigned peptidase (S01 family) Get druggable targets OG5_126639 All targets in OG5_126639
Schistosoma mansoni subfamily S1A unassigned peptidase (S01 family) Get druggable targets OG5_126639 All targets in OG5_126639
Loa Loa (eye worm) hypothetical protein Get druggable targets OG5_126639 All targets in OG5_126639
Onchocerca volvulus Get druggable targets OG5_126639 All targets in OG5_126639
By sequence similarity to non orthologous known druggable targets
Species Potential target Known druggable target Length Alignment span Identity
Schistosoma mansoni cercarial elastase (S01 family) protease, serine, 3 261 aa 234 aa 25.2 %
Schistosoma mansoni cercarial elastase (S01 family) protease, serine, 2 (trypsin 2) 247 aa 240 aa 25.8 %
Brugia malayi Trypsin family protein protease, serine, 1 (trypsin 1) 247 aa 287 aa 21.6 %
Obtained from network model

Ranking Plot

Putative Targets List

Species Potential target Raw Global Species
Trypanosoma cruzi oligopeptidase B-like protein, putative 0.0056 0.1236 0.3271
Onchocerca volvulus Arrow homolog 0.0032 0.0519 0.0519
Echinococcus multilocularis beta LACTamase domain containing family member 0.0037 0.0673 0.14
Echinococcus multilocularis Mastin 0.0031 0.0486 0.1011
Brugia malayi beta-lactamase family protein 0.0037 0.0673 0.0673
Onchocerca volvulus 0.0037 0.0673 0.0673
Trypanosoma cruzi hypothetical protein, conserved 0.0037 0.0673 0.1782
Schistosoma mansoni subfamily S1A unassigned peptidase (S01 family) 0.035 1 1
Trypanosoma cruzi hypothetical protein, conserved 0.0037 0.0673 0.1782
Echinococcus multilocularis guanine nucleotide binding protein G(s) subunit 0.0094 0.2354 0.4894
Schistosoma mansoni hypothetical protein 0.0031 0.0486 0.0486
Loa Loa (eye worm) GTP-binding regulatory protein Gs alpha-S chain 0.0094 0.2354 0.2354
Giardia lamblia Alanyl dipeptidyl peptidase 0.0015 0 0.5
Brugia malayi Protein kinase domain containing protein 0.0021 0.0192 0.0192
Echinococcus granulosus glycoprotein Antigen 5 0.0031 0.0486 0.1011
Leishmania major oligopeptidase b 0.0056 0.1236 0.3271
Loa Loa (eye worm) hypothetical protein 0.0026 0.0339 0.0339
Echinococcus granulosus prolyl endopeptidase 0.0142 0.3778 0.7855
Echinococcus multilocularis nicotinic acetylcholine receptor subunit alpha 8 0.008 0.1955 0.4064
Loa Loa (eye worm) hypothetical protein 0.035 1 1
Loa Loa (eye worm) low-density lipoprotein receptor repeat class B containing protein 0.0032 0.0519 0.0519
Mycobacterium ulcerans fusion of enoyl-CoA hydratase, EchA21 and lipase, LipE 0.0037 0.0673 0.2498
Loa Loa (eye worm) hypothetical protein 0.0037 0.0673 0.0673
Schistosoma mansoni tar DNA-binding protein 0.0064 0.1468 0.1468
Echinococcus multilocularis glycoprotein Antigen 5 0.0031 0.0486 0.1011
Trypanosoma brucei oligopeptidase b 0.0056 0.1236 0.3271
Loa Loa (eye worm) hypothetical protein 0.0032 0.0519 0.0519
Entamoeba histolytica dipeptidyl-peptidase, putative 0.0015 0 0.5
Schistosoma mansoni subfamily S1A unassigned peptidase (S01 family) 0.0031 0.0486 0.0486
Schistosoma mansoni family S12 unassigned peptidase (S12 family) 0.0037 0.0673 0.0673
Brugia malayi TAR-binding protein 0.0064 0.1468 0.1468
Onchocerca volvulus 0.0031 0.0486 0.0486
Toxoplasma gondii LsmAD domain-containing protein 0.0026 0.0339 0.0896
Mycobacterium ulcerans lipase LipD 0.0037 0.0673 0.2498
Schistosoma mansoni cercarial elastase (S01 family) 0.0031 0.0486 0.0486
Onchocerca volvulus 0.0031 0.0486 0.0486
Echinococcus multilocularis fibrillin 1 0.0032 0.0519 0.1079
Loa Loa (eye worm) trypsin family protein 0.0031 0.0486 0.0486
Echinococcus granulosus nicotinic acetylcholine receptor a11 subunit 0.008 0.1955 0.4064
Plasmodium vivax ataxin-2 like protein, putative 0.0026 0.0339 0.5029
Entamoeba histolytica hypothetical protein, conserved 0.0015 0 0.5
Echinococcus granulosus Tolloid protein 1 0.0032 0.0519 0.1079
Schistosoma mansoni Guanine nucleotide-binding protein G(s) subunit alpha (Adenylate cyclase-stimulating G alpha protein) 0.0094 0.2354 0.2354
