losartan [Ligand Id: 590] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL191 (Losartan, HGP1405, HGP-1405)
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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]
  • AT2 receptor/Angiotensin II type 2 (AT-2) receptor in Rat [ChEMBL: CHEMBL257] [GtoPdb: 35] [UniProtKB: P35351]
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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]
  • Type-1 angiotensin II receptor in Guinea pig [ChEMBL: CHEMBL1671613] [UniProtKB: Q9WV26]
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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 Inhibitory activity against angiotensin I converting enzyme (ACE) B 7.72 pIC50 19 nM IC50 J. Med. Chem. (2000) 43: 305-341 [PMID:10669559]
Angiotensin II type 1a (AT-1a) receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3374] [UniProtKB: P25104]
ChEMBL Concentration that gives 50% inhibition for binding of 125-I-[Sar1, IIe8] angiotensin to Angiotensin II receptor, type 1 in bovine adrenal cortex membrane. B 6.37 pIC50 425 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 369-374
ChEMBL Ability to displace [125I]- labelled [Sar1,Ileu8] from angiotensin II receptor of bovine adrenal cortex membranes B 6.38 pIC50 420 nM IC50 Bioorg. Med. Chem. Lett. (1992) 2: 1775-1779
ChEMBL In vitro Angiotensin II receptor antagonism in bovine adrenal cortex tissue. F 6.48 pIC50 330 nM IC50 Bioorg. Med. Chem. Lett. (1994) 4: 1703-1708
ChEMBL Binding affinity expressed as inhibitory concentration towards bovine adrenal cortex angiotensin II receptor was measured B 6.48 pIC50 330 nM IC50 Bioorg. Med. Chem. Lett. (1994) 4: 1709-1714
ChEMBL In vitro binding affinity to angiotensin II receptor in bovine adrenal cortex B 6.48 pIC50 330 nM IC50 Bioorg. Med. Chem. Lett. (1994) 4: 1819-1824
ChEMBL Binding affinity for angiotensin II receptor of bovine adrenal cortex B 6.52 pIC50 300 nM IC50 Bioorg. Med. Chem. Lett. (1994) 4: 183-188
ChEMBL Tested for binding affinity against angiotensin II receptor in bovine adrenal cortex B 6.8 pIC50 160 nM IC50 Bioorg. Med. Chem. Lett. (1995) 5: 2071-2076
ChEMBL Displacement of [125I]Ang2 from AT1 receptor in bovine adrenal cortex B 6.8 pIC50 160 nM IC50 Bioorg. Med. Chem. (2008) 16: 10301-10310 [PMID:18976926]
ChEMBL Displacement of [125 I]-AII (0.2 nM) from bovine adrenal cortical membrane angiotensin II (AII) receptor at 10e-7 M B 6.82 pIC50 150 nM IC50 Bioorg. Med. Chem. Lett. (1995) 5: 1903-1908
ChEMBL Inhibition of [125l]-All binding to bovine adrenal cortex B 6.92 pIC50 120 nM IC50 Bioorg. Med. Chem. Lett. (1994) 4: 177-182
ChEMBL Displacement of [125I]angiotensin-2 from bovine adrenal cortex AT1 receptor B 6.92 pIC50 120 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 2921-2926 [PMID:17412584]
ChEMBL In vitro for inhibition of [125I]-angiotensin II (0.1 nM) binding to angiotensin II receptor type 1 in membrane fractions of bovine adrenal cortex B 6.92 pIC50 120 nM IC50 J. Med. Chem. (1996) 39: 323-338 [PMID:8568823]
ChEMBL Displacement of [125I]AngII from type 1 angiotensin 2 receptor in bovine adrenal cortex B 7.02 pIC50 95 nM IC50 Bioorg. Med. Chem. (2012) 20: 4661-4667 [PMID:22750010]
ChEMBL Inhibition of [125I]AII binding to angiotensin II receptor of bovine adrenal cortex B 6.46 pEC50 350 nM EC50 Bioorg. Med. Chem. Lett. (1994) 4: 127-132
