Detailed information for compound 1442990

Basic information

Technical information
  • TDR Targets ID: 1442990
  • Name: N-[(5-bromo-2-methoxyphenyl)methyl]-5-[(4-met hylphenyl)methyl]-4-oxo-7,8-dihydro-6H-pyrazo lo[5,1-c][1,4]diazepine-2-carboxamide
  • MW: 497.384 | Formula: C24H25BrN4O3
  • H donors: 1 H acceptors: 3 LogP: 3.72 Rotable bonds: 7
    Rule of 5 violations (Lipinski): 1
  • SMILES: COc1ccc(cc1CNC(=O)c1nn2c(c1)C(=O)N(CCC2)Cc1ccc(cc1)C)Br
  • InChi: 1S/C24H25BrN4O3/c1-16-4-6-17(7-5-16)15-28-10-3-11-29-21(24(28)31)13-20(27-29)23(30)26-14-18-12-19(25)8-9-22(18)32-2/h4-9,12-13H,3,10-11,14-15H2,1-2H3,(H,26,30)
  • InChiKey: GZFUWNDINQLKDW-UHFFFAOYSA-N  

Network

Hover on a compound node to display the structore

Synonyms

  • N-[(5-bromo-2-methoxy-phenyl)methyl]-5-[(4-methylphenyl)methyl]-4-oxo-7,8-dihydro-6H-pyrazolo[5,1-c][1,4]diazepine-2-carboxamide
  • N-(5-bromo-2-methoxy-benzyl)-4-keto-5-(4-methylbenzyl)-7,8-dihydro-6H-pyrazolo[1,5-a][1,4]diazepine-2-carboxamide
  • G542-0620
  • NCGC00131558-01