Loa Loa (eye worm) hypothetical protein 0.0031 0.0486 0.0486
Trypanosoma brucei prolyl oligopeptidase, putative 0.0056 0.1236 0.3271
Echinococcus granulosus tissue type plasminogen activator 0.0021 0.0192 0.0398
Schistosoma mansoni subfamily S1A unassigned peptidase (S01 family) 0.0031 0.0486 0.0486
Brugia malayi Calcium binding EGF domain containing protein 0.0032 0.0519 0.0519
Loa Loa (eye worm) MH2 domain-containing protein 0.0121 0.3158 0.3158
Loa Loa (eye worm) hypothetical protein 0.0037 0.0673 0.0673
Loa Loa (eye worm) RNA binding protein 0.0064 0.1468 0.1468
Brugia malayi Trypsin-like protease protein 5 0.0031 0.0486 0.0486
Echinococcus granulosus enteropeptidase 0.0031 0.0486 0.1011
Schistosoma mansoni egf-like domain protein 0.0032 0.0519 0.0519
Brugia malayi Trypsin family protein 0.0031 0.0486 0.0486
Schistosoma mansoni tar DNA-binding protein 0.0064 0.1468 0.1468
Schistosoma mansoni subfamily S1A unassigned peptidase (S01 family) 0.0031 0.0486 0.0486
Onchocerca volvulus 0.0037 0.0673 0.0673
Trichomonas vaginalis penicillin-binding protein, putative 0.0037 0.0673 1
Loa Loa (eye worm) beta-LACTamase domain containing family member 0.0037 0.0673 0.0673
Trypanosoma brucei PAB1-binding protein , putative 0.0026 0.0339 0.0896
Brugia malayi Fibulin-1 precursor 0.0032 0.0519 0.0519
Loa Loa (eye worm) hypothetical protein 0.0032 0.0519 0.0519
Schistosoma mansoni subfamily S1A unassigned peptidase (S01 family) 0.0031 0.0486 0.0486
Leishmania major oligopeptidase B-like protein,serine peptidase, clan SC, family S9A-like protein 0.0056 0.1236 0.3271
Echinococcus multilocularis nicotinic acetylcholine receptor alpha subunit 0.008 0.1955 0.4064
Schistosoma mansoni tar DNA-binding protein 0.0064 0.1468 0.1468
Loa Loa (eye worm) hypothetical protein 0.0032 0.0519 0.0519
Brugia malayi nicotinic acetylcholine receptor alpha subunit, putative 0.008 0.1955 0.1955
Echinococcus granulosus guanine nucleotide binding protein Gs subunit 0.0094 0.2354 0.4894
Loa Loa (eye worm) hypothetical protein 0.0142 0.3778 0.3778
Echinococcus multilocularis guanine nucleotide binding protein G(s) subunit 0.0094 0.2354 0.4894
Schistosoma mansoni cercarial elastase (S01 family) 0.0031 0.0486 0.0486
Schistosoma mansoni family S12 unassigned peptidase (S12 family) 0.0037 0.0673 0.0673
Echinococcus multilocularis enteropeptidase 0.0031 0.0486 0.1011
Echinococcus granulosus beta LACTamase domain containing family member 0.0037 0.0673 0.14
Mycobacterium ulcerans beta-lactamase 0.0037 0.0673 0.2498
Trypanosoma cruzi prolyl endopeptidase 0.0142 0.3778 1
Mycobacterium ulcerans protease II (oligopeptidase B), PtrB 0.0056 0.1236 1
Loa Loa (eye worm) hypothetical protein 0.0032 0.0519 0.0519
Loa Loa (eye worm) bone morphogenetic protein 1b 0.0032 0.0519 0.0519
Onchocerca volvulus 0.0031 0.0486 0.0486
Brugia malayi Kringle domain containing protein 0.0021 0.0192 0.0192
Brugia malayi MH2 domain containing protein 0.0121 0.3158 0.3158
Trypanosoma cruzi serine peptidase, clan SC, family S9A-like protein, putative 0.0056 0.1236 0.3271
Schistosoma mansoni Guanine nucleotide-binding protein G(s) subunit alpha (Adenylate cyclase-stimulating G alpha protein) 0.0094 0.2354 0.2354
Echinococcus granulosus guanine nucleotide binding protein Gs subunit 0.0094 0.2354 0.4894
Loa Loa (eye worm) transcription factor SMAD2 0.0121 0.3158 0.3158
Onchocerca volvulus 0.035 1 1
Loa Loa (eye worm) hypothetical protein 0.0031 0.0486 0.0486
Entamoeba histolytica prolyl oligopeptidase family protein 0.0015 0 0.5
Trypanosoma brucei prolyl endopeptidase 0.0142 0.3778 1
Brugia malayi beta-lactamase 0.0037 0.0673 0.0673
Entamoeba histolytica prolyl oligopeptidase family protein 0.0015 0 0.5
Echinococcus multilocularis prolyl endopeptidase 0.0142 0.3778 0.7855
Echinococcus granulosus subfamily S1A unassigned peptidase S01 family 0.0031 0.0486 0.1011
Plasmodium falciparum cysteine repeat modular protein 1 0.0021 0.0192 0.5656
