Angiotensin
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Also known as US10370388Compound Angiotensin
Summary
Angiotensin (CHEMBL2391146) is a phase-3 clinical-stage protein targeting MAS1 and AGTR2; indicated across 3 conditions including hypertensive disorder and kidney disorder.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Protein
- Targets: 2 (MAS1, AGTR2)
- Indications: 3 conditions
- Clinical trials: 1
- Chemistry: 956.1 Da · C43H65N13O12
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL2391146 |
| Name | Angiotensin |
| Type | Protein |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 15171724 |
| Molecular formula | C43H65N13O12 |
| Molecular weight | 956.1 |
| InChIKey | JSQIKKVBLLHQSQ-AWJAZODESA-N |
SMILES: C[C@@H](C(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC2=CN=CN2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CC3=CC=C(C=C3)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)-1-[[(2S)-1-[(2S)-2-[[(1S)-1-carboxyethyl]carbamoyl]pyrrolidin-1-yl]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-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
Also known as: Angiotensin, ANGIOTENSIN, US10370388, Compound Angiotensin
Patent coverage: 478 distinct patent families (703 SureChEMBL compound mentions), from 1 matched compound structure(s). 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 |
|---|---|---|---|---|---|
| MAS1 | MAS1 | Agonist | 7.31 | P04201 | |
| AGTR2 | AT2 receptor | Agonist | 6.61 | 0.1% | P50052 |
Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Type-2 angiotensin II receptor.
Bioactivity
ChEMBL activities: 3 potent at pChembl ≥ 5 of 3 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| AGTR2 | 9.89 | IC50 | 0.13 | nM | CHEMBL_ACT_13336212 |
| AGTR2 | 9.05 | Ki | 0.9 | nM | CHEMBL_ACT_27725318 |
| AGTR2 | 8.74 | IC50 | 1.8 | nM | CHEMBL_ACT_27725315 |
Target pathways
Aggregated over 2 target gene(s): MAS1, AGTR2.
Top Reactome pathways
7 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Peptide ligand-binding receptors | 2 | AGTR2, MAS1 |
| Signal Transduction | 1 | AGTR2 |
| Signaling by GPCR | 1 | AGTR2 |
| Class A/1 (Rhodopsin-like receptors) | 1 | AGTR2 |
| GPCR downstream signalling | 1 | AGTR2 |
| G alpha (i) signalling events | 1 | AGTR2 |
| GPCR ligand binding | 1 | AGTR2 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| angiotensin-mediated vasodilation involved in regulation of systemic arterial blood pressure | 2 |
| G protein-coupled receptor signaling pathway | 2 |
| signal transduction | 2 |
| angiotensin-activated signaling pathway | 2 |
| adenylate cyclase-activating G protein-coupled receptor signaling pathway | 1 |
| positive regulation of canonical NF-kappaB signal transduction | 1 |
| regulation of inflammatory response | 1 |
| phospholipase C-activating angiotensin-activated signaling pathway | 1 |
| blood vessel remodeling | 1 |
| regulation of systemic arterial blood pressure by circulatory renin-angiotensin | 1 |
| brain renin-angiotensin system | 1 |
| inflammatory response | 1 |
| cell surface receptor signaling pathway | 1 |
| G protein-coupled receptor signaling pathway coupled to cGMP nucleotide second messenger | 1 |
| brain development | 1 |
Indications & clinical
Indications
3 indications (0 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 |
|---|---|---|---|
| hypertensive disorder | 3 | MONDO:0005044 | EFO:0000537 |
| kidney disorder | 3 | MONDO:0005240 | EFO:0003086 |
| chronic kidney disease | 3 | MONDO:0005300 | MONDO:0024327 |
Clinical trials
Total trials: 1.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE4 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00863252 | PHASE4 | COMPLETED | Mycophenolate Mofetil for IgA Nephropathy |
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.
19 molecules share ≥1 primary target. Top 19 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| LOSARTAN | ChEMBL + PubChem | Phase 4 (approved) | AGTR2 |
| OLMESARTAN MEDOXOMIL | ChEMBL + PubChem | Phase 4 (approved) | AGTR2 |
| ANGIOTENSIN II | ChEMBL | Phase 4 (approved) | AGTR2 |
| AZILSARTAN MEDOXOMIL | ChEMBL | Phase 4 (approved) | AGTR2 |
| BENAZEPRIL | ChEMBL | Phase 4 (approved) | AGTR2 |
| CANDESARTAN CILEXETIL | ChEMBL | Phase 4 (approved) | AGTR2 |
| DICLOFENAC | ChEMBL | Phase 4 (approved) | AGTR2 |
| IRBESARTAN | ChEMBL | Phase 4 (approved) | AGTR2 |
| MICONAZOLE | ChEMBL | Phase 4 (approved) | AGTR2 |
| SARALASIN | ChEMBL | Phase 4 (approved) | AGTR2 |
| TELMISARTAN | ChEMBL | Phase 4 (approved) | AGTR2 |
| OLMESARTAN | ChEMBL + PubChem | Phase 3 (approved) | AGTR2 |
| CANDESARTAN | ChEMBL | Phase 3 | AGTR2 |
| FORASARTAN | ChEMBL | Phase 2 | AGTR2 |
| OLODANRIGAN | ChEMBL | Phase 2 | AGTR2 |
| PRATOSARTAN | ChEMBL | Phase 2 | AGTR2 |
| TASOSARTAN | ChEMBL | Phase 2 | AGTR2 |
| Amiloride | PubChem | Approved | AGTR2 |
| Anagrelide | PubChem | Approved | AGTR2 |