BDBM82258 CAS_114798-26-4::Losartan::NSC_3961
SMILES CCCCc1nc(Cl)c(CO)n1Cc1ccc(cc1)-c1ccccc1-c1nnn[nH]1
InChI Key InChIKey=PSIFNNKUMBGKDQ-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 82 hits for monomerid = 82258
Affinity DataKi: 5nMAssay Description:Displacement of Europium-labeled angiotensin-2 from human AT1 receptor expressed in CHOK1 cell membranes after 120 mins by DELFIAMore data for this Ligand-Target Pair
Affinity DataKi: 5.70nMAssay Description:Binding against Angiotensin II receptor in a radioligand binding assay using [125I]-Sar1-Ile8 angiotensin-II as radioligand in rat adrenal cortical m...More data for this Ligand-Target Pair
Affinity DataKi: 11nMAssay Description:Displacement of [125I]-Angiotensin II from Angiotensin II type-1 receptor in VSMC cells (unknown origin) assessed as inhibition constant by competiti...More data for this Ligand-Target Pair
Affinity DataKi: 12nMAssay Description:Displacement of [3H]-Asp-{Nomega-[N-(4-propanoylaminobutyl)aminocarbonyl]}Arg-ValTyr-Ile-His-Pro-Phe-OH Tris(hydrotrifluoroacetate) from human AT1 re...More data for this Ligand-Target Pair
TargetType-1 angiotensin II receptor A(RAT)
Parke-Davis Pharmaceutical Research
Curated by PDSP Ki Database
Parke-Davis Pharmaceutical Research
Curated by PDSP Ki Database
TargetType-1 angiotensin II receptor A(RAT)
Parke-Davis Pharmaceutical Research
Curated by PDSP Ki Database
Parke-Davis Pharmaceutical Research
Curated by PDSP Ki Database
Affinity DataKi: 14nMAssay Description:Displacement of [125I]-Ang II from Angiotensin 2 type-1A receptor in rat vascular smooth muscle cells after 150 mins by gamma counting methodMore data for this Ligand-Target Pair
Affinity DataKi: 15nMAssay Description:Compound was evaluated for binding affinity against angiotensin II receptor, type 1 in rat liverMore data for this Ligand-Target Pair
TargetType-1 angiotensin II receptor A(RAT)
Parke-Davis Pharmaceutical Research
Curated by PDSP Ki Database
Parke-Davis Pharmaceutical Research
Curated by PDSP Ki Database
Affinity DataKi: 15nMAssay Description:Binding affinity against angiotensin II receptor from rat liver; n=8More data for this Ligand-Target Pair
Affinity DataKi: 17nMAssay Description:Displacement of [3H]-Angiotensin 2 from AT1 receptor in human PLC/PRF/5 cells after 20 mins by liquid scintillation countingMore data for this Ligand-Target Pair
TargetType-1 angiotensin II receptor A/Type-1 angiotensin II receptor B/Type-2 angiotensin II receptor(RAT)
Glaxo Research And Development
Curated by ChEMBL
Glaxo Research And Development
Curated by ChEMBL
Affinity DataKi: 32nMAssay Description:Tested for in vitro binding affinity against angiotensin II receptor of rat liverMore data for this Ligand-Target Pair
Affinity DataKi: 95nMAssay Description:In vitro antagonistic potency against angiotensin II receptor using [125I]- Sar,Ile8-angiotensin II as the radioligand in rat adrenal cortical membra...More data for this Ligand-Target Pair
TargetSolute carrier organic anion transporter family member 1B1(Homo sapiens (Human))
Ku Leuven
Curated by ChEMBL
Ku Leuven
Curated by ChEMBL
Affinity DataKi: 160nMAssay Description:Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cellsMore data for this Ligand-Target Pair
TargetSolute carrier organic anion transporter family member 1B3(Homo sapiens (Human))
Ku Leuven
Curated by ChEMBL
Ku Leuven
Curated by ChEMBL
Affinity DataKi: 890nMAssay Description:Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cellsMore data for this Ligand-Target Pair