Onchocerca volvulus Prolyl endopeptidase homolog 0.0142 0.3778 0.3778
Onchocerca volvulus 0.0031 0.0486 0.0486
Brugia malayi hypothetical protein 0.0031 0.0486 0.0486
Echinococcus granulosus tar DNA binding protein 0.0064 0.1468 0.3052
Brugia malayi hypothetical protein 0.0017 0.0062 0.0062
Loa Loa (eye worm) hypothetical protein 0.0037 0.0673 0.0673
Schistosoma mansoni tar DNA-binding protein 0.0064 0.1468 0.1468
Echinococcus multilocularis transmembrane protease serine 3 0.0031 0.0486 0.1011
Trichomonas vaginalis esterase, putative 0.0037 0.0673 1
Mycobacterium tuberculosis Probable peptidase 0.0056 0.1236 0.0935
Schistosoma mansoni cercarial elastase (S01 family) 0.0031 0.0486 0.0486
Loa Loa (eye worm) RNA recognition domain-containing protein domain-containing protein 0.0064 0.1468 0.1468
Trypanosoma cruzi PAB1-binding protein , putative 0.0026 0.0339 0.0896
Mycobacterium ulcerans esterase/lipase LipP 0.0037 0.0673 0.2498
Plasmodium vivax cysteine repeat modular protein 1, putative 0.0021 0.0192 0.2845
Schistosoma mansoni cercarial elastase (S01 family) 0.0031 0.0486 0.0486
Onchocerca volvulus 0.0319 0.9071 0.9071
Echinococcus granulosus nicotinic acetylcholine receptor alpha subunit 0.008 0.1955 0.4064
Brugia malayi Trypsin family protein 0.0031 0.0486 0.0486
Brugia malayi hypothetical protein 0.0026 0.0339 0.0339
Trichomonas vaginalis D-aminoacylase, putative 0.0037 0.0673 1
Giardia lamblia Alanyl dipeptidyl peptidase 0.0015 0 0.5
Echinococcus multilocularis tissue type plasminogen activator 0.0021 0.0192 0.0398
Echinococcus multilocularis nicotinic acetylcholine receptor a11 subunit 0.008 0.1955 0.4064
Plasmodium falciparum ataxin-2 like protein, putative 0.0026 0.0339 1
Entamoeba histolytica prolyl oligopeptidase family protein 0.0015 0 0.5
Schistosoma mansoni cercarial elastase (S01 family) 0.0031 0.0486 0.0486
Brugia malayi Hypothetical 52.5 kDa protein ZK945.1 in chromosome II, putative 0.0037 0.0673 0.0673
Schistosoma mansoni hypothetical protein 0.0021 0.0192 0.0192
Trypanosoma cruzi hypothetical protein, conserved 0.0021 0.0192 0.0507
Loa Loa (eye worm) nicotinic acetylcholine receptor alpha subunit 0.008 0.1955 0.1955
Mycobacterium tuberculosis Probable protease II PtrBb [second part] (oligopeptidase B) 0.0056 0.1236 0.0935
Leishmania major hypothetical protein, conserved 0.0021 0.0192 0.0507
Trichomonas vaginalis penicillin-binding protein, putative 0.0037 0.0673 1
Schistosoma mansoni cercarial elastase (S01 family) 0.0031 0.0486 0.0486
Mycobacterium tuberculosis Probable protease II PtrBa [first part] (oligopeptidase B) 0.0127 0.3336 0.4426
Loa Loa (eye worm) hypothetical protein 0.0031 0.0486 0.0486
Echinococcus granulosus transmembrane protease serine 3 0.0031 0.0486 0.1011
Entamoeba histolytica dipeptidyl-peptidase, putative 0.0015 0 0.5
Schistosoma mansoni subfamily M12A unassigned peptidase (M12 family) 0.0032 0.0519 0.0519
Brugia malayi GTP-binding regulatory protein Gs alpha-S chain, putative 0.0094 0.2354 0.2354
Mycobacterium ulcerans hypothetical protein 0.0037 0.0673 0.2498
Toxoplasma gondii ABC1 family protein 0.0037 0.0673 0.1782
Schistosoma mansoni prolyl oligopeptidase (S09 family) 0.0142 0.3778 0.3778
Loa Loa (eye worm) hypothetical protein 0.0031 0.0486 0.0486
Trichomonas vaginalis D-aminoacylase, putative 0.0037 0.0673 1
Toxoplasma gondii calcium binding egf domain-containing protein 0.0032 0.0519 0.1373
Schistosoma mansoni subfamily S1A unassigned peptidase (S01 family) 0.0031 0.0486 0.0486
Loa Loa (eye worm) TAR-binding protein 0.0064 0.1468 0.1468
Brugia malayi beta-lactamase family protein 0.0037 0.0673 0.0673
Schistosoma mansoni hypothetical protein 0.0031 0.0486 0.0486
Mycobacterium tuberculosis Possible penicillin-binding protein 0.0239 0.6688 1
Echinococcus multilocularis geminin 0.0176 0.481 1
Schistosoma mansoni cercarial elastase (S01 family) 0.0031 0.0486 0.0486