Targets

Known targets for this compound

Species Target name Source Bibliographic reference
Homo sapiens tumor protein p53 Starlite/ChEMBL No references
Homo sapiens SMAD family member 2 Starlite/ChEMBL No references
Homo sapiens TAR DNA binding protein Starlite/ChEMBL No references
Homo sapiens lamin A/C Starlite/ChEMBL No references
Homo sapiens glucagon-like peptide 1 receptor Starlite/ChEMBL No 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_128723 All targets in OG5_128723
Loa Loa (eye worm) intermediate filament tail domain-containing protein Get druggable targets OG5_128723 All targets in OG5_128723
Echinococcus multilocularis tar DNA binding protein Get druggable targets OG5_132461 All targets in OG5_132461
Loa Loa (eye worm) MH2 domain-containing protein Get druggable targets OG5_131716 All targets in OG5_131716
Echinococcus multilocularis musashi Get druggable targets OG5_128723 All targets in OG5_128723
Loa Loa (eye worm) hypothetical protein Get druggable targets OG5_128723 All targets in OG5_128723
Schistosoma japonicum ko:K07611 lamin, putative Get druggable targets OG5_128723 All targets in OG5_128723
Schistosoma japonicum expressed protein Get druggable targets OG5_128723 All targets in OG5_128723
Onchocerca volvulus Get druggable targets OG5_128723 All targets in OG5_128723
Echinococcus granulosus lamin dm0 Get druggable targets OG5_128723 All targets in OG5_128723
Schistosoma japonicum TAR DNA-binding protein 43, putative Get druggable targets OG5_132461 All targets in OG5_132461
Echinococcus multilocularis cytoplasmic intermediate filament protein Get druggable targets OG5_128723 All targets in OG5_128723
Schistosoma mansoni tar DNA-binding protein Get druggable targets OG5_132461 All targets in OG5_132461
Echinococcus granulosus tar DNA binding protein Get druggable targets OG5_132461 All targets in OG5_132461
Loa Loa (eye worm) RNA binding protein Get druggable targets OG5_132461 All targets in OG5_132461
Echinococcus multilocularis lamin dm0 Get druggable targets OG5_128723 All targets in OG5_128723
Brugia malayi RNA recognition motif domain containing protein Get druggable targets OG5_132461 All targets in OG5_132461
Schistosoma mansoni tar DNA-binding protein Get druggable targets OG5_132461 All targets in OG5_132461
Schistosoma mansoni lamin Get druggable targets OG5_128723 All targets in OG5_128723
Echinococcus multilocularis tumor protein p63 Get druggable targets OG5_140038 All targets in OG5_140038
Brugia malayi intermediate filament protein Get druggable targets OG5_128723 All targets in OG5_128723
Schistosoma mansoni intermediate filament proteins Get druggable targets OG5_128723 All targets in OG5_128723
Loa Loa (eye worm) hypothetical protein Get druggable targets OG5_128723 All targets in OG5_128723
Loa Loa (eye worm) TAR-binding protein Get druggable targets OG5_132461 All targets in OG5_132461
Schistosoma mansoni tar DNA-binding protein Get druggable targets OG5_132461 All targets in OG5_132461
Schistosoma japonicum expressed protein Get druggable targets OG5_128723 All targets in OG5_128723
Brugia malayi RNA binding protein Get druggable targets OG5_132461 All targets in OG5_132461
Loa Loa (eye worm) hypothetical protein Get druggable targets OG5_128723 All targets in OG5_128723
Echinococcus granulosus lamin Get druggable targets OG5_128723 All targets in OG5_128723
Schistosoma japonicum TAR DNA-binding protein 43, putative Get druggable targets OG5_132461 All targets in OG5_132461
Schistosoma mansoni lamin Get druggable targets OG5_128723 All targets in OG5_128723
Brugia malayi MH2 domain containing protein Get druggable targets OG5_131716 All targets in OG5_131716
Brugia malayi Intermediate filament tail domain containing protein Get druggable targets OG5_128723 All targets in OG5_128723
Loa Loa (eye worm) RNA recognition domain-containing protein domain-containing protein Get druggable targets OG5_132461 All targets in OG5_132461
Onchocerca volvulus Get druggable targets OG5_128723 All targets in OG5_128723
Loa Loa (eye worm) transcription factor SMAD2 Get druggable targets OG5_131716 All targets in OG5_131716
Brugia malayi TAR-binding protein Get druggable targets OG5_132461 All targets in OG5_132461
Schistosoma mansoni tar DNA-binding protein Get druggable targets OG5_132461 All targets in OG5_132461
Echinococcus granulosus intermediate filament protein Get druggable targets OG5_128723 All targets in OG5_128723
Loa Loa (eye worm) hypothetical protein Get druggable targets OG5_128723 All targets in OG5_128723
Echinococcus granulosus tumor protein p63 Get druggable targets OG5_140038 All targets in OG5_140038
Loa Loa (eye worm) intermediate filament protein Get druggable targets OG5_128723 All targets in OG5_128723
Schistosoma japonicum Lamin-C, putative Get druggable targets OG5_128723 All targets in OG5_128723
Schistosoma japonicum Intermediate filament protein ifa-1, putative Get druggable targets OG5_128723 All targets in OG5_128723
Echinococcus multilocularis lamin Get druggable targets OG5_128723 All targets in OG5_128723
Schistosoma mansoni tar DNA-binding protein Get druggable targets OG5_132461 All targets in OG5_132461
Echinococcus granulosus cytoplasmic intermediate filament protein Get druggable targets OG5_128723 All targets in OG5_128723

By sequence similarity to non orthologous known druggable targets
Species Potential target Known druggable target Length Alignment span Identity
Loa Loa (eye worm) pigment dispersing factor receptor c glucagon-like peptide 1 receptor 463 aa 388 aa 25.8 %
Brugia malayi MH2 domain containing protein SMAD family member 2 467 aa 405 aa 31.6 %

