Renzapride

Summary

Renzapride (CHEMBL296522) is a phase-3 clinical-stage small molecule targeting HTR4; indicated across 1 condition including irritable bowel syndrome.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (HTR4)
• Indications: 1 condition
• Clinical trials: 2
• Chemistry: 323.82 Da · C16H22ClN3O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL296522
Name	Renzapride
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	3035241
Molecular formula	C16H22ClN3O2
Molecular weight	323.82
InChIKey	GZSKEXSLDPEFPT-UHFFFAOYSA-N

SMILES: COC1=CC(=C(C=C1C(=O)NC2CCN3CCCC2C3)Cl)N

IUPAC name: 4-amino-N-(1-azabicyclo[3.3.1]nonan-4-yl)-5-chloro-2-methoxybenzamide

Also known as: ATL-1251, BRL 24924A, Brl-24924, BRL-24924A, Renzaprida, Renzapride, RENZAPRIDE

Patent coverage: 23 distinct patent families (59 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
HTR4	5-HT4 receptor	Full agonist	6.8	0%	Q13639

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Serotonin 3 (5-HT3) receptor, 5-hydroxytryptamine receptor 3A, 5-hydroxytryptamine receptor 4, 5-hydroxytryptamine receptor 4.

Bioactivity

ChEMBL activities: 7 potent at pChembl ≥ 5 of 7 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P35563	8.3	Ki	5.01	nM	CHEMBL_ACT_513469
P35563	8.28	Ki	5.3	nM	CHEMBL_ACT_1200298
P35563	8.25	Ki	5.6	nM	CHEMBL_ACT_283588
O70528	7.39	Ki	40.4	nM	CHEMBL_ACT_1200299
Q62758	7.36	ED50	44	nM	CHEMBL_ACT_1279228
Q62758	7.2	EC50	63.1	nM	CHEMBL_ACT_513467
Q62758	7.01	EC50	98	nM	CHEMBL_ACT_283587

Target pathways

Aggregated over 1 target gene(s): HTR4.

Top Reactome pathways

8 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	1	HTR4
Signaling by GPCR	1	HTR4
Class A/1 (Rhodopsin-like receptors)	1	HTR4
Amine ligand-binding receptors	1	HTR4
GPCR downstream signalling	1	HTR4
Serotonin receptors	1	HTR4
G alpha (s) signalling events	1	HTR4
GPCR ligand binding	1	HTR4

Dominant GO biological processes

GO term	Targets
G protein-coupled receptor signaling pathway	1
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	1
adenylate cyclase-activating G protein-coupled receptor signaling pathway	1
adenylate cyclase-activating serotonin receptor signaling pathway	1
adenylate cyclase-inhibiting serotonin receptor signaling pathway	1
chemical synaptic transmission	1
maintenance of gastrointestinal epithelium	1
regulation of appetite	1
mucus secretion	1
large intestinal transit	1
regulation of postsynapse assembly	1
system process	1
signal transduction	1
G protein-coupled serotonin receptor signaling pathway	1

Indications & clinical

Indications

1 indication (0 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
irritable bowel syndrome	3	MONDO:0005052	EFO:0000555

Clinical trials

Total trials: 2.

Phase distribution

Phase	Trials
PHASE3	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00268879	PHASE3	COMPLETED	Investigation of the Safety and Efficacy of Renzapride in Constipation Predominant Irritable Bowel Syndrome (IBS)
NCT00607971	PHASE3	TERMINATED	Long-Term Safety of Renzapride in Women With Constipation-Predominant Irritable Bowel Syndrome (IBS-C)

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.

16 molecules share ≥1 primary target. Top 16 by shared-target count:

Molecule	Source	Status	Shared targets
IMIPRAMINE	ChEMBL + PubChem	Phase 4 (approved)	HTR4
PRUCALOPRIDE	ChEMBL + PubChem	Phase 4 (approved)	HTR4
TEGASEROD	ChEMBL + PubChem	Phase 4 (approved)	HTR4
CISAPRIDE	ChEMBL	Phase 4 (approved)	HTR4
METOCLOPRAMIDE	ChEMBL	Phase 4 (approved)	HTR4
TROPISETRON	ChEMBL	Phase 4 (approved)	HTR4
SEROTONIN	ChEMBL	Phase 3	HTR4
FELCISETRAG	ChEMBL	Phase 2	HTR4
LITOXETINE	ChEMBL	Phase 2	HTR4
MEBUFOTENIN	ChEMBL	Phase 2	HTR4
PIBOSEROD	ChEMBL	Phase 2	HTR4
PRX-03140	ChEMBL	Phase 2	HTR4
VELUSETRAG	ChEMBL	Phase 2	HTR4
Cyproheptadine	PubChem	Approved	HTR4
Donepezil	PubChem	Approved	HTR4
Haloperidol	PubChem	Approved	HTR4