Affinity DataKi: >1.00E+4nMAssay Description:Displacement of [125I]angiotensin 2 from AT2 receptor in pig uterus membrane after 1.5 hrs by gamma countingMore data for this Ligand-Target Pair
Affinity DataKd: 12.6nMAssay Description:Antagonist activity at angiotensin AT1 receptor in rabbit thoracic aortic ringsMore data for this Ligand-Target Pair
Affinity DataIC50: 3nMAssay Description:Inhibitory activity against Angiotensin II receptor, type 1 induced contractions in isolated rabbit aortic ringsMore data for this Ligand-Target Pair
TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3A/3B(Homo sapiens (Human))
RhôNe-Poulenc Rorer
Curated by ChEMBL
RhôNe-Poulenc Rorer
Curated by ChEMBL
Affinity DataIC50: 1.30E+4nMAssay Description:Inhibition of guinea pig ventricular Phosphodiesterase 3 (PDE 3)More data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A/4B/4C/4D(Homo sapiens (Human))
RhôNe-Poulenc Rorer
Curated by ChEMBL
RhôNe-Poulenc Rorer
Curated by ChEMBL
Affinity DataIC50: 2.60E+4nMAssay Description:Inhibitory effect in cAMP-specific Phosphodiesterase 4 (PDE 4) isolated from guinea pig ventricular tissue.More data for this Ligand-Target Pair
TargetSolute carrier organic anion transporter family member 1B1(Homo sapiens (Human))
Ku Leuven
Curated by ChEMBL
Ku Leuven
Curated by ChEMBL
Affinity DataIC50: 288nMAssay Description:pIC50 values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cellsMore data for this Ligand-Target Pair
TargetSolute carrier organic anion transporter family member 1B3(Homo sapiens (Human))
Ku Leuven
Curated by ChEMBL
Ku Leuven
Curated by ChEMBL
Affinity DataIC50: 1.15E+3nMAssay Description:pIC50 values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cellsMore data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Binding affinity to type-2 angiotensin-2 receptor (unknown origin)More data for this Ligand-Target Pair
TargetType-1 angiotensin II receptor A(RAT)
Parke-Davis Pharmaceutical Research
Curated by PDSP Ki Database
Parke-Davis Pharmaceutical Research
Curated by PDSP Ki Database
Affinity DataIC50: 19nMAssay Description:Displacement of [125I]-Ang II from Angiotensin 2 type-1A receptor in rat vascular smooth muscle cells after 150 mins by gamma counting methodMore data for this Ligand-Target Pair
Affinity DataIC50: 3.20nMAssay Description:Displacement of [125I-Sar1-Ile8]Ang2 from human AT1 receptor expressed in HEK293 cell membrane incubated for 1 hr by gamma counting methodMore data for this Ligand-Target Pair
Affinity DataIC50: 61.1nMAssay Description:Antagonist activity at angiotensin 2 receptor type 1 in New Zealand White rabbit descending thoracic aorta rings assessed as inhibition of angiotensi...More data for this Ligand-Target Pair
Affinity DataIC50: 16.2nMAssay Description:Displacement of [125I]Sar1 Ile8-Ang 2 from angiotensin 2 AT1 receptor after 180 mins by gamma countingMore data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Displacement of [125I]Sar1 Ile8-Ang 2 from angiotensin 2 AT2 receptor after 180 mins by gamma countingMore data for this Ligand-Target Pair
Affinity DataIC50: 19nMAssay Description:Inhibitory activity against angiotensin I converting enzyme (ACE)Checked by AuthorMore data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Displacement of [125I]-Ang II from pig uterus membrane angiotensin II type 2 (AT2) receptorMore data for this Ligand-Target Pair
Affinity DataKd: 12.6nMAssay Description:Antagonist activity at angiotensin 2 AT1 receptor in Japanese White rabbits thoracic aorta assessed as inhibition of KCl-indcuced contraction after 6...More data for this Ligand-Target Pair