Obtained from network model

Ranking Plot


Putative Targets List


Species Potential target Raw Global Species
Brugia malayi Proteasome A-type and B-type family protein 0.0087 0.097 0.097
Echinococcus granulosus 20S proteasome subunit alpha 6 0.0087 0.097 0.095
Plasmodium falciparum proteasome subunit beta type-4 0.0087 0.097 0.0533
Schistosoma mansoni tar DNA-binding protein 0.0076 0.082 0.08
Brugia malayi proteasome subunit alpha type 6 0.0087 0.097 0.097
Leishmania major proteasome alpha 1 subunit, putative 0.0087 0.097 0.0533
Toxoplasma gondii adhesion regulating molecule region protein, putative 0.0097 0.1109 0.0154
Leishmania major proteasome beta 2 subunit, putative 0.0087 0.097 0.0533
Brugia malayi Proteasome subunit alpha type 7-1 0.0087 0.097 0.097
Leishmania major proteasome alpha 2 subunit, putative 0.0087 0.097 0.0533
Schistosoma mansoni tar DNA-binding protein 0.0076 0.082 0.08
Trypanosoma cruzi proteasome subunit beta type-2, putative 0.0162 0.2007 0.1148
Mycobacterium ulcerans proteasome PrcB 0.0737 1 1
Brugia malayi proteasome subunit alpha type 1 0.0087 0.097 0.097
Trypanosoma cruzi 20S proteasome subunit 0.0162 0.2007 0.1148
Loa Loa (eye worm) proteasome subunit alpha type 7-1 0.0087 0.097 0.097
Schistosoma mansoni proteasome catalytic subunit 3 (T01 family) 0.0737 1 1
Echinococcus multilocularis proteasome subunit alpha type 2 0.0087 0.097 0.095
Echinococcus granulosus intermediate filament protein 0.0033 0.021 0.0188
Plasmodium falciparum proteasome subunit alpha type-6, putative 0.0087 0.097 0.0533
Echinococcus multilocularis proteasome (prosome, macropain) 0.0737 1 1
Brugia malayi Adhesion regulating molecule conserved region family protein 0.0097 0.1109 0.1109
Schistosoma mansoni proteasome subunit alpha 7 (T01 family) 0.0087 0.097 0.095
Loa Loa (eye worm) proteasome A-type and B-type family protein 0.0087 0.097 0.097
Echinococcus granulosus tar DNA binding protein 0.0076 0.082 0.08
Plasmodium vivax proteasome subunit beta type-1, putative 0.0239 0.3082 0.2339
Echinococcus multilocularis musashi 0.0033 0.021 0.0188
Loa Loa (eye worm) TAR-binding protein 0.0076 0.082 0.082
Echinococcus multilocularis proteasome (prosome macropain) subunit alpha 0.0087 0.097 0.095
Loa Loa (eye worm) latrophilin receptor protein 2 0.0019 0.0022 0.0022
Brugia malayi proteasome subunit beta type 2 0.0162 0.2007 0.2007
Echinococcus multilocularis Proteasome subunit alpha type 7 0.0087 0.097 0.095
Toxoplasma gondii proteasome subunit beta type, putative 0.0737 1 1
Schistosoma mansoni subfamily T1A non-peptidase homologue (T01 family) 0.0087 0.097 0.095
Trichomonas vaginalis Family T1, proteasome beta subunit, threonine peptidase 0.0239 0.3082 0.2339
Echinococcus granulosus proteasome prosome macropain subunit beta 0.0239 0.3082 0.3067
Trichomonas vaginalis Family T1, proteasome beta subunit, threonine peptidase 0.0162 0.2007 0.1148
Plasmodium falciparum proteasome subunit alpha type-7, putative 0.0087 0.097 0.0533
Leishmania major proteasome alpha 7 subunit, putative 0.0087 0.097 0.0533
Schistosoma mansoni proteasome subunit beta 2 (T01 family) 0.0162 0.2007 0.1989
Loa Loa (eye worm) intermediate filament protein 0.0033 0.021 0.021
