Detailed information for compound 331728

Basic information

Technical information
  • TDR Targets ID: 331728
  • Name: 6-chloro-7-methoxy-1,1-dioxo-N-propan-2-yl-4H -benzo[e][1,2,4]thiadiazin-3-amine
  • MW: 303.765 | Formula: C11H14ClN3O3S
  • H donors: 2 H acceptors: 2 LogP: 1.61 Rotable bonds: 3
    Rule of 5 violations (Lipinski): 1
  • SMILES: COc1cc2c(cc1Cl)NC(=NS2(=O)=O)NC(C)C
  • InChi: 1S/C11H14ClN3O3S/c1-6(2)13-11-14-8-4-7(12)9(18-3)5-10(8)19(16,17)15-11/h4-6H,1-3H3,(H2,13,14,15)
  • InChiKey: WZNRNCKCVQCMQD-UHFFFAOYSA-N  


Substructure search Similarity search

Network

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Synonyms

  • 6-chloro-N-isopropyl-7-methoxy-1,1-dioxo-4H-benzo[e][1,2,4]thiadiazin-3-amine
  • (6-chloro-1,1-diketo-7-methoxy-4H-benzo[e][1,2,4]thiadiazin-3-yl)-isopropyl-amine

Targets

Known targets for this compound

Species Target name Source Bibliographic reference
Rattus norvegicus ATP-binding cassette sub-family C member 8 Starlite/ChEMBL References