Angiotensin II type 1a (AT-1a) receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3948] [UniProtKB: P34976]
ChEMBL Antagonist activity at AT1 receptor in KCl-contracted rabbit aortic strips after 60 mins F 6.7 pKd 199.53 nM Kd J. Med. Chem. (2008) 51: 2137-2146 [PMID:18318468]
ChEMBL Antagonist activity against AT1 receptor in Japanese White rabbit aortic strips assessed as reduction in angiotension-2-induced contractile response after 60 mins by Schild's plot analysis B 7.7 pKd 19.95 nM Kd Eur. J. Med. Chem. (2015) 103: 473-487 [PMID:26397395]
ChEMBL Antagonist activity at angiotensin AT1 receptor in rabbit thoracic aortic rings F 7.9 pKd 12.59 nM Kd Bioorg. Med. Chem. (2010) 18: 8418-8456 [PMID:21071232]
ChEMBL Antagonist activity at AT1 receptor assessed inhibition of angiotensin-2-induced contraction of rabbit thoracic aortic rings F 7.9 pKd 12.59 nM Kd Bioorg. Med. Chem. Lett. (2007) 17: 2921-2926 [PMID:17412584]
ChEMBL Antagonist activity at angiotensin 2 AT1 receptor in Japanese White rabbits thoracic aorta assessed as inhibition of KCl-indcuced contraction after 60 mins F 7.9 pKd 12.59 nM Kd Eur. J. Med. Chem. (2012) 49: 183-190 [PMID:22309912]
ChEMBL Antagonist activity at AT1 receptor in Japanese white rabbit thoracic aorta assessed as inhibition of KCl-induced contraction incubated 30 mins post KCl-induction for 1 hr F 7.9 pKd 12.59 nM Kd Bioorg. Med. Chem. (2012) 20: 4208-4216 [PMID:22727371]
ChEMBL Compound was evaluated for in vitro potency against angiotensin II receptor, type 1 in isolated rabbit aorta; value ranges from 8.27-8.70 B 8.27 pKd 5.37 nM Kd J. Med. Chem. (1992) 35: 3714-3717 [PMID:1433184]
ChEMBL pA2 value determined in vitro against angiotensin II receptor, type 1 using rabbit aortic rings B 8.43 pKd 3.71 nM Kd Bioorg. Med. Chem. Lett. (1994) 4: 173-176
ChEMBL In vitro binding affinity against Angiotensin II receptor in rabbit aorta rings B 8.8 pKd 1.58 nM Kd Bioorg. Med. Chem. Lett. (1994) 4: 87-92
ChEMBL Antagonist activity at angiotensin 2 receptor type 1 in New Zealand White rabbit descending thoracic aorta rings assessed as inhibition of angiotensin 2-induced contraction preincubated for 30 mins prior angiotensin 2 challenge F 7.21 pIC50 61.12 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 1649-1654 [PMID:22264484]
ChEMBL In vitro antagonist activity against angiotensin II receptor type 1 in rabbit aorta using [125I]-Sar, Ile AII. F 7.27 pIC50 54 nM IC50 J. Med. Chem. (1993) 36: 4239-4249 [PMID:8277506]
ChEMBL In vitro antagonist activity against angiotensin II receptor type 1 in rabbit aorta using [125I]-Sar, Ile AII. F 7.27 pIC50 54 nM IC50 J. Med. Chem. (1993) 36: 4230-4238 [PMID:8277505]
ChEMBL Displacement of [1251][Sar1,IIe8]AII from rabbit aorta Angiotensin II receptor, type 1 B 7.27 pIC50 54 nM IC50 J. Med. Chem. (1993) 36: 3738-3742 [PMID:8246245]
ChEMBL Displacement of [125I]-Sar1-Ile8-A II at the rabbit aorta angiotensin II receptor, type 1 B 7.3 pIC50 50 nM IC50 J. Med. Chem. (1993) 36: 591-609 [PMID:8496939]
ChEMBL In vitro binding affinity for angiotensin II AT1 receptor in rabbit aorta B 7.3 pIC50 50 nM IC50 J. Med. Chem. (1994) 37: 4068-4072 [PMID:7990105]
ChEMBL In vitro antagonistic activity for angiotensin II receptor, type 1 by displacing 125I[Sar, ILe8 ]AII radioligand in rabbit aorta membrane without using bovine serum albumin (BSA) F 7.3 pIC50 50 nM IC50 J. Med. Chem. (1993) 36: 2558-2568 [PMID:8355255]
