Compound Detail

CHEMBL1200791

OXYMETAZOLINE HYDROCHLORIDE

💊 Approved Drug

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💊 Approved Drug

Cc1cc(C(C)(C)C)c(O)c(C)c1CC1=NCCN1.Cl

ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID	CHEMBL1200791
Name	OXYMETAZOLINE HYDROCHLORIDE
Phase	Approved
Structure Type	MOL
InChI Key	BEEDODBODQVSIM-UHFFFAOYSA-N
Therapeutic	✓ Yes
Parent Compound	CHEMBL762
Active Moiety	CHEMBL762

Known Names

Afrazine Agn-199201 NSC-757254 Ocuclear Oximetazoline hydrochloride Oxymetazoline hcl Oxymetazoline hydrochloride Oxymetazoline hydrochloride component of kovanaze Rhofade SCH 9384 SCH-9384 Upneeq +1 more

Targets

Activities

Assay Types

PK Parameters

Publications

Known Names

Indications

Mechanisms

Molecular Properties

260.4

MW (Da)

2.85

ALogP

HBA

HBD

44.6

PSA (Å²)

0.86

QED

Ro5 Violations

Rot. Bonds

Drug Information

Molecule Type	Small molecule
First Approval	1986
Availability	OTC
Chirality	Achiral

Routes of Administration

Topical

USAN Stem	-azoline
USAN Year	1963

Extended Properties

Molecular Formula	C16H25ClN2O
MW	296.84
Aromatic Rings	1
Heavy Atoms	19
NP-Likeness	0.26

Mechanism of Action

Mechanism	Action Type	Target	Direct	Efficacy
Adrenergic receptor alpha agonist	AGONIST	Adrenergic receptor alpha	✓	✓

Indications

Blepharoptosis Common Cold Nasal Obstruction Rhinitis, Allergic, Seasonal Rhinitis, Allergic, Seasonal Rosacea Sinusitis Erythema Conjunctivitis, Allergic Presbyopia

Activity Summary

IC50 4 meas. best 5.0

EC50 2 meas. best 8.48

Target Activity Profile

Target	Type	Best pChEMBL	Mean pChEMBL	Best (nM)	# Data
Alpha-2A adrenergic receptor CHEMBL1867	EC50	8.48	8.48	3.3	1
5-hydroxytryptamine receptor 1A CHEMBL214	EC50	7.16	7.16	70.0	1
Plasmodium falciparum CHEMBL364	IC50	5.0	4.95	10000.0	4

Activity Data Samples

Top measurements by pChEMBL value

Target	Type	Rel.	Value	Units	pChEMBL	Assay	PubMed
Alpha-2A adrenergic receptor	EC50	=	3.29	nM	8.48	GPCR PRESTO-Tango dose-response in agonist mode with target: ADRA2A	-
5-hydroxytryptamine receptor 1A	EC50	=	70.0	nM	7.16	PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serot...	-
Plasmodium falciparum	IC50	=	10000.0	nM	5.0	Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR g...	19734910
Plasmodium falciparum	IC50	=	10000.0	nM	5.0	Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR g...	19734910
Plasmodium falciparum	IC50	=	12589.25	nM	4.9	Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR g...	19734910
Plasmodium falciparum	IC50	=	12589.25	nM	4.9	Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR gr...	19734910

Literature References

PubMed	DOI	Target Context	# Activities
-	10.6019/CHEMBL4689842	HEK-293T	10
-	10.6019/CHEMBL4689842	Fibroblast	9
-	10.6019/CHEMBL4689842	U2OS	8
-	10.6019/CHEMBL5209801	N-formyl peptide receptor 2	5
-	10.6019/CHEMBL5209801	Sphingosine 1-phosphate receptor 1	5
-	10.6019/CHEMBL5209801	C5a anaphylatoxin chemotactic receptor 1	5
-	10.6019/CHEMBL5209801	CX3C chemokine receptor 1	5
-	10.6019/CHEMBL5209801	Type-1 angiotensin II receptor	5
-	10.6019/CHEMBL5209801	Glucose-dependent insulinotropic receptor	5
-	10.6019/CHEMBL5209801	Free fatty acid receptor 4	5
-	10.6019/CHEMBL5209801	Adhesion G-protein coupled receptor F1	5
-	10.6019/CHEMBL5209801	Alpha-2A adrenergic receptor	5
-	10.6019/CHEMBL5209801	Beta-2 adrenergic receptor	5
-	10.6019/CHEMBL5209801	Glucagon-like peptide 1 receptor	5
-	10.6019/CHEMBL5209801	Apelin receptor	5
19734910	10.1038/nchembio.215	Plasmodium falciparum	4
-	10.6019/CHEMBL4495565	SARS-CoV-2	2
-	10.6019/CHEMBL5209801	G-protein coupled receptor 35	2
-	10.6019/CHEMBL5665443	Uracil-DNA glycosylase	1
-	10.6019/CHEMBL5060014	Tyrosine-protein kinase ABL1	1

Data from ChEMBL 36 via Core Engine