Predicted pathogen targets for this compound

By orthology
Species Potential target Known druggable target/s Ortholog Group
Leishmania major ATP-binding cassette protein subfamily C, member 5, putative Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania infantum ATP-binding cassette protein subfamily C, member 1, putative Get druggable targets OG5_126561 All targets in OG5_126561
Trypanosoma brucei gambiense multidrug resistance protein E,p-glycoprotein Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania infantum ATP-binding cassette protein subfamily C, member 5, putative Get druggable targets OG5_126561 All targets in OG5_126561
Cryptosporidium parvum ABC ATpase (2 ABC domains) with 10 transmembrane domains, adjacent duplicated gene Get druggable targets OG5_126561 All targets in OG5_126561
Trypanosoma cruzi multidrug resistance-associated protein, putative Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania braziliensis multidrug resistance protein, putative,p-glycoprotein, putative,ABC transporter, putative Get druggable targets OG5_126561 All targets in OG5_126561
Babesia bovis ABC transporter family protein Get druggable targets OG5_126561 All targets in OG5_126561
Neospora caninum hypothetical protein Get druggable targets OG5_126561 All targets in OG5_126561
Entamoeba histolytica ABC transporter, putative Get druggable targets OG5_126561 All targets in OG5_126561
Brugia malayi ABC transporter transmembrane region family protein Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania braziliensis p-glycoprotein e, putative Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania mexicana p-glycoprotein e, putative Get druggable targets OG5_126561 All targets in OG5_126561
Giardia lamblia Multidrug resistance-associated protein 1 Get druggable targets OG5_126561 All targets in OG5_126561
Schistosoma japonicum ko:K05667 ATP-binding cassette, subfamily C (CFTR/MRP), member 3, putative Get druggable targets OG5_126561 All targets in OG5_126561
Entamoeba histolytica ATP-binding cassette protein, putative Get druggable targets OG5_126561 All targets in OG5_126561
Candida albicans one of three genes similar to S. cerevisiae YCF1 (YDR135C) and BPT1 (YLL015W) Get druggable targets OG5_126561 All targets in OG5_126561
Babesia bovis ABC transporter family protein Get druggable targets OG5_126561 All targets in OG5_126561
Toxoplasma gondii ABC transporter transmembrane region domain-containing protein Get druggable targets OG5_126561 All targets in OG5_126561
Theileria parva ABC transporter, putative Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania infantum ABC-thiol transporter Get druggable targets OG5_126561 All targets in OG5_126561
Giardia lamblia Multidrug resistance-associated protein 1 Get druggable targets OG5_126561 All targets in OG5_126561
Theileria parva ABC transporter, putative Get druggable targets OG5_126561 All targets in OG5_126561
Theileria parva ABC transporter, putative Get druggable targets OG5_126561 All targets in OG5_126561
Candida albicans hypothetical protein Get druggable targets OG5_126561 All targets in OG5_126561
Theileria parva ABC transporter, putative Get druggable targets OG5_126561 All targets in OG5_126561
Entamoeba histolytica ATP-binding cassette protein, putative Get druggable targets OG5_126561 All targets in OG5_126561
Schistosoma japonicum Multidrug resistance-associated protein 4, putative Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania infantum ATP-binding cassette protein subfamily C, member 6, putative Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania mexicana multidrug resistance protein, putative,p-glycoprotein, putative,ABC transporter, putative Get druggable targets OG5_126561 All targets in OG5_126561
Loa Loa (eye worm) hypothetical protein Get druggable targets OG5_126561 All targets in OG5_126561
Trypanosoma brucei p-glycoprotein Get druggable targets OG5_126561 All targets in OG5_126561
Loa Loa (eye worm) multidrug resistance-associated protein Get druggable targets OG5_126561 All targets in OG5_126561
Entamoeba histolytica ATP-binding cassette protein, putative Get druggable targets OG5_126561 All targets in OG5_126561
Schistosoma mansoni multidrug resistance protein Get druggable targets OG5_126561 All targets in OG5_126561
Trypanosoma cruzi hypothetical protein Get druggable targets OG5_126561 All targets in OG5_126561
Theileria parva ABC transporter, putative Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania mexicana p-glycoprotein-like protein Get druggable targets OG5_126561 All targets in OG5_126561
Trypanosoma cruzi multidrug resistance-associated protein, putative Get druggable targets OG5_126561 All targets in OG5_126561
Entamoeba histolytica ATP-binding cassette protein, putative Get druggable targets OG5_126561 All targets in OG5_126561
Candida albicans one of three genes similar to S. cerevisiae YCF1 (YDR135C) and BPT1 (YLL015W) Get druggable targets OG5_126561 All targets in OG5_126561