ChEMBL In vitro inhibitory activity against angiotensin II rabbit aorta AT1 receptor using radioligand [125I]-Sar Ile-AII B 7.4 pIC50 40 nM IC50 J. Med. Chem. (1994) 37: 2808-2824 [PMID:8064808]
ChEMBL Evaluation of Angiotensin II antagonistic activity by displacement of [125I]-Sar Ile-AII at the rabbit aorta Angiotensin II receptor, type 1 F 7.4 pIC50 40 nM IC50 J. Med. Chem. (1993) 36: 3595-3605 [PMID:8246227]
ChEMBL In vitro inhibitory activity against Angiotensin II receptor, type 1 in rabbit aorta membrane preparations. B 7.52 pIC50 30 nM IC50 J. Med. Chem. (1995) 38: 3741-3758 [PMID:7562905]
ChEMBL In vitro antagonistic activity for AT1 receptor by displacing 125I[Sar, ILe8]AII radioligand in rabbit aorta membrane using 0.2% bovine serum albumin (BSA) F 7.72 pIC50 19 nM IC50 J. Med. Chem. (1993) 36: 2558-2568 [PMID:8355255]
ChEMBL Antagonist activity against AT1 receptor assessed as inhibition of Ang2-induced rabbit aortic strip contraction F 8 pIC50 10 nM IC50 J. Med. Chem. (2006) 49: 6451-6464 [PMID:17064065]
ChEMBL Inhibitory activity against Angiotensin II receptor, type 1 induced contractions in isolated rabbit aortic rings F 8.52 pIC50 3 nM IC50 Bioorg. Med. Chem. Lett. (1994) 4: 1297-1302
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]-Ang II from pig uterus membrane angiotensin II type 2 (AT2) receptor B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2004) 47: 5995-6008 [PMID:15537354]
ChEMBL Displacement of [125I]Sar1 Ile8-Ang 2 from angiotensin 2 AT2 receptor after 180 mins by gamma counting B 5 pIC50 >10000 nM IC50 Eur. J. Med. Chem. (2012) 49: 183-190 [PMID:22309912]
ChEMBL Displacement of [125I]-Sar1Ile8-angiotensin 2 from angiotensin 2 AT2 receptor (unknown origin) after 180 mins by gamma counting analysis B 5 pIC50 >10000 nM IC50 Eur. J. Med. Chem. (2013) 69: 44-54 [PMID:24007859]
ChEMBL Binding affinity to type-2 angiotensin-2 receptor (unknown origin) B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 1355-1359 [PMID:26810314]
ChEMBL Antagonist activity at angiotensin 2 receptor F 7.72 pIC50 19 nM IC50 J. Med. Chem. (2011) 54: 2529-2591 [PMID:21413808]
AT2 receptor/Angiotensin II type 2 (AT-2) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL257] [GtoPdb: 35] [UniProtKB: P35351]
ChEMBL In vitro inhibitory activity against angiotensin II rat midbrain AT2 receptor using radioligand [125I]-Sar Ile-AII B 4.13 pIC50 74000 nM IC50 J. Med. Chem. (1994) 37: 2808-2824 [PMID:8064808]
ChEMBL In vitro binding affinity for angiotensin II AT2 receptor in rat midbrain B 4.3 pIC50 50000 nM IC50 J. Med. Chem. (1994) 37: 4068-4072 [PMID:7990105]
ChEMBL In vitro antagonist activity against angiotensin II receptor type 2 in rat midbrain using [125I]-Sar,Ile AII. F 4.52 pIC50 >30000 nM IC50 J. Med. Chem. (1993) 36: 4230-4238 [PMID:8277505]
ChEMBL In vitro antagonist activity against angiotensin II type 2 (AT2) receptor in rat midbrain using [125I]- Sar, Ile AII. F 4.52 pIC50 >30000 nM IC50 J. Med. Chem. (1993) 36: 4239-4249 [PMID:8277506]
ChEMBL Displacement of [1251][Sar1,IIe8]AII from rat midbrain angiotensin II (AT2) receptor B 4.52 pIC50 >30000 nM IC50 J. Med. Chem. (1993) 36: 3738-3742 [PMID:8246245]
