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] |
| 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 | 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 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
