Pranlukast

Summary

Pranlukast (CHEMBL21333) is an approved small molecule (ATC R03DC02) targeting CYSLTR1 and CYSLTR2; indicated across 3 conditions including obstructive lung disease and sinusitis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: R03DC02
• Targets: 2 (CYSLTR1, CYSLTR2)
• Indications: 3 conditions
• Clinical trials: 3
• Chemistry: 481.5 Da · C27H23N5O4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL21333
Name	Pranlukast
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	4887
ATC	R03DC02
Molecular formula	C27H23N5O4
Molecular weight	481.5
InChIKey	NBQKINXMPLXUET-UHFFFAOYSA-N

SMILES: C1=CC=C(C=C1)CCCCOC2=CC=C(C=C2)C(=O)NC3=CC=CC4=C3OC(=CC4=O)C5=NNN=N5

IUPAC name: N-[4-oxo-2-(2H-tetrazol-5-yl)chromen-8-yl]-4-(4-phenylbutoxy)benzamide

Also known as: Azlaire, CCN 00401, CCN-00401, ONO 1078, ONO-1078, Onon, Pranlukast, RS 411, RS-411, SB 205312, SB-205312, pranlukast

Parent form; salt/anhydrous children: CHEMBL3810125

Patent coverage: 3,465 distinct patent families (12,755 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 11,877 (93%) 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
CYSLTR1	CysLT1 receptor	Antagonist	10	0.2%	Q9Y271
CYSLTR2	CysLT2 receptor	Antagonist	5.44	0.1%	Q9NS75

Broader ChEMBL bioactivity targets: 23 (assay-derived). Sample: Uracil nucleotide/cysteinyl leukotriene receptor, ATP-binding cassette sub-family C member 4, Cysteinyl leukotriene receptor 1, Androgen receptor, Bile acid receptor, D(1A) dopamine receptor, ATP-binding cassette sub-family C member 2, Progesterone receptor, Cysteinyl leukotriene receptor, 5-hydroxytryptamine receptor 1A.

Bioactivity

ChEMBL activities: 25 potent at pChembl ≥ 5 of 34 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
Q2NNR5	10.36	IC50	0.04	nM	CHEMBL_ACT_18067141
CYSLTR2	10.36	IC50	0.04	nM	CHEMBL_ACT_289539
CYSLTR2	9.1	Ki	0.8	nM	CHEMBL_ACT_117952
CYSLTR1	9.1	IC50	0.8	nM	CHEMBL_ACT_3408501
Q2NNR5	9.1	Ki	0.8	nM	CHEMBL_ACT_418734
Q2NNR5	9.1	Ki	0.8	nM	CHEMBL_ACT_788888
Q2NNR5	9	IC50	1	nM	CHEMBL_ACT_157932
CYSLTR2	9	Kd	1	nM	CHEMBL_ACT_348087
CYSLTR1	8.37	IC50	4.3	nM	CHEMBL_ACT_15657847
CYSLTR1	8.37	IC50	4.3	nM	CHEMBL_ACT_24792886
CYSLTR1	8.36	IC50	4.4	nM	CHEMBL_ACT_18067149
ABCC4	5.57	IC50	2700	nM	CHEMBL_ACT_18130822
DRD1	5.54	AC50	2880	nM	CHEMBL_ACT_25234741
ABCB11	5.53	IC50	2970	nM	CHEMBL_ACT_18129052
CYSLTR2	5.44	IC50	3620	nM	CHEMBL_ACT_15657844
GPR17	5.39	Ki	4060	nM	CHEMBL_ACT_14654733
HTR1A	5.39	AC50	4100	nM	CHEMBL_ACT_25164901
DRD3	5.35	AC50	4450	nM	CHEMBL_ACT_25194402
OPRM1	5.33	AC50	4640	nM	CHEMBL_ACT_25158052
PGR	5.21	AC50	6230	nM	CHEMBL_ACT_25204168
P25779	5.16	IC50	7000	nM	CHEMBL_ACT_3307715
SLC6A2	5.15	AC50	7060	nM	CHEMBL_ACT_25145877
PDE4A	5.09	AC50	8210	nM	CHEMBL_ACT_25206964
SLC6A3	5.08	AC50	8240	nM	CHEMBL_ACT_25124836
DRD1	5	AC50	10060	nM	CHEMBL_ACT_25115087

Target pathways

Aggregated over 2 target gene(s): CYSLTR1, CYSLTR2.

Top Reactome pathways

5 total, by targets touching each:

Pathway	Targets	Genes
Leukotriene receptors	2	CYSLTR1, CYSLTR2
G alpha (q) signalling events	2	CYSLTR1, CYSLTR2
LTC4-CYSLTR mediated IL4 production	2	CYSLTR1, CYSLTR2
G alpha (s) signalling events	1	CYSLTR2
Potential therapeutics for SARS	1	CYSLTR1

Dominant GO biological processes

GO term	Targets
neuropeptide signaling pathway	2
signal transduction	2
G protein-coupled receptor signaling pathway	2
leukotriene signaling pathway	2
inflammatory response to antigenic stimulus	1
endothelium development	1
calcium ion transport	1
chemotaxis	1
defense response	1
cell surface receptor signaling pathway	1
positive regulation of cytosolic calcium ion concentration	1
respiratory gaseous exchange by respiratory system	1
establishment of localization in cell	1
reactive oxygen species biosynthetic process	1
immune response	1

Indications & clinical

Indications

3 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
obstructive lung disease	4	MONDO:0002267	HP:0006536
sinusitis	3	MONDO:0005961	EFO:0007486
seasonal allergic rhinitis	3	MONDO:0005324	EFO:0003956

Clinical trials

Total trials: 3.

Phase distribution

Phase	Trials
PHASE3	2
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00127647	PHASE3	COMPLETED	An Approved Drug to Study a New Indication for Allergic Rhinitis (0476-327)
NCT00410735	PHASE3	COMPLETED	Study of ONO-1078 in Patients With Chronic Sinusitis
NCT03826485	PHASE1	UNKNOWN	Safety, Pharmacokinetic Study of PRIC in Healthy Adult Subjects

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.

11 molecules share ≥1 primary target. Top 11 by shared-target count:

Molecule	Source	Status	Shared targets
MONTELUKAST	ChEMBL	Phase 4 (approved)	CYSLTR1, CYSLTR2
ZAFIRLUKAST	ChEMBL	Phase 4 (approved)	CYSLTR1, CYSLTR2
GEMILUKAST	ChEMBL	Phase 2	CYSLTR1, CYSLTR2
POBILUKAST	ChEMBL	Phase 2	CYSLTR1, CYSLTR2
RITOLUKAST	ChEMBL	Phase 2	CYSLTR1, CYSLTR2
TOMELUKAST	ChEMBL	Phase 2	CYSLTR1, CYSLTR2
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	CYSLTR1
DIETHYLSTILBESTROL	ChEMBL	Phase 4 (approved)	CYSLTR1
ABLUKAST	ChEMBL	Phase 2	CYSLTR1
VERLUKAST	ChEMBL	Phase 2	CYSLTR1
Belzutifan	PubChem	Approved	CYSLTR1