Saralasin

Summary

Saralasin (CHEMBL938) is an approved protein targeting AGTR2.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Protein
• Targets: 1 (AGTR2)
• Chemistry: 912 Da · C42H65N13O10

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL938
Name	Saralasin
Type	Protein
Max phase	4
FDA approved	no
PubChem CID	6324663
Molecular formula	C42H65N13O10
Molecular weight	912
InChIKey	PFGWGEPQIUAZME-NXSMLHPHSA-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)CNC

IUPAC name: (2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[2-(methylamino)acetyl]amino]pentanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]propanoic acid

Also known as: Sar-arg-val-tyr-val-his-pro-ala, Saralasin, Saralasina, Saralasine, Sar-Arg-Val-Tyr-Val-His-Pro-Ala, SARALASIN

Parent form; salt/anhydrous children: CHEMBL1200670

Patent coverage: 1,896 distinct patent families (7,408 SureChEMBL compound mentions), from 3 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
AGTR2	AT2 receptor	Antagonist	9	0.1%	P50052

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

Bioactivity

ChEMBL activities: 25 potent at pChembl ≥ 5 of 25 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
AGTR1	10.18	IC50	0.07	nM	CHEMBL_ACT_438911
AGTR2	9.82	Ki	0.15	nM	CHEMBL_ACT_2381366
AGTR1	9.77	Ki	0.17	nM	CHEMBL_ACT_13342045
AGTR1	9.66	Ki	0.22	nM	CHEMBL_ACT_15097701
P25095	9.63	Kd	0.23	nM	CHEMBL_ACT_1074916
AGTR1	9.62	Ki	0.24	nM	CHEMBL_ACT_26333254
AGTR1	9.48	Ki	0.33	nM	CHEMBL_ACT_2381365
AGTR1	9.46	IC50	0.35	nM	CHEMBL_ACT_13342117
AGTR2	9.42	Ki	0.38	nM	CHEMBL_ACT_15097697
AGTR2	9.42	Ki	0.38	nM	CHEMBL_ACT_16466557
AGTR1	9.4	IC50	0.4	nM	CHEMBL_ACT_16501837
AGTR1	9.4	IC50	0.4	nM	CHEMBL_ACT_16838405
AGTR1	9.39	IC50	0.41	nM	CHEMBL_ACT_26333199
AGTR2	9.35	IC50	0.45	nM	CHEMBL_ACT_2381344
AGTR2	9.28	IC50	0.53	nM	CHEMBL_ACT_5166011
AGTR1	9.24	IC50	0.57	nM	CHEMBL_ACT_5165965
AGTR1	9.22	IC50	0.6	nM	CHEMBL_ACT_13336213
AGTR1	9.17	IC50	0.67	nM	CHEMBL_ACT_2381343
AGTR1	9	IC50	1	nM	CHEMBL_ACT_2573319
AGTR2	8.88	IC50	1.32	nM	CHEMBL_ACT_71130
P25095	8.77	IC50	1.69	nM	CHEMBL_ACT_71129
P29089	8.62	IC50	2.4	nM	CHEMBL_ACT_337042
P25095	8.22	EC50	6	nM	CHEMBL_ACT_19462440
P25095	8.12	EC50	7.5	nM	CHEMBL_ACT_19462281
AGTR1	7.96	EC50	11	nM	CHEMBL_ACT_19462127

Target pathways

Aggregated over 1 target gene(s): AGTR2.

Top Reactome pathways

7 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	1	AGTR2
Signaling by GPCR	1	AGTR2
Class A/1 (Rhodopsin-like receptors)	1	AGTR2
Peptide ligand-binding 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
blood vessel remodeling	1
regulation of systemic arterial blood pressure by circulatory renin-angiotensin	1
angiotensin-mediated vasodilation involved in regulation of systemic arterial blood pressure	1
brain renin-angiotensin system	1
inflammatory response	1
cell surface receptor signaling pathway	1
G protein-coupled receptor signaling pathway	1
G protein-coupled receptor signaling pathway coupled to cGMP nucleotide second messenger	1
brain development	1
regulation of blood pressure	1
negative regulation of heart rate	1
negative regulation of cell growth	1
regulation of metanephros size	1
exploration behavior	1
nitric oxide-cGMP-mediated signaling	1

Indications & clinical

Indications

0 indications (0 at ChEMBL trial phase 4).

Clinical trials

Total trials: 0.

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
TELMISARTAN	ChEMBL	Phase 4 (approved)	AGTR2
OLMESARTAN	ChEMBL + PubChem	Phase 3 (approved)	AGTR2
ANGIOTENSIN	ChEMBL	Phase 3	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