Loa Loa (eye worm) proteasome subunit alpha type 6 0.0087 0.097 0.097
Echinococcus multilocularis adhesion regulating molecule 1 0.0097 0.1109 0.109
Trypanosoma cruzi proteasome beta 6 subunit, putative 0.0239 0.3082 0.2339
Echinococcus multilocularis proteasome subunit alpha type 6 0.0087 0.097 0.095
Plasmodium falciparum proteasome subunit beta type-6, putative 0.0087 0.097 0.0533
Leishmania major proteasome beta-1 subunit, putative 0.0087 0.097 0.0533
Brugia malayi MH2 domain containing protein 0.0144 0.176 0.176
Wolbachia endosymbiont of Brugia malayi ATP-dependent protease peptidase subunit 0.0087 0.097 0.5
Plasmodium falciparum ATP-dependent protease subunit ClpQ 0.0087 0.097 0.0533
Brugia malayi calcium-independent alpha-latrotoxin receptor 2, putative 0.0019 0.0022 0.0022
Schistosoma mansoni subfamily T1A non-peptidase homologue (T01 family) 0.0087 0.097 0.095
Schistosoma mansoni adhesion regulating molecule 1 (110 kD cell membrane glycoprotein) 0.0097 0.1109 0.109
Leishmania major 20s proteasome beta 7 subunit, (putative) 0.0087 0.097 0.0533
Brugia malayi Intermediate filament tail domain containing protein 0.0033 0.021 0.021
Toxoplasma gondii proteasome subunit beta type 1, putative 0.0239 0.3082 0.2339
Plasmodium vivax proteasome subunit beta type-5, putative 0.0737 1 1
Brugia malayi proteasome subunit beta type 1 0.0239 0.3082 0.3082
Leishmania major proteasome beta 5 subunit, putative 0.0737 1 1
Loa Loa (eye worm) 20S proteasome alpha5 subunit 0.0087 0.097 0.097
Schistosoma mansoni tar DNA-binding protein 0.0076 0.082 0.08
Brugia malayi proteasome subunit alpha type 3 0.0087 0.097 0.097
Schistosoma mansoni hypothetical protein 0.0041 0.0329 0.0308
Echinococcus granulosus subfamily T1A non peptidase ue 0.0087 0.097 0.095
Leishmania major proteasome alpha 3 subunit, putative 0.0087 0.097 0.0533
Trichomonas vaginalis Family T1, proteasome beta subunit, threonine peptidase 0.0737 1 1
Loa Loa (eye worm) hypothetical protein 0.0033 0.021 0.021
Echinococcus granulosus lamin 0.0033 0.021 0.0188
Schistosoma mansoni proteasome subunit alpha 3 (T01 family) 0.0087 0.097 0.095
Echinococcus granulosus adhesion regulating molecule 1 0.0097 0.1109 0.109
Echinococcus granulosus proteasome subunit beta type 6 0.0087 0.097 0.095
Leishmania major proteasome beta 2 subunit, putative 0.0162 0.2007 0.162
Onchocerca volvulus 0.006 0.0587 0.4961
Leishmania major 20s proteasome beta 7 subunit, (putative) 0.0087 0.097 0.0533
Leishmania major 20s proteasome beta 7 subunit, (putative) 0.0087 0.097 0.0533
Plasmodium falciparum proteasome subunit alpha type-1, putative 0.0087 0.097 0.0533
Loa Loa (eye worm) hypothetical protein 0.0041 0.0329 0.0329
Trypanosoma cruzi proteasome subunit beta type-5, putative 0.0737 1 1
Plasmodium falciparum proteasome subunit alpha type-3, putative 0.0087 0.097 0.0533
Brugia malayi proteasome subunit alpha type 2 0.0087 0.097 0.097
Plasmodium falciparum proteasome subunit beta type-3, putative 0.0087 0.097 0.0533
Echinococcus granulosus proteasome subunit alpha type 6 0.0087 0.097 0.095
Leishmania major 20s proteasome beta 7 subunit, (putative) 0.0087 0.097 0.0533
Loa Loa (eye worm) RNA binding protein 0.0076 0.082 0.082
Loa Loa (eye worm) proteasome subunit alpha type 2 0.0087 0.097 0.097