ChEMBL Activity against low affinity Angiotensin II receptor, type 2 was measured from the ability to inhibit [125I]angiotensin II binding to rat uterine membrane B 5 pIC50 >10000 nM IC50 J. Med. Chem. (1993) 36: 101-110 [PMID:8421274]
ChEMBL In vitro inhibitory activity against Angiotensin II receptor, type 2 in rat midbrain membrane preparations. B 5.13 pIC50 7400 nM IC50 J. Med. Chem. (1995) 38: 3741-3758 [PMID:7562905]
Angiotensin type II receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163122] [UniProtKB: Q2XUH7]
ChEMBL Displacement of [125I]angiotensin 2 from AT2 receptor in pig uterus membrane after 1.5 hrs by gamma counting B 5 pKi >10000 nM Ki Bioorg. Med. Chem. (2010) 18: 4570-4590 [PMID:20493713]
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 5.54 pIC50 2882 nM IC50 DrugMatrix in vitro pharmacology data
Neutral endopeptidase/Neprilysin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944] [GtoPdb: 1611] [UniProtKB: P08473]
ChEMBL Inhibition of NEP (unknown origin) preincubated for 10 mins followed by fluorogenic substrate addition and measured after 20 mins by fluorescence assay B 5 pIC50 >10000 nM IC50 ACS Med Chem Lett (2019) 10: 86-91 [PMID:30655952]
Platelet glycoprotein VI (GPVI) in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3308912] [UniProtKB: Q9HCN6]
ChEMBL Antagonist activity at GP6 receptor in human platelet rich plasma assessed as inhibition of CVX-induced platelet aggregation preincubated for 5 mins followed by CVX addition measured after 5 mins by turbidimetric method B 4.96 pIC50 11000 nM IC50 J Med Chem (2017) 60: 322-337 [PMID:27996269]
ChEMBL Antagonist activity at GP6 receptor in human platelet rich plasma assessed as inhibition of collagen-induced platelet aggregation preincubated for 5 mins followed by collagen addition measured after 5 mins by turbidimetric method B 4.98 pIC50 10400 nM IC50 J Med Chem (2017) 60: 322-337 [PMID:27996269]
AT1 receptor in Human [GtoPdb: 34] [UniProtKB: P30556]
GtoPdb - - 8.7 pIC50 1.99 nM IC50 Heterogeneity of angiotensin receptor subtypes.. Medicinal Chemistry of the Renin-Angiotensin System. (1994);
Pharmacol Rev (1993) 45: 205-51 [PMID:8372104]
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 7.4 pKd 39.81 nM Kd Eur. J. Med. Chem. (2008) 43: 1808-1812 [PMID:18158200]
ChEMBL Antagonist activity at AT1 receptor in rat aortic rings F 8 pKd 10 nM Kd Bioorg. Med. Chem. (2008) 16: 10210-10215 [PMID:19013821]
ChEMBL Binding affinity against angiotensin II receptor from rat liver; n=8 B 7.84 pKi 14.6 nM Ki J. Med. Chem. (1993) 36: 2676-2688 [PMID:8410980]
ChEMBL Displacement of [125I]-Ang II from Angiotensin 2 type-1A receptor in rat vascular smooth muscle cells after 150 mins by gamma counting method B 7.86 pKi 13.86 nM Ki Bioorg. Med. Chem. (2016) 24: 2023-2031 [PMID:27004954]
ChEMBL Displacement of [125I]-Ang II from Angiotensin 2 type-1A receptor in rat vascular smooth muscle cells after 150 mins by gamma counting method B 7.72 pIC50 19.15 nM IC50 Bioorg. Med. Chem. (2016) 24: 2023-2031 [PMID:27004954]
ChEMBL Displacement of [125I]Sar1,Ile8-Ang2 from AT1 receptor in Wistar rat hepatic membrane B 8.17 pIC50 6.7 nM IC50 J. Med. Chem. (2008) 51: 2137-2146 [PMID:18318468]
AT1 receptor/Type-1 angiotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
ChEMBL Antagonist activity at angiotensin AT1 receptor F 8.48 pKd 3.31 nM Kd Bioorg. Med. Chem. (2010) 18: 8418-8456 [PMID:21071232]
