Angiotensin Ii

Summary

Angiotensin Ii (CHEMBL408403) is an approved protein (ATC C01CX09) targeting AGTR1, AGTR2, and KCNK3; indicated across 6 conditions including cardiovascular disorder and toxic shock syndrome.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Protein
• ATC class: C01CX09
• Targets: 3 (AGTR1, AGTR2, KCNK3)
• Indications: 6 conditions
• Clinical trials: 36
• Chemistry: 1046.2 Da · C50H71N13O12

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL408403
Name	Angiotensin Ii
Type	Protein
Max phase	4
FDA approved	yes
PubChem CID	172198
ChEBI	CHEBI:2719
ATC	C01CX09
Molecular formula	C50H71N13O12
Molecular weight	1046.2
InChIKey	CZGUSIXMZVURDU-JZXHSEFVSA-N

SMILES: CC[C@H](C)[C@@H](C(=O)N[C@@H](CC1=CN=CN1)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC3=CC=CC=C3)C(=O)O)NC(=O)[C@H](CC4=CC=C(C=C4)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(=O)O)N

IUPAC name: (3S)-3-amino-4-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[(2S)-2-[[(1S)-1-carboxy-2-phenylethyl]carbamoyl]pyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-oxobutanoic acid

ChEBI definition: An angiotensin II that acts on the central nervous system (PDB entry: 1N9V).

Other ChEBI roles (chemical / environmental): human metabolite.

Also known as: Angiotensin ii, Angiotensin ii (human type), Angiotensin ii human, Angiotensina ii, Angiotensine ii, Asp-arg-val-tyr-ile-his-pro-phe, Delivert, LJPC-501, Asp-Arg-Val-Tyr-Ile-His-Pro-Phe, Angiotensin II, Asp-Arg-Val-Tyr-Val-His-Pro-Phe, DRVWIHPF

Parent form; salt/anhydrous children: CHEMBL3989932, CHEMBL4303682

Patent coverage: 24,661 distinct patent families (76,759 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 74,734 (97%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
AGTR1	AT1 receptor	Full agonist	9.3	0.4%	P30556
AGTR2	AT2 receptor	Full agonist	10.2	0.1%	P50052
KCNK3	K2P3.1			0%	O14649

Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Angiotensin II receptor, Angiotensin II receptor (AT-1) type-1, Type-1 angiotensin II receptor, Type-1 angiotensin II receptor B, Type-1 angiotensin II receptor A, Type-1 angiotensin II receptor, Type-2 angiotensin II receptor.

Bioactivity

ChEMBL activities: 54 potent at pChembl ≥ 5 of 54 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
AGTR2	10.1	IC50	0.08	nM	CHEMBL_ACT_16838406
P25095	10	Ki	0.1	nM	CHEMBL_ACT_1771934
AGTR1	9.8	Ki	0.16	nM	CHEMBL_ACT_16528777
AGTR2	9.7	Ki	0.2	nM	CHEMBL_ACT_1613084
AGTR2	9.7	Ki	0.2	nM	CHEMBL_ACT_16466553
AGTR2	9.64	Ki	0.23	nM	CHEMBL_ACT_1512957
AGTR2	9.64	Ki	0.23	nM	CHEMBL_ACT_233722
P25095	9.62	Ki	0.24	nM	CHEMBL_ACT_1512956
AGTR1	9.62	Ki	0.24	nM	CHEMBL_ACT_16528718
P25095	9.62	Ki	0.24	nM	CHEMBL_ACT_233721
AGTR2	9.52	Ki	0.3	nM	CHEMBL_ACT_1825564
P29089	9.51	Ki	0.31	nM	CHEMBL_ACT_545583
P25095	9.4	IC50	0.4	nM	CHEMBL_ACT_2153788
P29089	9.4	IC50	0.4	nM	CHEMBL_ACT_633599
AGTR1	9.31	EC50	0.49	nM	CHEMBL_ACT_16528695
P25095	9.3	Ki	0.5	nM	CHEMBL_ACT_1825563
AGTR1	9.3	Ki	0.5	nM	CHEMBL_ACT_3189712
AGTR1	9.28	EC50	0.52	nM	CHEMBL_ACT_16528694
P25095	9.28	Ki	0.53	nM	CHEMBL_ACT_643058
P25095	9.28	IC50	0.53	nM	CHEMBL_ACT_99610
AGTR2	9.22	Ki	0.6	nM	CHEMBL_ACT_1772346
AGTR2	9.21	IC50	0.62	nM	CHEMBL_ACT_23163732
AGTR2	9.18	Ki	0.66	nM	CHEMBL_ACT_29081083
AGTR1	9.14	IC50	0.72	nM	CHEMBL_ACT_16528724
AGTR2	9.12	Ki	0.76	nM	CHEMBL_ACT_29081074
AGTR2	9.05	Ki	0.9	nM	CHEMBL_ACT_27155612
AGTR1	9.05	Ki	0.9	nM	CHEMBL_ACT_3189729
P29089	9.02	Ki	0.95	nM	CHEMBL_ACT_1613083
AGTR1	9	EC50	1	nM	CHEMBL_ACT_29081119
P25095	8.99	IC50	1.02	nM	CHEMBL_ACT_42001