Loa Loa (eye worm) RNA recognition domain-containing protein domain-containing protein 0.0076 0.082 0.082
Leishmania major hs1vu complex proteolytic subunit-like,hs1vu complex proteolytic subunit-like, threonine peptidase, Clan T(1), family T1B 0.0087 0.097 0.0533
Schistosoma mansoni proteasome subunit beta 2 (T01 family) 0.0162 0.2007 0.1989
Schistosoma mansoni cellular tumor antigen P53 0.006 0.0587 0.0566
Plasmodium falciparum proteasome subunit alpha type-4, putative 0.0087 0.097 0.0533
Schistosoma mansoni tar DNA-binding protein 0.0076 0.082 0.08
Schistosoma mansoni proteasome catalytic subunit 2 (T01 family) 0.0087 0.097 0.095
Schistosoma mansoni proteasome subunit beta 1 (T01 family) 0.0239 0.3082 0.3067
Trypanosoma brucei proteasome subunit beta type-5, putative 0.0737 1 1
Echinococcus multilocularis proteasome (prosome, macropain) subunit, beta 0.0162 0.2007 0.1989
Leishmania major proteasome alpha 5 subunit, putative,20S proteasome subunit alpha 5, (putative) 0.0087 0.097 0.0533
Toxoplasma gondii proteasome subunit beta type 2, putative 0.0162 0.2007 0.1148
Mycobacterium leprae proteasome (beta subunit) PrcB 0.0737 1 1
Brugia malayi Latrophilin receptor protein 2 0.0019 0.0022 0.0022
Echinococcus granulosus proteasome prosome macropain subunit beta type 0.0087 0.097 0.095
Loa Loa (eye worm) proteasome subunit alpha type 3 0.0087 0.097 0.097
Brugia malayi intermediate filament protein 0.0033 0.021 0.021
Trypanosoma brucei proteasome beta 6 subunit 0.0239 0.3082 0.2339
Schistosoma mansoni proteasome subunit alpha 2 (T01 family) 0.0087 0.097 0.095
Brugia malayi Proteasome A-type and B-type family protein 0.0087 0.097 0.097
Onchocerca volvulus Notchless protein homolog 0.0087 0.097 1
Brugia malayi TAR-binding protein 0.0076 0.082 0.082
Echinococcus multilocularis proteasome subunit beta (t family) proteasome (prosome macropain) subunit beta 0.0087 0.097 0.095
Loa Loa (eye worm) proteasome subunit beta type 1 0.0239 0.3082 0.3082
Brugia malayi RNA recognition motif domain containing protein 0.0076 0.082 0.082
Brugia malayi Proteasome A-type and B-type family protein 0.0087 0.097 0.097
Leishmania major 20s proteasome beta 7 subunit, (putative) 0.0087 0.097 0.0533
Giardia lamblia Proteasome subunit beta type 5 precursor 0.0737 1 1
Echinococcus multilocularis tar DNA binding protein 0.0076 0.082 0.08
Loa Loa (eye worm) pigment dispersing factor receptor c 0.006 0.0594 0.0594
Echinococcus multilocularis proteasome (prosome, macropain) subunit, beta 0.0239 0.3082 0.3067
Loa Loa (eye worm) hypothetical protein 0.006 0.0587 0.0587
Loa Loa (eye worm) transcription factor SMAD2 0.0144 0.176 0.176
Echinococcus multilocularis Proteasome subunit alpha type 7 0.0087 0.097 0.095
Echinococcus granulosus proteasome subunit beta t family 0.0087 0.097 0.095
Leishmania major 20s proteasome beta 7 subunit, (putative) 0.0087 0.097 0.0533
Onchocerca volvulus Proteasomal ubiquitin receptor ADRM1 homolog 0.0062 0.0616 0.5338
Plasmodium falciparum proteasome subunit alpha type-5, putative 0.0087 0.097 0.0533
Trypanosoma cruzi proteasome subunit beta type-5, putative 0.0737 1 1
Schistosoma mansoni subfamily T1A non-peptidase homologue (T01 family) 0.0087 0.097 0.095
