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, BIBR-277-SE, BIBR-277SE, C09CA07, Kinzalmono, Micardis, Pritor, Semintra, Telmisartan, Telmisartan actavis, Telmisartan teva, Tolura) |
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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] |
| ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] | ||||||||
| ChEMBL | Inhibition of human ABCG2 expressed in dog MDCK-II-BCRP cells mediated pheophorbide A efflux and measured after 60 mins using pheophorbide A as fluorescent substrate by flow cytometry | B | 4.77 | pIC50 | 16900 | nM | IC50 | Eur J Med Chem (2022) 237: 114346-114346 [PMID:35483322] |
| 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 | Partial agonist activity at PPARgamma (unknown origin) by TR-FRET-based competitive binding assay | B | 5.97 | pKi | 1080 | nM | Ki | ACS Med Chem Lett (2023) 14: 425-431 [PMID:37077388] |
| 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 | Agonist activity at human PPARgammaDEF receptor expressed in african green monkey COS7 cells transfected with pGal5-TK-pGL3/pRenilla-CMV assessed as intrinsic activity measured after 39 hrs by dual luciferase reporter assay | B | 5.37 | pEC50 | 4300 | nM | EC50 | Eur J Med Chem (2020) 195: 112258-112258 [PMID:32272420] |
| 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 | 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 | 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 | 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 (target type: ORGANISM) [ChEMBL: CHEMBL4888483] | ||||||||
| ChEMBL | Antimalarial activity against Plasmodium | F | 7.6 | pIC50 | 25 | nM | IC50 | Eur J Med Chem (2020) 195: 112275-112275 [PMID:32283298] |
| 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] |
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: AGTR1 | F | 8.27 | pIC50 | 5.4 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| 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 | Inhibition of AT1 receptor (unknown origin) | B | 8.7 | pIC50 | 2 | nM | IC50 | Eur J Med Chem (2019) 173: 261-273 [PMID:31009912] |
| 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 | 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]-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]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]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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