Target pathways

Aggregated over 3 target gene(s): AGTR1, AGTR2, KCNK3.

Top Reactome pathways

19 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	2	AGTR1, AGTR2
Signaling by GPCR	2	AGTR1, AGTR2
Class A/1 (Rhodopsin-like receptors)	2	AGTR1, AGTR2
Peptide ligand-binding receptors	2	AGTR1, AGTR2
GPCR downstream signalling	2	AGTR1, AGTR2
GPCR ligand binding	2	AGTR1, AGTR2
Neuronal System	1	KCNK3
Potassium Channels	1	KCNK3
Tandem pore domain potassium channels	1	KCNK3
TWIK-releated acid-sensitive K+ channel (TASK)	1	KCNK3
Membrane Trafficking	1	AGTR1
Muscle contraction	1	KCNK3
G alpha (q) signalling events	1	AGTR1
G alpha (i) signalling events	1	AGTR2
Phase 4 - resting membrane potential	1	KCNK3
Cardiac conduction	1	KCNK3
Vesicle-mediated transport	1	AGTR1
Cargo recognition for clathrin-mediated endocytosis	1	AGTR1
Clathrin-mediated endocytosis	1	AGTR1

Dominant GO biological processes

GO term	Targets
inflammatory response	2
G protein-coupled receptor signaling pathway	2
angiotensin-activated signaling pathway	2
blood vessel diameter maintenance	2
signal transduction	2
regulation of cell growth	1
kidney development	1
renin-angiotensin regulation of aldosterone production	1
maintenance of blood vessel diameter homeostasis by renin-angiotensin	1
regulation of systemic arterial blood pressure by renin-angiotensin	1
phospholipase C-activating G protein-coupled receptor signaling pathway	1
positive regulation of cytosolic calcium ion concentration	1
Rho protein signal transduction	1
positive regulation of macrophage derived foam cell differentiation	1
regulation of vasoconstriction	1

Indications & clinical

Indications

6 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
cardiovascular disorder	4	MONDO:0004995	EFO:0000319
toxic shock syndrome	3	MONDO:0001881	EFO:0006834
hypertensive disorder	3	MONDO:0005044	EFO:0000537
postural orthostatic tachycardia syndrome	1	MONDO:0011479	EFO:1000645
hepatorenal syndrome	1	MONDO:0001382	MONDO:0001382
preeclampsia	0	MONDO:0005081	EFO:0000668

Clinical trials

Total trials: 36.

