Mozavaptan

Summary

Mozavaptan (CHEMBL420762) is an approved small molecule targeting AVPR1A, AVPR1B, and AVPR2.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• Targets: 3 (AVPR1A, AVPR1B, AVPR2)
• Chemistry: 427.5 Da · C27H29N3O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL420762
Name	Mozavaptan
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	119369
Molecular formula	C27H29N3O2
Molecular weight	427.5
InChIKey	WRNXUQJJCIZICJ-UHFFFAOYSA-N

SMILES: CC1=CC=CC=C1C(=O)NC2=CC=C(C=C2)C(=O)N3CCCC(C4=CC=CC=C43)N(C)C

IUPAC name: N-[4-[5-(dimethylamino)-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl]phenyl]-2-methylbenzamide

Also known as: Mozavaptan, Mozavaptane, SID170466304, MOZAVAPTAN, mozavaptan, Mozavaptan hydrochlorideÊ, Mozavaptan hydrochlorideÂ

Parent form; salt/anhydrous children: CHEMBL5087555

Patent coverage: 108 distinct patent families (244 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 151 (62%) 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
AVPR1A	V1A receptor	Antagonist	7.1	4.6%	P37288
AVPR1B	V1B receptor	Antagonist	4.8	0.4%	P47901
AVPR2	V2 receptor	Inverse agonist	8.1	0%	P30518

Broader ChEMBL bioactivity targets: 13 (assay-derived). Sample: Vasopressin V2 receptor, Vasopressin V1a receptor, Oxytocin receptor, Vasopressin V1 receptor, Vasopressin V1 receptor, 5-hydroxytryptamine receptor 1A, Muscarinic acetylcholine receptor M1, Sodium-dependent serotonin transporter, Alpha-1A adrenergic receptor, Mu-type opioid receptor.

Bioactivity

ChEMBL activities: 13 potent at pChembl ≥ 5 of 16 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
AVPR2	8.03	Ki	9.42	nM	CHEMBL_ACT_32615
AVPR2	8.01	Ki	9.7	nM	CHEMBL_ACT_12108252
Q00788	7.92	IC50	12	nM	CHEMBL_ACT_1252848
AVPR1A	6.71	Ki	195	nM	CHEMBL_ACT_12108249
Q00788	6.52	IC50	300	nM	CHEMBL_ACT_1276466
AVPR2	6.3	IC50	500	nM	CHEMBL_ACT_1276468
OXTR	6.18	Ki	660	nM	CHEMBL_ACT_12108246
SLC6A4	5.9	AC50	1261	nM	CHEMBL_ACT_25151763
P30560	5.85	IC50	1400	nM	CHEMBL_ACT_1252847
AVPR1A	5.7	IC50	2000	nM	CHEMBL_ACT_1276467
OPRM1	5.61	AC50	2484	nM	CHEMBL_ACT_25158611
P30560	5.3	IC50	5000	nM	CHEMBL_ACT_1276465
HTR1A	5.24	AC50	5797	nM	CHEMBL_ACT_25165460

Target pathways

Aggregated over 3 target gene(s): AVPR1A, AVPR1B, AVPR2.

Top Reactome pathways

8 total, by targets touching each:

Pathway	Targets	Genes
Vasopressin-like receptors	3	AVPR1A, AVPR1B, AVPR2
G alpha (q) signalling events	2	AVPR1A, AVPR1B
Defective AVP does not bind AVPR1A,B and causes neurohypophyseal diabetes insipidus (NDI)	2	AVPR1A, AVPR1B
G alpha (s) signalling events	1	AVPR2
Vasopressin regulates renal water homeostasis via Aquaporins	1	AVPR2
Cargo recognition for clathrin-mediated endocytosis	1	AVPR2
Clathrin-mediated endocytosis	1	AVPR2
Defective AVP does not bind AVPR2 and causes neurohypophyseal diabetes insipidus (NDI)	1	AVPR2

Dominant GO biological processes

GO term	Targets
regulation of systemic arterial blood pressure by vasopressin	3
G protein-coupled receptor signaling pathway	3
cellular response to hormone stimulus	3
positive regulation of vasoconstriction	3
signal transduction	3
positive regulation of systemic arterial blood pressure	2
positive regulation of cytosolic calcium ion concentration	2
positive regulation of cell population proliferation	2
telencephalon development	2
transport across blood-brain barrier	2
regulation of blood pressure	2
positive regulation of blood pressure	2
maternal aggressive behavior	1
generation of precursor metabolites and energy	1
negative regulation of female receptivity	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.