Loa Loa (eye worm) hypothetical protein 0.008 0.1955 0.1955
Schistosoma mansoni tar DNA-binding protein 0.0064 0.1468 0.1468
Brugia malayi prolyl oligopeptidase family protein 0.0142 0.3778 0.3778
Loa Loa (eye worm) beta-lactamase 0.0037 0.0673 0.0673
Onchocerca volvulus 0.0037 0.0673 0.0673
Onchocerca volvulus 0.0031 0.0486 0.0486
Brugia malayi Trypsin family protein 0.0031 0.0486 0.0486
Schistosoma mansoni cercarial elastase (S01 family) 0.0031 0.0486 0.0486
Trypanosoma cruzi oligopeptidase b 0.0056 0.1236 0.3271
Loa Loa (eye worm) hypothetical protein 0.035 1 1
Schistosoma mansoni prolyl oligopeptidase (S09 family) 0.0142 0.3778 0.3778
Echinococcus granulosus Mastin 0.0031 0.0486 0.1011
Brugia malayi Chymotrypsin-like protease CTRL-1 precursor 0.0031 0.0486 0.0486
Trypanosoma brucei serine peptidase, clan SC, family S9A-like protein 0.0056 0.1236 0.3271
Schistosoma mansoni Guanine nucleotide-binding protein G(s) subunit alpha (Adenylate cyclase-stimulating G alpha protein) 0.0094 0.2354 0.2354
Loa Loa (eye worm) hypothetical protein 0.0021 0.0192 0.0192
Schistosoma mansoni aminopeptidase PILS (M01 family) 0.0031 0.0486 0.0486
Echinococcus multilocularis Peptidase S1 S6, chymotrypsin Hap 0.0031 0.0486 0.1011
Schistosoma mansoni subfamily S1A unassigned peptidase (S01 family) 0.035 1 1
Toxoplasma gondii calcium binding egf domain-containing protein 0.0032 0.0519 0.1373
Trypanosoma cruzi PAB1-binding protein , putative 0.0026 0.0339 0.0896
Schistosoma mansoni hypothetical protein 0.0176 0.481 0.481
Plasmodium falciparum ataxin-2 like protein, putative 0.0026 0.0339 1
Echinococcus multilocularis laminin 0.0032 0.0519 0.1079
Echinococcus granulosus laminin 0.0032 0.0519 0.1079
Echinococcus granulosus nicotinic acetylcholine receptor subunit alpha 8 0.008 0.1955 0.4064
Loa Loa (eye worm) hypothetical protein 0.0037 0.0673 0.0673
Toxoplasma gondii prolyl endopeptidase 0.0142 0.3778 1
Leishmania major prolyl oligopeptidase, putative,serine peptidase clan SC, family S9A, putative 0.0142 0.3778 1
Trypanosoma brucei hypothetical protein, conserved 0.0037 0.0673 0.1782
Loa Loa (eye worm) hypothetical protein 0.0037 0.0673 0.0673
Onchocerca volvulus Putative nachr subunit 0.008 0.1955 0.1955
Loa Loa (eye worm) multiple epidermal growth factor-like domains 6 0.0032 0.0519 0.0519
Mycobacterium leprae PROBABLE PROTEASE II PTRBB (OLIGOPEPTIDASE B) 0.0056 0.1236 1
Loa Loa (eye worm) TK/ROR protein kinase 0.0021 0.0192 0.0192
Echinococcus granulosus Peptidase S1 S6 chymotrypsin Hap 0.0031 0.0486 0.1011
Schistosoma mansoni hypothetical protein 0.0176 0.481 0.481
Onchocerca volvulus 0.0021 0.0192 0.0192
Echinococcus multilocularis tar DNA binding protein 0.0064 0.1468 0.3052
Echinococcus multilocularis subfamily S1A unassigned peptidase (S01 family) 0.0031 0.0486 0.1011
Loa Loa (eye worm) hypothetical protein 0.0037 0.0673 0.0673
Plasmodium vivax hypothetical protein, conserved 0.0037 0.0673 1
Trichomonas vaginalis D-aminoacylase, putative 0.0037 0.0673 1
Brugia malayi RNA binding protein 0.0064 0.1468 0.1468
Loa Loa (eye worm) hypothetical protein 0.0032 0.0519 0.0519
Brugia malayi Low-density lipoprotein receptor repeat class B containing protein 0.0032 0.0519 0.0519
Brugia malayi RNA recognition motif domain containing protein 0.0064 0.1468 0.1468
Leishmania major hypothetical protein, conserved 0.0037 0.0673 0.1782
Leishmania major hypothetical protein, conserved 0.0026 0.0339 0.0896
Schistosoma mansoni cercarial elastase (S01 family) 0.0031 0.0486 0.0486
Trypanosoma cruzi oligopeptidase b 0.0056 0.1236 0.3271
Schistosoma mansoni cercarial elastase (S01 family) 0.0031 0.0486 0.0486
Loa Loa (eye worm) hypothetical protein 0.0031 0.0486 0.0486
Toxoplasma gondii kringle domain-containing protein 0.0021 0.0192 0.0507
Echinococcus multilocularis Tolloid protein 1 0.0032 0.0519 0.1079
Schistosoma mansoni cercarial elastase (S01 family) 0.0031 0.0486 0.0486
Echinococcus granulosus geminin 0.0176 0.481 1

