Rilmenidine

Summary

Rilmenidine (CHEMBL289480) is an approved small molecule (ATC C02AC06); indicated across 1 condition including hypertensive disorder.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C02AC06
• Indications: 1 condition
• Clinical trials: 1
• Chemistry: 180.25 Da · C10H16N2O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL289480
Name	Rilmenidine
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	68712
ATC	C02AC06
Molecular formula	C10H16N2O
Molecular weight	180.25
InChIKey	CQXADFVORZEARL-UHFFFAOYSA-N

SMILES: C1CC1C(C2CC2)NC3=NCCO3

IUPAC name: N-(dicyclopropylmethyl)-4,5-dihydro-1,3-oxazol-2-amine

Also known as: Hyperium, Rilmenidina, Rilmenidine, rilmenidine, SID11111726, SID11111727, SID11113329, SID50103956, SID85231209, SID90340708, SID104171229, SID510678

Parent form; salt/anhydrous children: CHEMBL1256674

Patent coverage: 747 distinct patent families (2,657 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

Broader ChEMBL bioactivity targets: 17 (assay-derived). Sample: Geminin, Alpha-2A adrenergic receptor, Alpha-2C adrenergic receptor, Alpha-2B adrenergic receptor, Thyrotropin receptor, Adrenergic receptor alpha-2, 5-hydroxytryptamine receptor 1A, Alpha-1A adrenergic receptor, Kappa-type opioid receptor, Cytochrome P450 2D6.

Bioactivity

ChEMBL activities: 36 potent at pChembl ≥ 5 of 49 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
Q4G017	7.95	Ki	11.22	nM	CHEMBL_ACT_10964086
Q4G017	7.95	Ki	11.22	nM	CHEMBL_ACT_12460994
ADRA2C	7.9	Ki	12.59	nM	CHEMBL_ACT_10964114
Q4G017	7.9	Ki	12.59	nM	CHEMBL_ACT_16610439
ADRA2A	7.44	Ki	36.31	nM	CHEMBL_ACT_10964100
ADRA2B	7.37	Ki	42.66	nM	CHEMBL_ACT_10964107
NISCH	7.23	Ki	59.16	nM	CHEMBL_ACT_2564068
NISCH	7.23	Ki	59.2	nM	CHEMBL_ACT_2564069
ADRA2B	7.15	Ki	70.79	nM	CHEMBL_ACT_1267917
NISCH	7.13	Ki	74.13	nM	CHEMBL_ACT_657322
Q4G017	7.08	Ki	83.1	nM	CHEMBL_ACT_15197880
ADRA2A	6.75	Ki	180	nM	CHEMBL_ACT_15197907
ADRA2A	6.75	EC50	177.8	nM	CHEMBL_ACT_16610371
ADRA2A	6.74	Ki	182	nM	CHEMBL_ACT_1267916
ADRA2C	6.72	EC50	190.6	nM	CHEMBL_ACT_1267924
ADRA2A	6.56	EC50	275.4	nM	CHEMBL_ACT_1267922
ADRA2C	6.54	Ki	288.4	nM	CHEMBL_ACT_1267918
ADRA2A	6.52	Ki	300	nM	CHEMBL_ACT_16610354
CYP2D6	6.4	Potency	398.1	nM	CHEMBL_ACT_4965783
CYP2D6	6.4	AC50	398.1	nM	CHEMBL_ACT_5988118
ADRA2B	6.14	EC50	724.4	nM	CHEMBL_ACT_1267923
ADRA2A	5.88	AC50	1308	nM	CHEMBL_ACT_25221640
OPRK1	5.76	AC50	1721	nM	CHEMBL_ACT_25129950
ADRA2A	5.58	AC50	2600	nM	CHEMBL_ACT_25220435
ADRA1A	5.47	AC50	3400	nM	CHEMBL_ACT_25230262
ADRA2A	5.46	AC50	3490	nM	CHEMBL_ACT_25156087
ADRA1A	5.36	AC50	4390	nM	CHEMBL_ACT_25138244
ADRA1A	5.22	Ki	6026	nM	CHEMBL_ACT_1267921
ADRA2C	5.17	AC50	6800	nM	CHEMBL_ACT_25148454
ADRA2B	5.12	AC50	7500	nM	CHEMBL_ACT_25144260

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

1 indication (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
hypertensive disorder	4	MONDO:0005044	EFO:0000537

Clinical trials

Total trials: 1.

Phase distribution

Phase	Trials
PHASE4	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00892892	PHASE4	WITHDRAWN	Sympathetic Nerve Activity in Renal Failure

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

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).