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ChEMBL ligand: CHEMBL191 (Allisartan, Angizaar, Dup-89, E-3174, Exp-3174, EXP3174, HGP-1405, HGP1405, Losartan, Losartan carboxylic acid, Losartic, Lozap, NSC-758699) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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: 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 | 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 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 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 | 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 | Displacement of [125I]Sar1,I1e8-AII from AT1 receptor in rabbit aorta membrane | B | 7.4 | pIC50 | 40 | nM | IC50 | RSC Med Chem (2022) 13: 1300-1321 [PMID:36439976] |
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] |
ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] | ||||||||
ChEMBL | Inhibition of ABCG2 (unknown origin) expressed in human HEK293-A cells membrane vesicles assessed inhibition of ABCG2-mediated urate transport activity by rapid filtration technique | B | 4.46 | pIC50 | 35000 | nM | IC50 | Eur J Med Chem (2022) 237: 114346-114346 [PMID:35483322] |
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] |
ChEMBL | Antagonist activity at GP6 in human platelet assessed as reduction in collagen-induced platelet-aggregation preincubated for 60 secs followed by collagen stimulation by light transmission aggregometry | B | 5.4 | pIC50 | 4000 | nM | IC50 | J Med Chem (2020) 63: 12213-12242 [PMID:32463237] |
ChEMBL | Antagonist activity at GP6 in human platelet assessed as reduction in CRP-induced platelet-aggregation preincubated for 60 secs followed by collagen stimulation by light transmission aggregometry | B | 5.4 | pIC50 | 4000 | nM | IC50 | J Med Chem (2020) 63: 12213-12242 [PMID:32463237] |
TP receptor/Thromboxane A2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069] [GtoPdb: 346] [UniProtKB: P21731] | ||||||||
ChEMBL | Modulation of TxA2 receptor in human platelets assessed as reduction in U46619-induced platelet aggregation preincubated for 5 min followed by U46619 stimulation | B | 4.7 | pIC50 | 20000 | nM | IC50 | J Med Chem (2020) 63: 12213-12242 [PMID:32463237] |
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 [125I]-Angiotensin II from Angiotensin II type-1 receptor in VSMC cells (unknown origin) assessed as inhibition constant by competition radioligand binding assay | B | 7.98 | pKi | 10.5 | nM | Ki | Bioorg Med Chem Lett (2023) 90: 129349-129349 [PMID:37236375] |
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 | Displacement of [125I]-Angiotensin II from Angiotensin II type-1 receptor in VSMC cells (unknown origin) by competition radioligand binding assay | B | 7.83 | pIC50 | 14.64 | nM | IC50 | Bioorg Med Chem Lett (2023) 90: 129349-129349 [PMID:37236375] |
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 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]