Vercirnon

Summary

Vercirnon (CHEMBL2178578) is a phase-3 clinical-stage small molecule targeting CCR9; indicated across 3 conditions including ulcerative colitis and crohn disease.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (CCR9)
• Indications: 3 conditions
• Clinical trials: 4
• Chemistry: 444.9 Da · C22H21ClN2O4S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2178578
Name	Vercirnon
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	10343454
Molecular formula	C22H21ClN2O4S
Molecular weight	444.9
InChIKey	JRWROCIMSDXGOZ-UHFFFAOYSA-N

SMILES: CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)NC2=C(C=C(C=C2)Cl)C(=O)C3=CC=[N+](C=C3)[O-]

IUPAC name: 4-tert-butyl-N-[4-chloro-2-(1-oxidopyridin-1-ium-4-carbonyl)phenyl]benzenesulfonamide

Also known as: CCX282, GSK-1605786, GSK1605786, Vercirnon, Verecimon, VERCIRNON, VERCIRNON SODIUM

Parent form; salt/anhydrous children: CHEMBL3039505

Patent coverage: 119 distinct patent families (349 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
CCR9	CCR9	Antagonist	8.22	0%	P51686

Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: C-C chemokine receptor type 2, C-C chemokine receptor type 9.

Bioactivity

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

Target	pChembl	Type	Value	Unit	Activity ID
CCR2	10	Kd	0.1	nM	CHEMBL_ACT_25100068
CCR9	8.96	Ki	1.1	nM	CHEMBL_ACT_16563153
CCR9	8.66	Ki	2.19	nM	CHEMBL_ACT_29285270
CCR9	8.62	Ki	2.4	nM	CHEMBL_ACT_29285269
CCR9	8.59	IC50	2.6	nM	CHEMBL_ACT_18924224
CCR9	8.55	IC50	2.8	nM	CHEMBL_ACT_12149717
CCR9	8.55	IC50	2.8	nM	CHEMBL_ACT_18924223
CCR9	8.43	Ki	3.7	nM	CHEMBL_ACT_16562228
CCR9	8.3	IC50	5	nM	CHEMBL_ACT_16616108
CCR9	8.22	IC50	6	nM	CHEMBL_ACT_12149718
CCR9	8	IC50	10	nM	CHEMBL_ACT_15679041
CCR9	8	Ki	10	nM	CHEMBL_ACT_16562214
CCR9	7.96	IC50	11	nM	CHEMBL_ACT_15679070
CCR9	6.27	IC50	539	nM	CHEMBL_ACT_15679072

Target pathways

Aggregated over 1 target gene(s): CCR9.

Top Reactome pathways

8 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	1	CCR9
Signaling by GPCR	1	CCR9
Class A/1 (Rhodopsin-like receptors)	1	CCR9
Peptide ligand-binding receptors	1	CCR9
Chemokine receptors bind chemokines	1	CCR9
GPCR downstream signalling	1	CCR9
G alpha (i) signalling events	1	CCR9
GPCR ligand binding	1	CCR9

Dominant GO biological processes

GO term	Targets
CD8-positive, gamma-delta intraepithelial T cell differentiation	1
chemotaxis	1
immune response	1
cellular defense response	1
G protein-coupled receptor signaling pathway	1
positive regulation of cytosolic calcium ion concentration	1
calcium-mediated signaling	1
cell chemotaxis	1
signal transduction	1
chemokine-mediated signaling pathway	1

Indications & clinical

Indications

3 indications (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
ulcerative colitis	2	MONDO:0005101	EFO:0000729
Crohn disease	2	MONDO:0005011	EFO:0000384
celiac disease	2	MONDO:0005130	EFO:0001060

Clinical trials

Total trials: 4.

Phase distribution

Phase	Trials
PHASE1	3
PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01658605	PHASE2	WITHDRAWN	A Study to Investigate the Efficacy and Safety of GSK1605786 for Treatment of Patients With Active Ulcerative Colitis
NCT01489943	PHASE1	COMPLETED	A Study to Investigate the Effect of GSK1605786 on Hepatic Cytochrome P450, and BCRP and OATP1B1 Transport in Healthy Adult Subjects
NCT01611805	PHASE1	COMPLETED	Japanese Phase I of GSK1605786
NCT01827631	PHASE1	COMPLETED	Single and Repeat Dose Pharmacokinetic Study of GSK1605786 in Healthy Chinese 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

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