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

Molecule	Source	Status	Shared targets
DESMOPRESSIN	ChEMBL + PubChem	Phase 4 (approved)	AVPR1A, AVPR1B, AVPR2
OXYTOCIN	ChEMBL + PubChem	Phase 4 (approved)	AVPR1A, AVPR1B, AVPR2
ATOSIBAN	ChEMBL	Phase 4 (approved)	AVPR1A, AVPR1B, AVPR2
CARBETOCIN	ChEMBL	Phase 4 (approved)	AVPR1A, AVPR1B, AVPR2
VASOPRESSIN	ChEMBL	Phase 4 (approved)	AVPR1A, AVPR1B, AVPR2
NELIVAPTAN	ChEMBL	Phase 2	AVPR1A, AVPR1B, AVPR2
ORNIPRESSIN	ChEMBL	Phase 2	AVPR1A, AVPR1B, AVPR2
PECAVAPTAN	ChEMBL	Phase 2	AVPR1A, AVPR1B, AVPR2
SELEPRESSIN	ChEMBL	Phase 2	AVPR1A, AVPR1B, AVPR2
PIMOZIDE	ChEMBL + PubChem	Phase 4 (approved)	AVPR1A, AVPR2
RIFAMPIN	ChEMBL + PubChem	Phase 4 (approved)	AVPR1A, AVPR2
TEGASEROD	ChEMBL + PubChem	Phase 4 (approved)	AVPR1A, AVPR2
BALSALAZIDE	ChEMBL	Phase 4 (approved)	AVPR1A, AVPR2
BOSUTINIB	ChEMBL	Phase 4 (approved)	AVPR1A, AVPR2
CHLORHEXIDINE	ChEMBL	Phase 4 (approved)	AVPR1A, AVPR2
CONIVAPTAN	ChEMBL	Phase 4 (approved)	AVPR1A, AVPR2
FLUSPIRILENE	ChEMBL	Phase 4 (approved)	AVPR1A, AVPR2
NITAZOXANIDE	ChEMBL	Phase 4 (approved)	AVPR1A, AVPR2
PYRVINIUM	ChEMBL	Phase 4 (approved)	AVPR1A, AVPR2
RIFAXIMIN	ChEMBL	Phase 4 (approved)	AVPR1A, AVPR2
TOLVAPTAN	ChEMBL	Phase 4 (approved)	AVPR1A, AVPR2
BALOVAPTAN	ChEMBL	Phase 3	AVPR1A, AVPR2
LIXIVAPTAN	ChEMBL	Phase 3	AVPR1A, AVPR2
OTILONIUM BROMIDE	ChEMBL	Phase 3	AVPR1A, AVPR2
BENZETHONIUM	ChEMBL	Phase 2	AVPR1A, AVPR2
DOMIPHEN	ChEMBL	Phase 2	AVPR1A, AVPR2
RELCOVAPTAN	ChEMBL	Phase 2	AVPR1A, AVPR2
Abiraterone	PubChem	Approved	AVPR1A, AVPR2
acetylcysteine	PubChem	Approved	AVPR1A, AVPR2
Aclidinium Bromide	PubChem	Approved	AVPR1A, AVPR2
Acyclovir	PubChem	Approved	AVPR1A, AVPR2
Afatinib	PubChem	Approved	AVPR1A, AVPR2
Allopurinol	PubChem	Approved	AVPR1A, AVPR2
Almotriptan	PubChem	Approved	AVPR1A, AVPR2
Alogliptin	PubChem	Approved	AVPR1A, AVPR2
aminolevulinic acid	PubChem	Approved	AVPR1A, AVPR2
Anagrelide	PubChem	Approved	AVPR1A, AVPR2
Apixaban	PubChem	Approved	AVPR1A, AVPR2
Aprepitant	PubChem	Approved	AVPR1A, AVPR2
Belzutifan	PubChem	Approved	AVPR1A, AVPR2
Bosentan	PubChem	Approved	AVPR1A, AVPR2
Clofarabine	PubChem	Approved	AVPR1A, AVPR2
Clozapine	PubChem	Approved	AVPR1A, AVPR2
Crizotinib	PubChem	Approved	AVPR1A, AVPR2
Dacarbazine	PubChem	Approved	AVPR1A, AVPR2
Desloratadine	PubChem	Approved	AVPR1A, AVPR2
Desoxycorticosterone Pivalate	PubChem	Approved	AVPR1A, AVPR2
Didanosine	PubChem	Approved	AVPR1A, AVPR2
Dihydroergotamine	PubChem	Approved	AVPR1A, AVPR2
Erythromycin	PubChem	Approved	AVPR1A, AVPR2
Ethambutol	PubChem	Approved	AVPR1A, AVPR2
Fidaxomicin	PubChem	Approved	AVPR1A, AVPR2
Fulvestrant	PubChem	Approved	AVPR1A, AVPR2
Ganciclovir	PubChem	Approved	AVPR1A, AVPR2
Gefitinib	PubChem	Approved	AVPR1A, AVPR2
Glycopyrrolate	PubChem	Approved	AVPR1A, AVPR2
Leucovorin	PubChem	Approved	AVPR1A, AVPR2
Linagliptin	PubChem	Approved	AVPR1A, AVPR2
Methotrexate	PubChem	Approved	AVPR1A, AVPR2
Olanzapine	PubChem	Approved	AVPR1A, AVPR2