Schistosoma mansoni multidrug resistance protein Get druggable targets OG5_126561 All targets in OG5_126561
Cryptosporidium parvum ATP-binding cassette protein Get druggable targets OG5_126561 All targets in OG5_126561
Trypanosoma congolense multidrug resistance-associated protein, putative Get druggable targets OG5_126561 All targets in OG5_126561
Echinococcus granulosus multidrug resistance associated protein 7 Get druggable targets OG5_126561 All targets in OG5_126561
Schistosoma japonicum Multidrug resistance-associated protein 1, putative Get druggable targets OG5_126561 All targets in OG5_126561
Theileria parva ABC transporter, putative Get druggable targets OG5_126561 All targets in OG5_126561
Trypanosoma cruzi multidrug resistance protein E, putative Get druggable targets OG5_126561 All targets in OG5_126561
Giardia lamblia Multidrug resistance-associated protein 1 Get druggable targets OG5_126561 All targets in OG5_126561
Echinococcus multilocularis multidrug resistance associated protein 4 Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania mexicana ABC-thiol transporter Get druggable targets OG5_126561 All targets in OG5_126561
Theileria parva ABC transporter, putative Get druggable targets OG5_126561 All targets in OG5_126561
Theileria parva ABC transporter, putative Get druggable targets OG5_126561 All targets in OG5_126561
Echinococcus granulosus multidrug resistance associated protein 1 Get druggable targets OG5_126561 All targets in OG5_126561
Theileria parva ABC transporter, putative Get druggable targets OG5_126561 All targets in OG5_126561
Candida albicans vacuolar ABC transporter similar to multiple drug resistance-associated protein Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania mexicana ATP-binding cassette protein subfamily C, member 1, putative Get druggable targets OG5_126561 All targets in OG5_126561
Candida albicans similar to vacuolar membrane ATP-dependant transporter, metal resistance protein Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania braziliensis p-glycoprotein e Get druggable targets OG5_126561 All targets in OG5_126561
Schistosoma japonicum Multidrug resistance-associated protein 4, putative Get druggable targets OG5_126561 All targets in OG5_126561
Theileria parva ABC transporter, putative Get druggable targets OG5_126561 All targets in OG5_126561
Loa Loa (eye worm) hypothetical protein Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania infantum p-glycoprotein e Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania mexicana p-glycoprotein e Get druggable targets OG5_126561 All targets in OG5_126561
Babesia bovis ABC transporter family protein Get druggable targets OG5_126561 All targets in OG5_126561
Echinococcus multilocularis multidrug resistance associated protein 7 Get druggable targets OG5_126561 All targets in OG5_126561
Entamoeba histolytica hypothetical protein Get druggable targets OG5_126561 All targets in OG5_126561
Echinococcus granulosus multidrug resistance associated protein 4 Get druggable targets OG5_126561 All targets in OG5_126561
Candida albicans one of three genes similar to S. cerevisiae YCF1 (YDR135C) and BPT1 (YLL015W) Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania infantum ATP-binding cassette protein subfamily C, member 2, putative Get druggable targets OG5_126561 All targets in OG5_126561
Schistosoma japonicum Canalicular multispecific organic anion transporter 2, putative Get druggable targets OG5_126561 All targets in OG5_126561
Trypanosoma brucei gambiense multidrug resistance-associated protein, putative,p-glycoprotein Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania infantum pentamidine resistance protein 1 Get druggable targets OG5_126561 All targets in OG5_126561
Cryptosporidium hominis SI:dZ52I16.4 (novel ABC transporter similar to human multidrug-resistance proteins (MRP)) Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania major pentamidine resistance protein 1 Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania braziliensis ABC-thiol transporter Get druggable targets OG5_126561 All targets in OG5_126561
Candida albicans vacuolar ABC transporter similar to multiple drug resistance-associated protein Get druggable targets OG5_126561 All targets in OG5_126561
Theileria parva ABC transporter, putative Get druggable targets OG5_126561 All targets in OG5_126561
Schistosoma japonicum Multidrug resistance-associated protein 7, putative Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania donovani pentamidine resistance protein 1 Get druggable targets OG5_126561 All targets in OG5_126561
Entamoeba histolytica multidrug resistance protein, putative Get druggable targets OG5_126561 All targets in OG5_126561
Candida albicans similar to vacuolar membrane ATP-dependant transporter, metal resistance protein Get druggable targets OG5_126561 All targets in OG5_126561