ChEMBL Displacement of [3H]-Angiotensin 2 from AT1 receptor in human PLC/PRF/5 cells after 20 mins by liquid scintillation counting B 7.77 pKi 17 nM Ki J. Med. Chem. (2016) 59: 1925-1945 [PMID:26824643]
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 7.92 pKi 12 nM Ki J. Med. Chem. (2016) 59: 1925-1945 [PMID:26824643]
ChEMBL Displacement of Europium-labeled angiotensin-2 from human AT1 receptor expressed in CHOK1 cell membranes after 120 mins by DELFIA B 8.3 pKi 5.01 nM Ki ACS Med Chem Lett (2019) 10: 86-91 [PMID:30655952]
ChEMBL Inhibition of ATR1 (unknown origin) B 6.46 pIC50 350 nM IC50 J Med Chem (2019) 62: 8915-8930 [PMID:31083946]
ChEMBL In vitro inhibitory activity against angiotensin II receptor type 1, in human adrenal membrane preparations. B 7.06 pIC50 88 nM IC50 J. Med. Chem. (1995) 38: 3741-3758 [PMID:7562905]
ChEMBL Displacement of [125I]Sar1Ile8-Ang2 from human AT1 receptor expressed in CHO-K1 cell membranes after 180 mins B 7.54 pIC50 28.6 nM IC50 Eur. J. Med. Chem. (2015) 103: 473-487 [PMID:26397395]
ChEMBL Inhibition against human angiotensin II receptor, type 1 (AG2-R) B 7.55 pIC50 28 nM IC50 J. Med. Chem. (2004) 47: 888-899 [PMID:14761190]
ChEMBL Displacement of [125I]Sar1Ile8-Ang2 from angiotensin AT1 receptor after 180 mins by gamma counting B 7.79 pIC50 16.2 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 7.79 pIC50 16.2 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 7.79 pIC50 16.2 nM IC50 Eur. J. Med. Chem. (2013) 69: 44-54 [PMID:24007859]
ChEMBL Displacement of 125I-labelled Sar1-Ile8-angiotensin-2 from human AT1 receptor B 7.79 pIC50 16.2 nM IC50 MedChemComm (2015) 6: 1479-1483
ChEMBL Tested for inhibition of Angiotensin II receptor, type 1 in the absence of bovine serum albumin (BSA) B 8.1 pIC50 8 nM IC50 Bioorg. Med. Chem. Lett. (1994) 4: 29-34
ChEMBL Displacement of 125[I-Sar1-Ile8]ANG II from human AT1 receptor expressed in HEK293 membranes after 1 hr by gamma counting B 8.22 pIC50 6 nM IC50 Eur. J. Med. Chem. (2012) 55: 358-374 [PMID:22889560]
ChEMBL Displacement of [125I-Sar1-Ile8]-ANG2 from human Angiotensin 2 type-1 receptor expressed in HEK293 cells after 1 hr by gamma counting analysis B 8.25 pIC50 5.62 nM IC50 Eur. J. Med. Chem. (2013) 62: 352-370 [PMID:23376252]
ChEMBL Displacement of 125[I-Sar1-Ile8]ANG II from human AT1 receptor expressed in HEK293 membranes after 1 hr by gamma counting B 8.25 pIC50 5.62 nM IC50 Eur. J. Med. Chem. (2012) 55: 358-374 [PMID:22889560]
ChEMBL Displacement of [125I-Sar1-Ile8]Ang2 from human AT1 receptor expressed in HEK293 cell membrane incubated for 1 hr by gamma counting method B 8.49 pIC50 3.24 nM IC50 Bioorg. Med. Chem. (2016) 24: 4444-4451 [PMID:27480029]
GtoPdb - - 8.7 pIC50 1.99 nM IC50 Heterogeneity of angiotensin receptor subtypes.. Medicinal Chemistry of the Renin-Angiotensin System. (1994);
Pharmacol Rev (1993) 45: 205-51 [PMID:8372104]
ChEMBL Inhibition of angiotensin AT1 receptor B 9.48 pIC50 0.33 nM IC50 Bioorg. Med. Chem. (2012) 20: 4208-4216 [PMID:22727371]
Type-1 angiotensin II receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1671613] [UniProtKB: Q9WV26]
ChEMBL Inhibition of [125I]angiotensin binding to a guinea pig adrenal membrane preparation which corresponds to Angiotensin II receptor, type 1 B 7.74 pIC50 18 nM IC50 J. Med. Chem. (1993) 36: 1245-1254 [PMID:8487261]