Activities

Activity type Activity value Assay description Source Reference
ID50 (functional) = 0.5 uM hr-1 kg-1 Antithrombotic efficacy was determined in a rabbit (A-V) shunt model ChEMBL. 11266160
Ki (binding) = 0.06 nM Binding affinity towards human Serine protease FXa ChEMBL. 11266160
Ki (binding) = 0.06 nM Binding affinity towards human Serine protease FXa ChEMBL. 11266160
Ki (binding) = 0.08 nM Binding affinity towards Rabbit Coagulation factor X in a rabbit arterio-venous (A-V) shunt model ChEMBL. 11266160
Ki (binding) = 0.08 nM Binding affinity towards Rabbit Coagulation factor X in a rabbit arterio-venous (A-V) shunt model ChEMBL. 11266160
Ki (binding) = 60 nM Binding affinity towards human trypsin ChEMBL. 11266160
Ki (binding) = 60 nM Binding affinity towards human trypsin ChEMBL. 11266160
Ki (binding) = 1250 nM Binding affinity towards human thrombin ChEMBL. 11266160
Ki (binding) = 1250 nM Binding affinity towards human thrombin ChEMBL. 11266160

Phenotypes

Whole-cell/tissue/organism interactions

We have no records of whole-cell/tissue assays done with this compound What does this mean?

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

1 literature reference was collected for this gene.

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