Giardia lamblia ABC transporter, putative Get druggable targets OG5_126561 All targets in OG5_126561
Giardia lamblia MRP-like ABC transporter Get druggable targets OG5_126561 All targets in OG5_126561
Trypanosoma brucei multidrug resistance protein E Get druggable targets OG5_126561 All targets in OG5_126561
Loa Loa (eye worm) ABC transporter transmembrane region family protein Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania major ATP-binding cassette protein subfamily C, member 1, putative Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania major p-glycoprotein e Get druggable targets OG5_126561 All targets in OG5_126561
Trypanosoma brucei multidrug resistance-associated protein, putative Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania braziliensis multidrug resistance protein, putative,p-glycoprotein, putative,ABC transporter, putative Get druggable targets OG5_126561 All targets in OG5_126561
Schistosoma japonicum ko:K05674 ATP-binding cassette, subfamily C (CFTR/MRP), member 10, putative Get druggable targets OG5_126561 All targets in OG5_126561
Theileria parva ABC transporter, putative Get druggable targets OG5_126561 All targets in OG5_126561
Echinococcus multilocularis multidrug resistance associated protein 1 Get druggable targets OG5_126561 All targets in OG5_126561
Babesia bovis ABC transporter, ATP-binding protein domain containing protein Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania mexicana multidrug resistance protein, copy 1-like protein Get druggable targets OG5_126561 All targets in OG5_126561
Brugia malayi multidrug resistance related protein 1 Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania major ABC-thiol transporter Get druggable targets OG5_126561 All targets in OG5_126561
Trypanosoma brucei multidrug resistance-associated protein, putative Get druggable targets OG5_126561 All targets in OG5_126561
Loa Loa (eye worm) hypothetical protein Get druggable targets OG5_126561 All targets in OG5_126561
Schistosoma mansoni multidrug resistance protein Get druggable targets OG5_126561 All targets in OG5_126561
Theileria parva ABC transporter, putative Get druggable targets OG5_126561 All targets in OG5_126561
Trypanosoma congolense multidrug resistance protein A Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania major ATP-binding cassette protein subfamily C, member 6, putative Get druggable targets OG5_126561 All targets in OG5_126561
Leishmania major ATP-binding cassette protein subfamily C, member 2, putative Get druggable targets OG5_126561 All targets in OG5_126561
Schistosoma mansoni multidrug resistance protein Get druggable targets OG5_126561 All targets in OG5_126561
Schistosoma japonicum Multidrug resistance-associated protein 4, putative Get druggable targets OG5_126561 All targets in OG5_126561
Candida albicans one of three genes similar to S. cerevisiae YCF1 (YDR135C) and BPT1 (YLL015W) Get druggable targets OG5_126561 All targets in OG5_126561
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
Entamoeba histolytica ABC transporter, putative 0.0017 0 0.5
Giardia lamblia ABC transporter, putative 0.0017 0 1
Schistosoma mansoni alzheimer's disease beta-amyloid related 0.0112 0.028 0.4151
Echinococcus granulosus guanine nucleotide binding protein Gs subunit 0.0045 0.0081 0.1278
Entamoeba histolytica ATP-binding cassette protein, putative 0.0017 0 0.5
Toxoplasma gondii chorismate synthase, putative 0.3415 1 1
Mycobacterium leprae probable 3-phosphoshikimate 1-carboxyvinyl transferase AroA (5-ENOLPYRUVYLSHIKIMATE-3-PHOSPHATE SYNTHASE) (EPSP SYNTHASE) (EPSPS 0.0322 0.0899 0.1715
Loa Loa (eye worm) hypothetical protein 0.013 0.0333 0.5023
Loa Loa (eye worm) ABC transporter transmembrane region family protein 0.0017 0 0.0006
Mycobacterium leprae 3-dehydroquinate synthase AroB 0.0126 0.0319 0.0516
Loa Loa (eye worm) hypothetical protein 0.0065 0.0141 0.2129
Echinococcus multilocularis protoporphyrinogen oxidase 0.0041 0.007 0.1097
Mycobacterium tuberculosis Probable chorismate synthase AroF (5-enolpyruvylshikimate-3-phosphate phospholyase) 0.1684 0.4906 1
Echinococcus multilocularis geminin 0.0165 0.0436 0.6895
Loa Loa (eye worm) hypothetical protein 0.0041 0.007 0.1052
Plasmodium vivax chorismate synthase 0.3415 1 1
Brugia malayi Uncharacterized hematopoietic stem/progenitor cells protein MDS029 0.0099 0.024 0.2806
Loa Loa (eye worm) hypothetical protein 0.0242 0.0663 1
Echinococcus multilocularis guanine nucleotide binding protein G(s) subunit 0.0045 0.0081 0.1278
Trypanosoma cruzi UDP-galactopyranose mutase 0.0041 0.007 1
Schistosoma mansoni Guanine nucleotide-binding protein G(s) subunit alpha (Adenylate cyclase-stimulating G alpha protein) 0.0045 0.0081 0.12
Echinococcus granulosus cdgsh iron sulfur domain containing protein 0.0232 0.0632 1
Entamoeba histolytica multidrug resistance protein, putative 0.0017 0 0.5
Chlamydia trachomatis phosphoshikimate 1-carboxyl vinyltransferase 0.0322 0.0899 0.0835
Brugia malayi hypothetical protein 0.0041 0.007 0.0811