TargetMultidrug and toxin extrusion protein 1(Homo sapiens (Human))
University Of California
Curated by ChEMBL
University Of California
Curated by ChEMBL
Affinity DataIC50: >2.50E+5nMAssay Description:Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assayMore data for this Ligand-Target Pair
TargetType-1 angiotensin II receptor A(RAT)
Parke-Davis Pharmaceutical Research
Curated by PDSP Ki Database
Parke-Davis Pharmaceutical Research
Curated by PDSP Ki Database
Affinity DataIC50: 6.70nMAssay Description:Displacement of [125I]Sar1,Ile8-Ang2 from AT1 receptor in Wistar rat hepatic membraneMore data for this Ligand-Target Pair
Affinity DataIC50: 19nMAssay Description:Antagonist activity at angiotensin 2 receptorMore data for this Ligand-Target Pair
Affinity DataKd: 200nMAssay Description:Antagonist activity at AT1 receptor in KCl-contracted rabbit aortic strips after 60 minsMore data for this Ligand-Target Pair
Affinity DataKd: 3.72nMAssay Description:pA2 value determined in vitro against angiotensin II receptor, type 1 using rabbit aortic ringsMore data for this Ligand-Target Pair
Affinity DataKd: 1.58nMAssay Description:In vitro binding affinity against Angiotensin II receptor in rabbit aorta ringsMore data for this Ligand-Target Pair
Affinity DataIC50: 95nMAssay Description:Displacement of [125I]AngII from type 1 angiotensin 2 receptor in bovine adrenal cortexMore data for this Ligand-Target Pair
Affinity DataIC50: 5.62nMAssay Description:Displacement of 125[I-Sar1-Ile8]ANG II from human AT1 receptor expressed in HEK293 membranes after 1 hr by gamma countingMore data for this Ligand-Target Pair
Affinity DataIC50: 6nMAssay Description:Displacement of 125[I-Sar1-Ile8]ANG II from human AT1 receptor expressed in HEK293 membranes after 1 hr by gamma countingMore data for this Ligand-Target Pair
Affinity DataIC50: 16.2nMAssay Description:Displacement of [125I]Sar1Ile8-Ang2 from angiotensin AT1 receptor after 180 mins by gamma countingMore data for this Ligand-Target Pair
Affinity DataKd: 12.6nMAssay Description:Antagonist activity at AT1 receptor in Japanese white rabbit thoracic aorta assessed as inhibition of KCl-induced contraction incubated 30 mins post ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.330nMAssay Description:Inhibition of angiotensin AT1 receptorMore data for this Ligand-Target Pair
TargetType-1 angiotensin II receptor A/Type-1 angiotensin II receptor B/Type-2 angiotensin II receptor(RAT)
Glaxo Research And Development
Curated by ChEMBL
Glaxo Research And Development
Curated by ChEMBL
Affinity DataIC50: 19nMAssay Description:Inhibition of radioligand [3H]angiotensin II binding to angiotensin II receptor of rat adrenal cortical membraneMore data for this Ligand-Target Pair
TargetType-1/Type-2 angiotensin II receptor(Homo sapiens (Human))
Exploratory Chemistry Merck Sharp And Dohme Research Laboratories
Curated by ChEMBL
Exploratory Chemistry Merck Sharp And Dohme Research Laboratories
Curated by ChEMBL
Affinity DataIC50: 50nMAssay Description:Binding affinity towards Angiotensin receptor from rabbit aortaMore data for this Ligand-Target Pair
TargetType-1 angiotensin II receptor A/Type-1 angiotensin II receptor B/Type-2 angiotensin II receptor(RAT)
Glaxo Research And Development
Curated by ChEMBL
Glaxo Research And Development
Curated by ChEMBL
Affinity DataIC50: 13nMAssay Description:Competitive inhibition of Angiotensin II receptor binding of radiolabeled AII to rat adrenal glomerulosa tissue by 50%More data for this Ligand-Target Pair