[3H]losartan [Ligand Id: 3941] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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] |
| 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/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] |
| GtoPdb | - | - | 8.21 | pKd | 6.2 | nM | Kd | Eur J Pharmacol (1993) 247: 193-8 [PMID:8282008] |
| 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] |
| ChEMBL | Inhibition of angiotensin AT1 receptor | B | 9.48 | pIC50 | 0.33 | nM | IC50 | Bioorg Med Chem (2012) 20: 4208-4216 [PMID:22727371] |
| AT1 receptor in Rat [GtoPdb: 34] [UniProtKB: P29089, P25095] | ||||||||
| GtoPdb | - | - | 8.21 | pKd | 6.2 | nM | Kd | Eur J Pharmacol (1993) 247: 193-8 [PMID:8282008] |
| 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/Type-1B angiotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL263] [GtoPdb: 34] [UniProtKB: P29089] | ||||||||
| GtoPdb | - | - | 8.21 | pKd | 6.2 | nM | Kd | Eur J Pharmacol (1993) 247: 193-8 [PMID:8282008] |
| 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 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]
