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

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ChEMBL ligand: CHEMBL1016 (Blopress, Candemore, Candesartan, Candesartan cilexetil related compound g, CV-11974, NSC-759858)
  • 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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  • BLT2 receptor/Leukotriene B4 receptor 2 in Human [ChEMBL: CHEMBL3191] [GtoPdb: 268] [UniProtKB: Q9NPC1]
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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
GroEL/GroES in Escherichia coli (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106139] [UniProtKB: Q548M1, Q7BGE6]
ChEMBL Inhibition of Escherichia coli GroEL expressed in Escherichia coliDH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured soluble pig heart MDH refolding by measuring MDH enzyme activity using sodium mesoxalate as substrate after 20 to 40 mins by malachite green dye based spectrometric analysis B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (2019) 29: 1106-1112 [PMID:30852084]
HSP60/HSP10 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106131] [UniProtKB: P10809, P61604]
ChEMBL Inhibition of human N-terminal octa-His-tagged HSP60 expressed in Escherichia coli Rosetta(DE3) pLysS/human HSP10 expressed in Escherichia coli Rosetta(DE3) assessed as reduction in HSP60/HSP10-mediated denatured MDH refolding by measuring MDH enzyme activity using sodium mesoxalate as substrate after 40 to 60 mins by malachite green dye based spectrometric analysis B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (2019) 29: 1106-1112 [PMID:30852084]
BLT2 receptor/Leukotriene B4 receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3191] [GtoPdb: 268] [UniProtKB: Q9NPC1]
ChEMBL Agonist activity at human BLT2 overexpressed in CHO-K1 cells assessed as accumulation of inositol monophosphate measured after 90 mins by HTRF assay F 4.82 pEC50 15000 nM EC50 ACS Med Chem Lett (2021) 12: 1261-1266 [PMID:34413955]
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 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]