Brugia malayi proteasome subunit alpha type 4 0.0087 0.097 0.097
Echinococcus granulosus proteasome prosome macropain subunit alpha 0.0087 0.097 0.095
Loa Loa (eye worm) intermediate filament tail domain-containing protein 0.0033 0.021 0.021
Schistosoma mansoni tar DNA-binding protein 0.0076 0.082 0.08
Trypanosoma brucei proteasome subunit beta type-2, putative 0.0162 0.2007 0.1148
Echinococcus multilocularis lamin 0.0033 0.021 0.0188
Loa Loa (eye worm) hypothetical protein 0.0019 0.0022 0.0022
Plasmodium falciparum proteasome subunit beta type-5 0.0737 1 1
Schistosoma mansoni proteasome catalytic subunit 1 (T01 family) 0.0087 0.097 0.095
Brugia malayi Corticotropin releasing factor receptor 2 precursor, putative 0.006 0.0594 0.0594
Loa Loa (eye worm) proteasome subunit alpha type 1 0.0087 0.097 0.097
Leishmania major proteasome alpha 7 subunit, putative 0.0087 0.097 0.0533
Plasmodium falciparum proteasome subunit beta type-2, putative 0.0162 0.2007 0.162
Trypanosoma cruzi proteasome beta 6 subunit, putative 0.0239 0.3082 0.2339
Loa Loa (eye worm) proteasome subunit beta type 3 0.0087 0.097 0.097
Echinococcus granulosus Proteasome subunit alpha beta 0.0087 0.097 0.095
Plasmodium falciparum proteasome subunit beta type-7, putative 0.0087 0.097 0.0533
Entamoeba histolytica probable proteasome subunit beta type 2, putative 0.0162 0.2007 0.1148
Echinococcus multilocularis Proteasome, subunit alpha beta 0.0087 0.097 0.095
Loa Loa (eye worm) proteasome subunit beta type 2 0.0162 0.2007 0.2007
Schistosoma mansoni proteasome subunit alpha 1 (T01 family) 0.0087 0.097 0.095
Echinococcus granulosus Proteasome subunit alpha type 7 0.0087 0.097 0.095
Echinococcus multilocularis subfamily T1A non peptidase ue 0.0087 0.097 0.095
Schistosoma mansoni intermediate filament proteins 0.0033 0.021 0.0188
Echinococcus granulosus proteasome subunit beta type 7 0.0087 0.097 0.095
Loa Loa (eye worm) proteasome A-type and B-type family protein 0.0087 0.097 0.097
Mycobacterium tuberculosis Proteasome beta subunit PrcB; assembles with alpha subunit PrcA. 0.0737 1 1
Plasmodium vivax proteasome subunit beta type-2, putative 0.0162 0.2007 0.1148
Schistosoma mansoni proteasome subunit beta 2 (T01 family) 0.0087 0.097 0.095
Loa Loa (eye worm) PAS-3 protein 0.0087 0.097 0.097
Schistosoma mansoni proteasome subunit beta 4 (T01 family) 0.0087 0.097 0.095
Leishmania major proteasome beta 6 subunit, putative,20S proteasome beta 6 subunit, putative 0.0239 0.3082 0.2747
Loa Loa (eye worm) proteasome A-type and B-type family protein 0.0087 0.097 0.097
Plasmodium falciparum proteasome subunit beta type-1, putative 0.0239 0.3082 0.2747
Brugia malayi proteasome subunit beta type 3 0.0087 0.097 0.097
Echinococcus multilocularis Proteasome subunit alpha type 7 0.0087 0.097 0.095
Echinococcus granulosus proteasome prosome macropain subunit beta 0.0162 0.2007 0.1989
Schistosoma mansoni proteasome subunit alpha 6 (T01 family) 0.0087 0.097 0.095
Brugia malayi latrophilin 2 splice variant baaae 0.0041 0.0329 0.0329
Entamoeba histolytica proteasome subunit beta type 5 precursor, putative 0.0737 1 1
Trichomonas vaginalis Family T1, proteasome beta subunit, threonine peptidase 0.0162 0.2007 0.1148