ChEMBL Compound was tested for in vitro inhibition of specific binding of [I-125]AII to Angiotensin II receptor, type 1 in guinea pig adrenal membrane preparation B 7.74 pIC50 18 nM IC50 Bioorg. Med. Chem. Lett. (1994) 4: 2615-2620
AT1 receptor in Human [GtoPdb: 34] [UniProtKB: P30556]
GtoPdb - - 8.7 pIC50 1.99 nM IC50 Heterogeneity of angiotensin receptor subtypes.. Medicinal Chemistry of the Renin-Angiotensin System. (1994);
Pharmacol Rev (1993) 45: 205-51 [PMID:8372104]
AT1 receptor/Type-1B angiotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL263] [GtoPdb: 34] [UniProtKB: P29089]
ChEMBL In vitro antagonistic potency against angiotensin II receptor using [125I]- Sar,Ile8-angiotensin II as the radioligand in rat adrenal cortical membranes F 7.02 pKi 95 nM Ki J. Med. Chem. (1992) 35: 4751-4763 [PMID:1469703]
ChEMBL Compound was evaluated for binding affinity against angiotensin II receptor, type 1 in rat liver B 7.83 pKi 14.63 nM Ki J. Med. Chem. (1992) 35: 3714-3717 [PMID:1433184]
ChEMBL Displacement of [125I]-Sar1-Ile8-A II from rat adrenal Angiotensin-1 (AT-1) receptor B 8.44 pKi 3.6 nM Ki J. Med. Chem. (1994) 37: 2371-2386 [PMID:8057285]
ChEMBL Activity against high affinity Angiotensin II receptor, type 1 was measured from the ability to inhibit [125I]angiotensin II binding to rat uterine membrane. B 4.44 pIC50 36000 nM IC50 J. Med. Chem. (1993) 36: 101-110 [PMID:8421274]
ChEMBL Inhibition of [125-I]-labeled angiotensin II binding to AT1 receptor in rat uterine membranes B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (1994) 4: 2591-2596
ChEMBL Inhibition of [125I]angiotensin-II binding to the angiotensin II receptor type 1 in rat uterine membranes B 7.44 pIC50 36 nM IC50 J. Med. Chem. (1993) 36: 2172-2181 [PMID:8340920]
ChEMBL Inhibition of specific binding of [125I]angiotensin-II to angiotensin 1 receptor in rat lung membrane preparation B 7.46 pIC50 35 nM IC50 J. Med. Chem. (1993) 36: 4040-4051 [PMID:8258826]
ChEMBL Binding affinity against angiotensin II receptor in rat smooth muscle cell preparations B 7.59 pIC50 26 nM IC50 J. Med. Chem. (1991) 34: 3105-3114 [PMID:1920360]
ChEMBL In vitro antagonistic activity by displacement of [125I]-Sar1-Ile8-A II at the rat adrenal cortical aorta Angiotensin II receptor, type 1 F 7.72 pIC50 19 nM IC50 J. Med. Chem. (1993) 36: 591-609 [PMID:8496939]
ChEMBL Concentration required to inhibit binding of radioligand [125I]AII to angiotensin II receptor, type 1 in rat adrenal glomerulosa tissue B 7.72 pIC50 19 nM IC50 J. Med. Chem. (1992) 35: 2658-2667 [PMID:1635064]
ChEMBL Binding affinity for Angiotensin II receptor, type 1 measured by ability to displace [125I]- A II from its specific binding site in rat liver membrane B 7.85 pIC50 14 nM IC50 J. Med. Chem. (1993) 36: 3371-3380 [PMID:8230127]
ChEMBL Tested for binding affinity against angiotensin II receptor in rat adrenal cortex B 8.09 pIC50 8.2 nM IC50 Bioorg. Med. Chem. Lett. (1995) 5: 2071-2076
ChEMBL Binding affinity for rat angiotensin II receptor, type 1 B 8.17 pIC50 6.7 nM IC50 J. Med. Chem. (2004) 47: 2574-2586 [PMID:15115399]
ChEMBL Binding affinity against angiotensin II receptor type 1 (AT1) from rat liver. B 8.3 pIC50 5 nM IC50 J. Med. Chem. (1993) 36: 1735-1745 [PMID:8510101]

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, 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]