Phase distribution

Phase	Trials
PHASE4	12
Not specified	9
PHASE3	5
PHASE1	5
PHASE2	3
PHASE2/PHASE3	1
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04592744	PHASE4	ENROLLING_BY_INVITATION	Angiotensin 2 for AKI After OLT
NCT06122987	PHASE4	RECRUITING	Hemodynamic Response to Angiotensin-II When Used as the Second Vasopressor Agent for Septic Shock
NCT06487585	PHASE4	RECRUITING	ANG-First Trial (Angiotensin II as First-Line Vasopressor Therapy in Cardiac Surgery)
NCT06746753	PHASE4	NOT_YET_RECRUITING	Mechanistic Assessment of Norepinephrine Therapy vs. Angiotensin-II in Septic Shock
NCT07212686	PHASE4	ENROLLING_BY_INVITATION	Synthetic Angiotensin II/Giapreza in Pediatric Patients With Refractory Hypotension
NCT01502787	PHASE4	COMPLETED	Comparison of Nebivolol and Metoprolol With Exercise and Angiotensin II in Hypertensive Patients
NCT03733145	PHASE4	COMPLETED	Angiotensin II in General Anesthesia
NCT04529005	PHASE4	COMPLETED	Angiotensin II in the Perioperative Management of Hypotension in Kidney Transplant Recipients
NCT04558359	PHASE4	COMPLETED	Renin and Renal Biomarker Response to Angiotensin II
NCT04904562	PHASE4	TERMINATED	Angiotensin II for Distributive Shock
NCT05193370	PHASE4	WITHDRAWN	Angiotensin II vs. Vasopressin in Septic Shock
NCT05824767	PHASE4	COMPLETED	Serum Biomarkers to Predict Response to Angiotensin II in Septic Shock
NCT04901169	PHASE2/PHASE3	ACTIVE_NOT_RECRUITING	Angiotensin II in Liver Transplantation
NCT06615102	PHASE3	RECRUITING	Reducing Cardiac-surgery Associated Acute Kidney Injury Occurence by Administering Angiotensin II
NCT01508468	PHASE3	COMPLETED	Evaluate Rituximab Treatment for Idiopathic Membranous Nephropathy
NCT02338843	PHASE3	COMPLETED	A Phase 3 Study of LJPC-501 in Patients With Catecholamine-Resistant Hypotension
NCT03302650	PHASE3	SUSPENDED	Angiotensin II for Septic Shock Treatment
NCT05199493	PHASE3	COMPLETED	Reducing Acute Kidney Injury Occurence by Administering Angiotensin II
NCT00711789	PHASE2	UNKNOWN	Angiotensin in Septic Kidney Injury Trial
NCT03431077	PHASE2	COMPLETED	A Study of LJPC-501 in Pediatric Patients With Hypotension
NCT04048707	PHASE2	WITHDRAWN	Angiotensin 2 for Hepatorenal Syndrome
NCT01426529	PHASE1	ACTIVE_NOT_RECRUITING	Caveolin-1 and Vascular Dysfunction
NCT02966665	PHASE1	RECRUITING	: Vascular Function in Health and Disease
NCT00962949	PHASE1	COMPLETED	The Renin-Aldosterone Axis in Postural Tachycardia Syndrome
NCT01393782	PHASE1	COMPLETED	Intravenous AII for the Treatment of Severe Hypotension in High Output Shock: A Pilot Study
NCT01906307	PHASE1	TERMINATED	A Phase 1 Study of LJPC-501 in Patients With Hepatorenal Syndrome
NCT06157580	EARLY_PHASE1	COMPLETED	Balance of Angiotensin II Receptors in Vessel Function After Preeclampsia
NCT06234592	Not specified	RECRUITING	The Effect of Vasopressor Therapy on Renal Perfusion in Septic Shock
NCT00901745	Not specified	COMPLETED	Interaction of Apelin and Angiotensin in the Human Forearm Circulation
NCT01024543	Not specified	COMPLETED	Role of Angiotensin II in Insulin-induced Microvascular Activity
NCT01049646	Not specified	COMPLETED	Interaction of Apelin and Angiotensin in the Systemic Circulation
NCT01456208	Not specified	TERMINATED	Genetic Mechanisms in Human Hypertension
NCT01511042	Not specified	TERMINATED	Vascular Dysfunction in Diabetes: Genes and Hormones
NCT01702688	Not specified	WITHDRAWN	Evaluation of Lysine-Specific Demethylase 1
NCT03245528	Not specified	APPROVED_FOR_MARKETING	Expanded Access for LJPC-501
NCT04408326	Not specified	UNKNOWN	Efficacy and Safety of Angiotensin II Use in Coronavirus Disease(COVID)-19 Patients With Acute Respiratory Distress Syndrome