Schistosoma mansoni proteasome subunit beta 3 (T01 family) 0.0087 0.097 0.095
Leishmania major proteasome beta 7 subunit, putative 0.0087 0.097 0.0533
Giardia lamblia Proteasome subunit beta type 2 0.0162 0.2007 0.1148
Leishmania major proteasome alpha 1 subunit, putative 0.0087 0.097 0.0533
Brugia malayi RNA binding protein 0.0076 0.082 0.082
Schistosoma mansoni lamin 0.0033 0.021 0.0188
Echinococcus multilocularis 20S proteasome subunit alpha 6 0.0087 0.097 0.095
Loa Loa (eye worm) hypothetical protein 0.006 0.0594 0.0594
Echinococcus granulosus proteasome prosome macropain 0.0737 1 1
Echinococcus granulosus tumor protein p63 0.0408 0.5425 0.5415
Loa Loa (eye worm) MH2 domain-containing protein 0.0144 0.176 0.176
Brugia malayi Proteasome subunit alpha type 1 0.0087 0.097 0.097
Loa Loa (eye worm) proteasome A-type and B-type family protein 0.0737 1 1
Brugia malayi Calcitonin receptor-like protein seb-1 0.006 0.0594 0.0594
Schistosoma mansoni proteasome subunit beta 3 (T01 family) 0.0087 0.097 0.095
Schistosoma mansoni lamin 0.0033 0.021 0.0188
Schistosoma mansoni proteasome subunit alpha 4 (T01 family) 0.0087 0.097 0.095
Giardia lamblia Proteasome subunit beta type 1 0.0239 0.3082 0.2339
Echinococcus multilocularis proteasome (prosome macropain) subunit beta type 0.0087 0.097 0.095
Echinococcus granulosus proteasome subunit alpha type 2 0.0087 0.097 0.095
Echinococcus multilocularis proteasome subunit beta type 6 0.0087 0.097 0.095
Echinococcus multilocularis lamin dm0 0.0033 0.021 0.0188
Loa Loa (eye worm) hypothetical protein 0.0032 0.0202 0.0202
Entamoeba histolytica proteasome subunit beta type 1, putative 0.0239 0.3082 0.2339
Echinococcus granulosus lamin dm0 0.0033 0.021 0.0188
Echinococcus multilocularis tumor protein p63 0.0408 0.5425 0.5415
Loa Loa (eye worm) hypothetical protein 0.0097 0.1109 0.1109
Leishmania major proteasome beta 3 subunit, putative 0.0087 0.097 0.0533
Plasmodium falciparum proteasome subunit alpha type-2, putative 0.0087 0.097 0.0533
Echinococcus multilocularis proteasome subunit beta type 7 0.0087 0.097 0.095
Brugia malayi 20S proteasome alpha5 subunit 0.0087 0.097 0.097

Activities

Activity type Activity value Assay description Source Reference
Potency (functional) = 1.5849 um PUBCHEM_BIOASSAY: qHTS Assay for Modulators of Lamin A Splicing. (Class of assay: confirmatory) ChEMBL. No reference
Potency (functional) 10 uM PubChem BioAssay. qHTS of GLP-1 Receptor Inverse Agonists (Inhibition Mode). (Class of assay: confirmatory) ChEMBL. No reference
Potency (functional) 12.5893 uM PubChem BioAssay. qHTS of TDP-43 Inhibitors. (Class of assay: confirmatory) ChEMBL. No reference
Potency (functional) = 15.8489 um PUBCHEM_BIOASSAY: qHTS Screen for Compounds that Selectively Target Cancer Cells with p53 Mutations: Cytotoxicity of p53 Null Cells at the Nonpermissive Temperature. (Class of assay: confirmatory) ChEMBL. No reference
Potency (functional) 17.7828 uM PUBCHEM_BIOASSAY: qHTS for Inhibitors of TGF-b. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID588856, AID588860] ChEMBL. No reference

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

No literature references available for this target.

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