telmisartan [Ligand Id: 592] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1017 (BIBR-277, BIBR 277 SE, BIBR-277-SE, Telmisartan, BIBR-277 SE, C09CA07, BIBR-277SE, Micardis, Tolura)
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  • AT2 receptor/Angiotensin II type 2 (AT-2) receptor in Human [ChEMBL: CHEMBL4607] [GtoPdb: 35] [UniProtKB: P50052]
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  • glycine receptor α1 subunit/Glycine receptor subunit alpha-1 in Human [ChEMBL: CHEMBL5845] [GtoPdb: 423] [UniProtKB: P23415]
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  • Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8]
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  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Mouse [ChEMBL: CHEMBL2128] [GtoPdb: 593] [UniProtKB: P23204]
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  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Mouse [ChEMBL: CHEMBL2458] [GtoPdb: 594] [UniProtKB: P35396]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238]
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  • AT1 receptor in Human [GtoPdb: 34] [UniProtKB: P30556]
  • AT1 receptor/Type-1A angiotensin II receptor in Rat [ChEMBL: CHEMBL329] [GtoPdb: 34] [UniProtKB: P25095]
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  • AT1 receptor/Type-1 angiotensin II receptor in Human [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
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  • AT1 receptor in Human [GtoPdb: 34] [UniProtKB: P30556]
  • AT1 receptor/Type-1B angiotensin II receptor in Rat [ChEMBL: CHEMBL263] [GtoPdb: 34] [UniProtKB: P29089]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Angiotensin-converting enzyme in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1808] [GtoPdb: 1613] [UniProtKB: P12821]
ChEMBL Inhibition of ACE (unknown origin) assessed as 3-Hydroxybutyril-glycil-glycil-glycine conversion to 3-hydroxybutyric acid after 60 mins by WST assay B 5.22 pKi 6000 nM Ki J. Med. Chem. (2013) 56: 8377-8388 [PMID:24088053]
AT2 receptor/Angiotensin II type 2 (AT-2) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4607] [GtoPdb: 35] [UniProtKB: P50052]
ChEMBL Displacement of [125I]Sar1 Ile8-Ang 2 from angiotensin 2 AT2 receptor after 180 mins by gamma counting B 9.48 pIC50 0.33 nM IC50 Eur. J. Med. Chem. (2012) 49: 183-190 [PMID:22309912]
glycine receptor α1 subunit/Glycine receptor subunit alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5845] [GtoPdb: 423] [UniProtKB: P23415]
ChEMBL Potentiation of human GlyR-alpha1 expressed in Xenopus laevis oocytes assessed as induction of glycine-activated currents after 1 to 4 days by two-electrode voltage clamp assay B 5.49 pEC50 3200 nM EC50 J. Med. Chem. (2015) 58: 2958-2966 [PMID:25790278]
Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8]
ChEMBL Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay B 4.75 pIC50 17900 nM IC50 J. Med. Chem. (2013) 56: 781-795 [PMID:23241029]
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
ChEMBL Displacement of radiolabeled GW-2433 from human PPARalpha ligand binding domain expressed in Escherichia coli B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 1399-1404 [PMID:20079636]
ChEMBL Agonist activity at human PPARalpha expressed in african green monkey CV1 cells by Gal4 transactivation assay F 5 pEC50 >10000 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 1399-1404 [PMID:20079636]
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2128] [GtoPdb: 593] [UniProtKB: P23204]
ChEMBL Agonist activity at mouse PPARalpha expressed in african green monkey CV1 cells by Gal4 transactivation assay F 5 pEC50 >10000 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 1399-1404 [PMID:20079636]
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