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

158 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
LOSARTAN	ChEMBL + PubChem	Phase 4 (approved)	AGTR1, AGTR2
OLMESARTAN MEDOXOMIL	ChEMBL + PubChem	Phase 4 (approved)	AGTR1, AGTR2
CANDESARTAN CILEXETIL	ChEMBL	Phase 4 (approved)	AGTR1, AGTR2
IRBESARTAN	ChEMBL	Phase 4 (approved)	AGTR1, AGTR2
SARALASIN	ChEMBL	Phase 4 (approved)	AGTR1, AGTR2
TELMISARTAN	ChEMBL	Phase 4 (approved)	AGTR1, AGTR2
OLMESARTAN	ChEMBL + PubChem	Phase 3 (approved)	AGTR1, AGTR2
CANDESARTAN	ChEMBL	Phase 3	AGTR1, AGTR2
FORASARTAN	ChEMBL	Phase 2	AGTR1, AGTR2
OLODANRIGAN	ChEMBL	Phase 2	AGTR1, AGTR2
PRATOSARTAN	ChEMBL	Phase 2	AGTR1, AGTR2
TASOSARTAN	ChEMBL	Phase 2	AGTR1, AGTR2
Anagrelide	PubChem	Approved	AGTR1, AGTR2
CRIZOTINIB	ChEMBL + PubChem	Phase 4 (approved)	AGTR1
MEXILETINE	ChEMBL + PubChem	Phase 4 (approved)	KCNK3
PROPAFENONE	ChEMBL + PubChem	Phase 4 (approved)	KCNK3
RIFAMPIN	ChEMBL + PubChem	Phase 4 (approved)	AGTR1
ROPIVACAINE	ChEMBL + PubChem	Phase 4 (approved)	KCNK3
SPARSENTAN	ChEMBL + PubChem	Phase 4 (approved)	AGTR1
TEGASEROD	ChEMBL + PubChem	Phase 4 (approved)	AGTR1
ALFACALCIDOL	ChEMBL	Phase 4 (approved)	AGTR1
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	AGTR1
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	AGTR1
AZILSARTAN MEDOXOMIL	ChEMBL	Phase 4 (approved)	AGTR2
BALSALAZIDE	ChEMBL	Phase 4 (approved)	AGTR1
BENAZEPRIL	ChEMBL	Phase 4 (approved)	AGTR2
BENZBROMARONE	ChEMBL	Phase 4 (approved)	AGTR1
BUPIVACAINE	ChEMBL	Phase 4 (approved)	KCNK3
BUTOCONAZOLE	ChEMBL	Phase 4 (approved)	AGTR1
CALCITRIOL	ChEMBL	Phase 4 (approved)	AGTR1
CARVEDILOL	ChEMBL	Phase 4 (approved)	AGTR1
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	AGTR1
DABIGATRAN ETEXILATE	ChEMBL	Phase 4 (approved)	AGTR1
DESOGESTREL	ChEMBL	Phase 4 (approved)	AGTR1
DICLOFENAC	ChEMBL	Phase 4 (approved)	AGTR2
DISULFIRAM	ChEMBL	Phase 4 (approved)	AGTR1
DOFETILIDE	ChEMBL	Phase 4 (approved)	AGTR1
DONEPEZIL	ChEMBL	Phase 4 (approved)	AGTR1
EFAVIRENZ	ChEMBL	Phase 4 (approved)	AGTR1
EPALRESTAT	ChEMBL	Phase 4 (approved)	AGTR1
EPROSARTAN	ChEMBL	Phase 4 (approved)	AGTR1
ETIDOCAINE	ChEMBL	Phase 4 (approved)	KCNK3
FELODIPINE	ChEMBL	Phase 4 (approved)	AGTR1
FENTICONAZOLE	ChEMBL	Phase 4 (approved)	AGTR1
GUAIFENESIN	ChEMBL	Phase 4 (approved)	AGTR1
HALOPERIDOL	ChEMBL	Phase 4 (approved)	AGTR1
IBANDRONIC ACID	ChEMBL	Phase 4 (approved)	AGTR1
INDOCYANINE GREEN ACID FORM	ChEMBL	Phase 4 (approved)	AGTR1
IVACAFTOR	ChEMBL	Phase 4 (approved)	AGTR1
LEFLUNOMIDE	ChEMBL	Phase 4 (approved)	AGTR1
LOVASTATIN	ChEMBL	Phase 4 (approved)	AGTR1
MICONAZOLE	ChEMBL	Phase 4 (approved)	AGTR2
MILTEFOSINE	ChEMBL	Phase 4 (approved)	AGTR1
NIFEDIPINE	ChEMBL	Phase 4 (approved)	AGTR1
NIMESULIDE	ChEMBL	Phase 4 (approved)	AGTR1
NITAZOXANIDE	ChEMBL	Phase 4 (approved)	AGTR1
NORGESTIMATE	ChEMBL	Phase 4 (approved)	AGTR1
NOSCAPINE	ChEMBL	Phase 4 (approved)	AGTR1
OXYMETHOLONE	ChEMBL	Phase 4 (approved)	AGTR1
PIMOZIDE	ChEMBL	Phase 4 (approved)	AGTR1