Mycobacterium tuberculosis 3-phosphoshikimate 1-carboxyvinyltransferase AroA (5-enolpyruvylshikimate-3-phosphate synthase) (EPSP synthase) (EPSPS) 0.0126 0.0319 0.0516
Giardia lamblia MRP-like ABC transporter 0.0017 0 1
Loa Loa (eye worm) hypothetical protein 0.0017 0 0.0006
Mycobacterium tuberculosis 3-dehydroquinate synthase AroB 0.0126 0.0319 0.0516
Toxoplasma gondii histone lysine-specific demethylase 0.0041 0.007 0.0069
Schistosoma mansoni amine oxidase 0.0041 0.007 0.103
Trypanosoma cruzi UDP-galactopyranose mutase 0.0041 0.007 1
Schistosoma mansoni Guanine nucleotide-binding protein G(s) subunit alpha (Adenylate cyclase-stimulating G alpha protein) 0.0045 0.0081 0.12
Trypanosoma brucei multidrug resistance protein E 0.0017 0 0.5
Echinococcus granulosus geminin 0.0165 0.0436 0.6895
Mycobacterium ulcerans flavin-containing monoamine oxidase AofH 0.0578 0.1651 0.1593
Mycobacterium tuberculosis Probable flavin-containing monoamine oxidase AofH (amine oxidase) (MAO) 0.0537 0.1531 0.3023
Brugia malayi GTP-binding regulatory protein Gs alpha-S chain, putative 0.0045 0.0081 0.0945
Loa Loa (eye worm) hypothetical protein 0.0041 0.007 0.1052
Schistosoma mansoni CDGSH-type Zn finger-containing protein-like protein 0.0246 0.0674 1
Schistosoma mansoni Guanine nucleotide-binding protein G(s) subunit alpha (Adenylate cyclase-stimulating G alpha protein) 0.0045 0.0081 0.12
Echinococcus multilocularis guanine nucleotide binding protein G(s) subunit 0.0045 0.0081 0.1278
Entamoeba histolytica ATP-binding cassette protein, putative 0.0017 0 0.5
Echinococcus multilocularis cdgsh iron sulfur domain containing protein 0.0232 0.0632 1
Toxoplasma gondii shikimate dehydrogenase substrate binding domain-containing protein 0.0322 0.0899 0.0899
Schistosoma mansoni hypothetical protein 0.0165 0.0436 0.6474
Mycobacterium ulcerans chorismate synthase 0.3415 1 1
Mycobacterium ulcerans UDP-N-acetylglucosamine 1-carboxyvinyltransferase 0.0197 0.053 0.0463
Schistosoma mansoni Lysine-specific histone demethylase 1 0.0041 0.007 0.103
Echinococcus multilocularis lysine specific histone demethylase 1A 0.0041 0.007 0.1097
Echinococcus granulosus lysine specific histone demethylase 1A 0.0041 0.007 0.1097
Echinococcus granulosus guanine nucleotide binding protein Gs subunit 0.0045 0.0081 0.1278
Loa Loa (eye worm) hypothetical protein 0.0017 0 0.0006
Mycobacterium ulcerans flavin-containing monoamine oxidase AofH 0.0578 0.1651 0.1593
Schistosoma mansoni hypothetical protein 0.0246 0.0674 1
Brugia malayi amine oxidase, flavin-containing family protein 0.0041 0.007 0.0811
Giardia lamblia Multidrug resistance-associated protein 1 0.0017 0 1
Wolbachia endosymbiont of Brugia malayi UDP-N-acetylglucosamine 1-carboxyvinyltransferase 0.0197 0.053 0.5
Brugia malayi SWIRM domain containing protein 0.0041 0.007 0.0811
Schistosoma mansoni hypothetical protein 0.0165 0.0436 0.6474
Giardia lamblia Multidrug resistance-associated protein 1 0.0017 0 1
Schistosoma mansoni 3-dehydroquinate synthase 0.0126 0.0319 0.4738
Entamoeba histolytica ATP-binding cassette protein, putative 0.0017 0 0.5
Chlamydia trachomatis UDP-N-acetylglucosamine 1-carboxyvinyltransferase 0.0197 0.053 0.0463
Brugia malayi Amyloid A4 extracellular domain containing protein 0.0307 0.0855 1
Loa Loa (eye worm) hypothetical protein 0.0041 0.007 0.1052
Echinococcus multilocularis 0.0041 0.007 0.1097
Entamoeba histolytica ATP-binding cassette protein, putative 0.0017 0 0.5
Toxoplasma gondii histone lysine-specific demethylase LSD1/BHC110/KDMA1A 0.0041 0.007 0.0069
Entamoeba histolytica hypothetical protein 0.0017 0 0.5
Trypanosoma brucei multidrug resistance-associated protein, putative 0.0017 0 0.5
Echinococcus granulosus lysine specific histone demethylase 1A 0.0041 0.007 0.1097
Loa Loa (eye worm) hypothetical protein 0.0041 0.007 0.1052
Mycobacterium leprae Chorismate synthase AroF (5-enolpyruvylshikimate-3-phosphate phospholyase). 0.1684 0.4906 1
Schistosoma mansoni amine oxidase 0.0041 0.007 0.103
Plasmodium falciparum chorismate synthase 0.3415 1 1
Treponema pallidum UDP-N-acetylglucosamine 1-carboxyvinyltransferase 0.0197 0.053 0.5
Trypanosoma brucei p-glycoprotein 0.0017 0 0.5
Onchocerca volvulus 0.0099 0.024 1
Trypanosoma brucei multidrug resistance-associated protein, putative 0.0017 0 0.5
Schistosoma mansoni Protoporphyrinogen oxidase chloroplast/mitochondrial precursor 0.0041 0.007 0.103
Leishmania major UDP-galactopyranose mutase 0.0041 0.007 1
Loa Loa (eye worm) hypothetical protein 0.0041 0.007 0.1052
Loa Loa (eye worm) hypothetical protein 0.0099 0.024 0.3622
Mycobacterium ulcerans 3-dehydroquinate synthase 0.0126 0.0319 0.0251
Mycobacterium ulcerans 3-phosphoshikimate 1-carboxyvinyltransferase 0.0322 0.0899 0.0835
Chlamydia trachomatis dehyroquinate synthase 0.0126 0.0319 0.0251
Loa Loa (eye worm) GTP-binding regulatory protein Gs alpha-S chain 0.0045 0.0081 0.1225
Loa Loa (eye worm) hypothetical protein 0.0041 0.007 0.1052