ChEMBL Displacement of radiolabeled GW-2433 from human PPARdelta ligand binding domain expressed in Escherichia coli B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 1399-1404 [PMID:20079636]
ChEMBL Agonist activity at human PPARdelta expressed in african green monkey CV1 cells by Gal4 transactivation assay F 5 pEC50 >10000 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 1399-1404 [PMID:20079636]
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2458] [GtoPdb: 594] [UniProtKB: P35396]
ChEMBL Agonist activity at mouse PPARdelta expressed in african green monkey CV1 cells by Gal4 transactivation assay F 5 pEC50 >10000 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 1399-1404 [PMID:20079636]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
ChEMBL Displacement of radiolabeled ((5-{4-[Methyl-pyridin-2yl-amino)-ethoxy]-benzyl}-thiazolidine-2,4-dione) from human PPARgamma ligand binding domain expressed in Escherichia coli B 4.91 pIC50 12200 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 1399-1404 [PMID:20079636]
ChEMBL Transactivation of Gal4 fused human PPARgamma LBD expressed in African green monkey COS7 cells after 42 hrs by dual luciferase reporter gene assay B 5.3 pEC50 4970 nM EC50 Eur J Med Chem (2017) 126: 590-603 [PMID:27918994]
ChEMBL Transactivation at Gal4 fused PPARgamma LBD (unknown origin) expressed in African green monkey COS7 cells after 42 hrs by luciferase assay B 5.33 pEC50 4710 nM EC50 Eur J Med Chem (2016) 124: 138-152 [PMID:27569195]
ChEMBL Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in African green monkey COS7 cells after 42 hrs by dual luciferase reporter gene assay B 5.33 pEC50 4700 nM EC50 Eur J Med Chem (2016) 124: 49-62 [PMID:27560282]
ChEMBL Activity at full length human PPARgamma transfected in CV1 cells assessed as transactivation activity after 24 hrs by PPRE-TK- luciferase reporter gene assay B 5.35 pEC50 4500 nM EC50 J. Med. Chem. (2015) 58: 5381-5394 [PMID:25734377]
ChEMBL Transactivation of Gal4-fused human PPARgamma transfected in COS7 cells co-transfected with pGAL5-TK-pGL3 and pRennilla-CMV incubated for 39 hrs by dual luciferase reporter assay B 5.37 pEC50 4280 nM EC50 Eur J Med Chem (2020) 185: 111748-111748 [PMID:31648125]
ChEMBL Activation of Gal4-tagged human PPARgamma expressed in CHO cells by luciferase reporter gene assay B 5.47 pEC50 3400 nM EC50 Bioorg. Med. Chem. (2010) 18: 5885-5895 [PMID:20656494]
ChEMBL Agonist activity at human PPARgamma expressed in african green monkey CV1 cells by Gal4 transactivation assay F 5.69 pEC50 2020 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 1399-1404 [PMID:20079636]
ChEMBL Agonist activity at human PPARgamma expressed in CV-1 cells by reporter gene assay B 5.69 pEC50 2020 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 1098-1103 [PMID:24462665]
ChEMBL Transactivation of GAL4-tagged human PPARgamma expressed in African green monkey COS7 cells after 36 hrs by luciferase reporter gene assay B 5.69 pEC50 2020 nM EC50 Eur J Med Chem (2019) 173: 261-273 [PMID:31009912]
ChEMBL Partial agonist activity at human PPARgamma-LBD/Gal4 DNA binding domain by transactivation assay B 5.82 pEC50 1520 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 767-772 [PMID:23265881]
ChEMBL Partial agonist activity at human PPARgamma-LBD/Gal4 DNA binding domain by transactivation assay B 5.82 pEC50 1520 nM EC50 J. Med. Chem. (2011) 54: 4219-4233 [PMID:21557540]
ChEMBL Displacement of Fluoromone from GST-tagged recombinant human PPARgamma ligand binding domain by LanthaScreen TR-FRET assay B 6.15 pEC50 700 nM EC50 Eur J Med Chem (2016) 124: 49-62 [PMID:27560282]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238]
ChEMBL Agonist activity at mouse PPARgamma expressed in african green monkey CV1 cells by Gal4 transactivation assay F 5.39 pEC50 4060 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 1399-1404 [PMID:20079636]
