Procaine

Summary

Procaine (CHEMBL569) is an approved small-molecule local anaesthetic (ATC N01BA52) targeting RYR1 and RYR2; indicated across 2 conditions including hemorrhoid and osteomyelitis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N01BA52 (+3 more)
• Targets: 2 (RYR1, RYR2)
• Indications: 2 conditions
• Clinical trials: 2
• Chemistry: 236.31 Da · C13H20N2O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL569
Name	Procaine
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	4914
ChEBI	CHEBI:8430
ATC	N01BA52, N01BA02, S01HA05, C05AD05
Molecular formula	C13H20N2O2
Molecular weight	236.31
InChIKey	MFDFERRIHVXMIY-UHFFFAOYSA-N

SMILES: CCN(CC)CCOC(=O)C1=CC=C(C=C1)N

IUPAC name: 2-(diethylamino)ethyl 4-aminobenzoate

ChEBI definition: A benzoate ester, formally the result of esterification of 4-aminobenzoic acid with 2-diethylaminoethanol but formed experimentally by reaction of ethyl 4-aminobenzoate with 2-diethylaminoethanol.

Pharmacological roles (ChEBI): local anaesthetic, central nervous system depressant, peripheral nervous system drug, drug allergen.

Also known as: NSC-169497, Procaina, Procaine, Solution of novocain, procaine, SID11111696, SID11111697, SID90341175, Vitamin H3, PROCAINE

Parent form; salt/anhydrous children: CHEMBL1200841

Patent coverage: 47,886 distinct patent families (170,694 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
RYR1	RyR1			1%	P21817
RYR2	RyR2			0.3%	Q92736

Broader ChEMBL bioactivity targets: 6 (assay-derived). Sample: 5-hydroxytryptamine receptor 3A, Amine oxidase [flavin-containing] A, Thyrotropin receptor, Histamine H3 receptor, Muscarinic acetylcholine receptor M1, Cytochrome P450 2D6.

Bioactivity

ChEMBL activities: 3 potent at pChembl ≥ 5 of 11 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
HRH3	5.06	AC50	8700	nM	CHEMBL_ACT_25201141
CYP2D6	5	Potency	10000	nM	CHEMBL_ACT_4998369
CYP2D6	5	AC50	10000	nM	CHEMBL_ACT_6046039

Target pathways

Aggregated over 2 target gene(s): RYR1, RYR2.

Top Reactome pathways

6 total, by targets touching each:

Pathway	Targets	Genes
Stimuli-sensing channels	2	RYR1, RYR2
Transport of small molecules	2	RYR1, RYR2
Muscle contraction	2	RYR1, RYR2
Cardiac conduction	2	RYR1, RYR2
Ion homeostasis	2	RYR1, RYR2
Ion channel transport	2	RYR1, RYR2

Dominant GO biological processes

GO term	Targets
response to hypoxia	2
calcium ion transport	2
striated muscle contraction	2
release of sequestered calcium ion into cytosol by sarcoplasmic reticulum	2
response to caffeine	2
release of sequestered calcium ion into cytosol	2
regulation of cytosolic calcium ion concentration	2
cellular response to caffeine	2
monoatomic ion transport	2
intracellular calcium ion homeostasis	2
calcium-mediated signaling	2
monoatomic ion transmembrane transport	2
transmembrane transport	2
calcium ion transmembrane transport	2
outflow tract morphogenesis	1

Indications & clinical

Indications

2 indications (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
hemorrhoid	4	MONDO:0004872	EFO:0009552
osteomyelitis	0	MONDO:0005246	EFO:0003102

Clinical trials

Total trials: 2.

Phase distribution

Phase	Trials
PHASE2	1
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02735317	PHASE2	UNKNOWN	Efficacy and Safety of FORRAD® for the Management of Radiation-induced Mucositis in Patients With Nasopharyngeal Carcinoma Receiving IMRT
NCT02726620	Not specified	COMPLETED	Decision Support for Intraoperative Low Blood Pressure

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

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.

4 molecules share ≥1 primary target. Top 4 by shared-target count:

Molecule	Source	Status	Shared targets
ALADORIAN	ChEMBL	Phase 2	RYR2
Caffeine	PubChem	Approved	RYR2
Dantrolene	PubChem	Approved	RYR2
Oxolinic Acid	PubChem	Approved	RYR2