Activities

Activity type Activity value Assay description Source Reference
Activity (binding) = 7.7 % Activation of SUR1 in rat pancreatic islets assessed as residual insulin release at 10 uM in presence of 16.7 mM glucose ChEMBL. 22077416
Activity (binding) = 20.6 % Activation of SUR1 in rat pancreatic islets assessed as residual insulin release at 1 uM in presence of 16.7 mM glucose ChEMBL. 22077416
Activity (binding) = 73.8 % Activation of SUR1 in rat pancreatic islets assessed as residual insulin release at 0.1 uM in presence of 16.7 mM glucose ChEMBL. 22077416
EC50 (functional) = 37 uM Concentration required to relax KCl induced rat aorta ring contractions by 50% upon incubation with the compound at 37 degree C for 90 mins ChEMBL. 16033278
IC50 (functional) = 0.24 uM Concentration required to inhibit insulin release in rat pancreatic islets by 50% upon incubation with the compound at 37 degree C for 90 mins ChEMBL. 16033278
IC50 (binding) = 0.24 uM Activation of SUR1 in rat pancreatic islets assessed as inhibition of glucose-induced insulin secretion ChEMBL. 22077416
Release (functional) = 7.7 % Percent residual insulin release in rat pancreatic islets upon incubation with the compound (10 uM) at 37 degree C for 90 mins ChEMBL. 16033278
Release (functional) = 20.6 % Percent residual insulin release in rat pancreatic islets upon incubation with the compound (1 uM) at 37 degree C for 90 mins ChEMBL. 16033278
Release (functional) = 73.8 % Percent residual insulin release in rat pancreatic islets upon incubation with the compound (0.1 uM) at 37 degree C for 90 mins ChEMBL. 16033278
Selectivity (functional) = 154.2 Ratio of EC50 required to relax KCl induced rat aorta ring contractions to that of IC50 required to inhibit insulin release in rat pancreatic islets ChEMBL. 16033278

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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