Plasmodium berghei (target type: ORGANISM) [ChEMBL: CHEMBL612653]
ChEMBL HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells F 7.6 pIC50 25 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2012) 109: 8511-8516 [PMID:22586124]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL HARVARD: Inhibition of blood stage Plasmodium falciparum 3D7 infection F 5.3 pIC50 >5000 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2012) 109: 8511-8516 [PMID:22586124]
ChEMBL HARVARD: Inhibition of blood stage Plasmodium falciparum Dd2 infection F 5.3 pIC50 >5000 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2012) 109: 8511-8516 [PMID:22586124]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 infected in RBCs by firefly luciferase reporter gene assay F 5.79 pIC50 1612 nM IC50 Antimicrob. Agents Chemother. (2010) 54: 3597-3604 [PMID:20547797]
AT1 receptor in Human [GtoPdb: 34] [UniProtKB: P30556]
GtoPdb - - 8.4 pIC50 - - - Drugs (1998) 56: 1039-44; discussion 1045-6 [PMID:9878991]
AT1 receptor/Type-1A angiotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL329] [GtoPdb: 34] [UniProtKB: P25095]
ChEMBL Displacement of [125I]SI-Ang2 from AT1 receptor in Sprague-Dawley rat liver membrane B 9.64 pKi 0.23 nM Ki J. Med. Chem. (2010) 53: 1076-1085 [PMID:20073471]
ChEMBL Displacement of [125I]-SI-Ang-2 from AT1 receptor in Rattus norvegicus Sprague-Dawley (rat) liver membranes after 2 hr B 9.64 pKi 0.23 nM Ki Med Chem Res (2009) 18: 611-628
AT1 receptor/Type-1 angiotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
ChEMBL Inhibition of angiotensin AT1 receptor B 6.82 pIC50 150 nM IC50 Bioorg. Med. Chem. (2012) 20: 4208-4216 [PMID:22727371]
GtoPdb - - 8.4 pIC50 - - - Drugs (1998) 56: 1039-44; discussion 1045-6 [PMID:9878991]
ChEMBL Inhibition of AT1 receptor B 8.52 pIC50 3 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 1399-1404 [PMID:20079636]
ChEMBL Antagonist activity at human AT1 receptor expressed in CHO cells measured after overnight incubation by luciferase reporter gene assay B 8.7 pIC50 2 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 1098-1103 [PMID:24462665]
ChEMBL Inhibition of AT1 receptor (unknown origin) B 8.7 pIC50 2 nM IC50 Eur J Med Chem (2019) 173: 261-273 [PMID:31009912]
ChEMBL Displacement of [125I]Sar1Ile8-Ang2 from angiotensin AT1 receptor after 180 mins by gamma counting B 9 pIC50 1 nM IC50 Bioorg. Med. Chem. (2012) 20: 4208-4216 [PMID:22727371]
ChEMBL Displacement of [125I]Sar1 Ile8-Ang 2 from angiotensin 2 AT1 receptor after 180 mins by gamma counting B 9 pIC50 1 nM IC50 Eur. J. Med. Chem. (2012) 49: 183-190 [PMID:22309912]
ChEMBL Displacement of [125I]-Sar1Ile8-angiotensin 2 from angiotensin 2 AT1 receptor (unknown origin) after 180 mins by gamma counting analysis B 9 pIC50 1 nM IC50 Eur. J. Med. Chem. (2013) 69: 44-54 [PMID:24007859]
ChEMBL Displacement of [125I]Tyr4-Sar1,Ile8-Angiotensin II from human Angiotensin 1 receptor after B 9.31 pIC50 0.49 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 767-772 [PMID:23265881]
ChEMBL Displacement of [125I]Tyr4-Sar1,Ile8-Angiotensin II from human Angiotensin 1 receptor after 60 mins by scintillation counting B 9.31 pIC50 0.49 nM IC50 J. Med. Chem. (2011) 54: 4219-4233 [PMID:21557540]
AT1 receptor in Human [GtoPdb: 34] [UniProtKB: P30556]
GtoPdb - - 8.4 pIC50 - - - Drugs (1998) 56: 1039-44; discussion 1045-6 [PMID:9878991]
AT1 receptor/Type-1B angiotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL263] [GtoPdb: 34] [UniProtKB: P29089]
ChEMBL Inhibition of specific binding of [125I]angiotensin-II to angiotensin 1 receptor in rat lung membrane preparation B 8.52 pIC50 3 nM IC50 J. Med. Chem. (1993) 36: 4040-4051 [PMID:8258826]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]