Glafenine

Summary

Glafenine (CHEMBL146095) is an approved small-molecule non-narcotic analgesic (ATC N02BG03); indicated across 2 conditions.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N02BG03
• Indications: 2 conditions
• Chemistry: 372.8 Da · C19H17ClN2O4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL146095
Name	Glafenine
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	3474
ChEBI	CHEBI:31653
ATC	N02BG03
Molecular formula	C19H17ClN2O4
Molecular weight	372.8
InChIKey	GWOFUCIGLDBNKM-UHFFFAOYSA-N

SMILES: C1=CC=C(C(=C1)C(=O)OCC(CO)O)NC2=C3C=CC(=CC3=NC=C2)Cl

IUPAC name: 2,3-dihydroxypropyl 2-[(7-chloroquinolin-4-yl)amino]benzoate

ChEBI definition: A carboxylic ester that is 2,3-dihydroxypropyl anthranilate in which the amino group is substituted by a 7-chloroquinolin-4-yl group. A non-steroidal anti-inflammatory drug, glafenine and its hydrochloride salt were used for the relief of all types of pain, but high incidence of anaphylactic reactions resulted in their withdrawal from the market.

Pharmacological roles (ChEBI): non-narcotic analgesic, non-steroidal anti-inflammatory drug, inhibitor.

Also known as: Glafenin, Glafenina, Glafenine, NSC-757808, R 1707, R-1707, SID26748455, glafenine, GLAFENINE

Parent form; salt/anhydrous children: CHEMBL1572751

Patent coverage: 716 distinct patent families (2,714 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 2,692 (99%) 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

Broader ChEMBL bioactivity targets: 27 (assay-derived). Sample: Lysine-specific demethylase 4E, 15-hydroxyprostaglandin dehydrogenase [NAD(+)], Equilibrative nucleoside transporter 1, Thromboxane A2 receptor, Bile salt export pump, Muscarinic acetylcholine receptor M2, Muscarinic acetylcholine receptor M1, Motilin receptor, Prostaglandin G/H synthase 1, Sodium-dependent noradrenaline transporter.

Bioactivity

ChEMBL activities: 14 potent at pChembl ≥ 5 of 31 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P62813	7.34	AC50	46	nM	CHEMBL_ACT_25130226
PDE4D	6.77	AC50	170	nM	CHEMBL_ACT_25184939
ADORA3	5.86	AC50	1395	nM	CHEMBL_ACT_25198572
KCNH2	5.85	AC50	1400	nM	CHEMBL_ACT_25117294
CHRM2	5.37	AC50	4299	nM	CHEMBL_ACT_25195550
PTGS1	5.33	AC50	4628	nM	CHEMBL_ACT_25205971
KDR	5.16	AC50	6963	nM	CHEMBL_ACT_25168093
ADORA3	5.14	AC50	7200	nM	CHEMBL_ACT_25133832
CHRM1	5.12	AC50	7507	nM	CHEMBL_ACT_25210052
CYP3A4	5.1	Potency	7943	nM	CHEMBL_ACT_4949597
CYP3A4	5.1	Potency	7943	nM	CHEMBL_ACT_5018518
SLC29A1	5.09	AC50	8100	nM	CHEMBL_ACT_25141184
PDE4A	5.08	AC50	8300	nM	CHEMBL_ACT_25206901
TBXA2R	5.01	AC50	9800	nM	CHEMBL_ACT_25197496

Target pathways

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

Indications & clinical

Indications

2 indications (2 at ChEMBL trial phase 4).

The 2 indication records carry no mapped disease name (EFO/MeSH-only); none shown.

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

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