[3H]candesartan [Ligand Id: 6907] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1016 (Candesartan, CV-11974, Candesartan cilexetil related compound g)
  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • Angiotensin II type 1a (AT-1a) receptor in Bovine [ChEMBL: CHEMBL3374] [UniProtKB: P25104]
  • Angiotensin II type 1a (AT-1a) receptor in Rabbit [ChEMBL: CHEMBL3948] [UniProtKB: P34976]
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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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  • β3-adrenoceptor/Beta-3 adrenergic receptor in Human [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
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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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 6.16 pKi 689.5 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 5.91 pIC50 1219.9 nM IC50 DrugMatrix in vitro pharmacology data
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 5.76 pKi 1754.4 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 5.42 pIC50 3843 nM IC50 DrugMatrix in vitro pharmacology data
Angiotensin II type 1a (AT-1a) receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3374] [UniProtKB: P25104]
ChEMBL Displacement of [125 I]-AII (0.2 nM) from bovine adrenal cortical membrane angiotensin II (AII) receptor at 10e-7 M B 6.96 pIC50 110 nM IC50 Bioorg. Med. Chem. Lett. (1995) 5: 1903-1908
ChEMBL Inhibition of specific binding of [125 I ] Angiotensin-II (0.2 nM) to bovine adrenal cortex B 6.96 pIC50 110 nM IC50 J. Med. Chem. (1993) 36: 2182-2195 [PMID:8340921]
ChEMBL Concentration required to inhibit [125I]AII binding to Angiotensin II receptor from membrane fractions of bovine adrenal cortex B 6.96 pIC50 110 nM IC50 Bioorg. Med. Chem. Lett. (1994) 4: 35-40
Angiotensin II type 1a (AT-1a) receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3948] [UniProtKB: P34976]
ChEMBL Inhibitory activity against Angiotensin II receptor, type 1 in rat adrenal membrane B 9.19 pKi 0.64 nM Ki J. Med. Chem. (1996) 39: 625-656 [PMID:8576904]
ChEMBL Inhibitory activity against Angiotensin II receptor, type 1 in rabbit aorta B 7.55 pIC50 28 nM IC50 J. Med. Chem. (1996) 39: 625-656 [PMID:8576904]
AT2 receptor/Angiotensin II type 2 (AT-2) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4607] [GtoPdb: 35] [UniProtKB: P50052]
ChEMBL Binding affinity to type-2 angiotensin-2 receptor (unknown origin) B 5 pKi >10000 nM Ki Bioorg. Med. Chem. Lett. (2016) 26: 1355-1359 [PMID:26810314]
β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
ChEMBL DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) B 5.49 pKi 3200 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) B 5.37 pIC50 4300 nM IC50 DrugMatrix in vitro pharmacology data
CYP2C9/Cytochrome P450 2C9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3397] [GtoPdb: 1326] [UniProtKB: P11712]
ChEMBL DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 5.52 pIC50 3000 nM IC50 DrugMatrix in vitro pharmacology data
CYP3A4/Cytochrome P450 3A4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL340] [GtoPdb: 1337] [UniProtKB: P08684]
ChEMBL DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin) B 5.05 pIC50 9000 nM IC50 DrugMatrix in vitro pharmacology data
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr)) B 5.48 pIC50 3276.9 nM IC50 DrugMatrix in vitro pharmacology data
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.52 pKi 3039.8 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.51 pIC50 3065.2 nM IC50 DrugMatrix in vitro pharmacology data
erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
ChEMBL DRUGMATRIX: Protein Tyrosine Kinase, ERBB2 (HER2) enzyme inhibition (substrate: Poly(Glu:Tyr)) B 5.23 pIC50 5947.2 nM IC50 DrugMatrix in vitro pharmacology data
CYP5A1/Thromboxane-A synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1835] [GtoPdb: 1353] [UniProtKB: P24557]
ChEMBL DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2) B 5.51 pIC50 3059.4 nM IC50 DrugMatrix in vitro pharmacology data
AT1 receptor in Human [GtoPdb: 34] [UniProtKB: P30556]
GtoPdb - - 10.29 pKd - - - Eur. J. Pharmacol. (1999) 367: 413-22 [PMID:10079018]
AT1 receptor/Type-1A angiotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL329] [GtoPdb: 34] [UniProtKB: P25095]
ChEMBL Antagonist activity at AT1 receptor in rat aorta F 8 pKd 10 nM Kd Eur. J. Med. Chem. (2008) 43: 1808-1812 [PMID:18158200]
ChEMBL Antagonist activity at AT1 receptor in rat aortic rings F 8.5 pKd 3.16 nM Kd Bioorg. Med. Chem. (2008) 16: 10210-10215 [PMID:19013821]
AT1 receptor/Type-1 angiotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
GtoPdb - - 10.29 pKd - - - Eur. J. Pharmacol. (1999) 367: 413-22 [PMID:10079018]
ChEMBL Displacement of [125I-Sar1-Ile8]-Ang2 from human angiotensin 2 receptor type 1 receptor expressed in HEK293 cells after 1 hr by gamma counting analysis B 7.98 pKi 10.4 nM Ki Eur J Med Chem (2018) 145: 273-290 [PMID:29329002]
ChEMBL Displacement of [3H]-Asp-{Nomega-[N-(4-propanoylaminobutyl)aminocarbonyl]}Arg-ValTyr-Ile-His-Pro-Phe-OH Tris(hydrotrifluoroacetate) from human AT1 receptor transfected in CHO cells co-expressing Galpha16-mtAEQ after 2 hrs by liquid scintillation counting B 8.46 pKi 3.5 nM Ki J. Med. Chem. (2016) 59: 1925-1945 [PMID:26824643]
ChEMBL Binding affinity to angiotensin AT1 receptor B 6.96 pIC50 110 nM IC50 Bioorg. Med. Chem. (2010) 18: 8418-8456 [PMID:21071232]
ChEMBL Displacement of [3H]-Asp-{Nomega-[N-(4-propanoylaminobutyl)aminocarbonyl]}Arg-ValTyr-Ile-His-Pro-Phe-OH Tris(hydrotrifluoroacetate) from human AT1 receptor transfected in CHO cells co-expressing Galpha16-mtAEQ after 2 hrs by liquid scintillation counting B 7.97 pIC50 10.72 nM IC50 J. Med. Chem. (2016) 59: 1925-1945 [PMID:26824643]
ChEMBL Displacement of [3H]-Angiotensin 2 from human AT1 receptor transfected in CHOK1 cells preincubated for 30 mins with bovine serum albumin followed by radioligand addition by liquid scintillation counting B 9.16 pIC50 0.69 nM IC50 J. Med. Chem. (2016) 59: 1925-1945 [PMID:26824643]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]