Cilomilast

Summary

Cilomilast (CHEMBL511115) is a phase-3 clinical-stage small molecule; indicated across 1 condition including chronic obstructive pulmonary disease.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 1 condition
• Clinical trials: 1
• Chemistry: 343.4 Da · C20H25NO4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL511115
Name	Cilomilast
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	151170
Molecular formula	C20H25NO4
Molecular weight	343.4
InChIKey	CFBUZOUXXHZCFB-UHFFFAOYSA-N

SMILES: COC1=C(C=C(C=C1)C2(CCC(CC2)C(=O)O)C#N)OC3CCCC3

IUPAC name: 4-cyano-4-(3-cyclopentyloxy-4-methoxyphenyl)cyclohexane-1-carboxylic acid

Also known as: Ariflo, Cilomilast, SB 207499, SB-207499, SB207499, cilomilast, CILOMILAST, SID144206070, rel-Cilomilast

Patent coverage: 530 distinct patent families (1,703 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

Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Phosphodiesterase 4, Phosphodiesterase 4, 3’,5’-cyclic-AMP phosphodiesterase 4A, 3’,5’-cyclic-AMP phosphodiesterase 4B, 3’,5’-cyclic-AMP phosphodiesterase 4D, 3’,5’-cyclic-AMP phosphodiesterase 4C, 3’,5’-cyclic-AMP phosphodiesterase 4B.

Bioactivity

ChEMBL activities: 64 potent at pChembl ≥ 5 of 66 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
PDE4A	8	IC50	10	nM	CHEMBL_ACT_862683
PDE4D	7.96	IC50	11	nM	CHEMBL_ACT_19334633
PDE4D	7.96	IC50	11	nM	CHEMBL_ACT_19400651
PDE4D	7.96	IC50	11	nM	CHEMBL_ACT_3117850
PDE4D	7.89	IC50	13	nM	CHEMBL_ACT_22788688
PDE4B	7.6	IC50	25	nM	CHEMBL_ACT_19400666
PDE4B	7.6	IC50	25	nM	CHEMBL_ACT_3117845
PDE4D	7.57	IC50	27	nM	CHEMBL_ACT_6225535
PDE4A	7.52	IC50	30	nM	CHEMBL_ACT_982951
PDE4B	7.43	IC50	37	nM	CHEMBL_ACT_6225499
PDE4A	7.42	Ki	38	nM	CHEMBL_ACT_1160158
PDE4A	7.42	IC50	38	nM	CHEMBL_ACT_149776
PDE4A	7.42	IC50	38	nM	CHEMBL_ACT_348579
PDE4A	7.42	Ki	38	nM	CHEMBL_ACT_609047
PDE4D	7.41	IC50	39	nM	CHEMBL_ACT_1802651
PDE4A	7.4	IC50	40	nM	CHEMBL_ACT_311422
P14270	7.31	IC50	49	nM	CHEMBL_ACT_982959
PDE4A	7.21	IC50	62	nM	CHEMBL_ACT_13366531
PDE4D	7.2	IC50	63	nM	CHEMBL_ACT_25011020
PDE4D	7.2	IC50	63	nM	CHEMBL_ACT_311417
PDE4B	7.15	IC50	71	nM	CHEMBL_ACT_704159
PDE4A	7.14	IC50	73	nM	CHEMBL_ACT_1160157
PDE4A	7.14	IC50	73	nM	CHEMBL_ACT_609046
PDE4D	7.1	IC50	79	nM	CHEMBL_ACT_906408
PDE4B	7.08	IC50	84	nM	CHEMBL_ACT_1802648
PDE4B	7.02	IC50	95	nM	CHEMBL_ACT_13864589
PDE4A	7.02	IC50	95	nM	CHEMBL_ACT_22875412
PDE4B	7.02	IC50	95	nM	CHEMBL_ACT_24867615
PDE4A	7.02	IC50	95	nM	CHEMBL_ACT_961795
PDE4A	7	IC50	100	nM	CHEMBL_ACT_1038921

Target pathways

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

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
chronic obstructive pulmonary disease	3	MONDO:0005002	EFO:0000341

Clinical trials

Total trials: 1.

Phase distribution

Phase	Trials
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00103922	PHASE3	COMPLETED	Study In Subjects With COPD (Chronic Obstructive Pulmonary Disease)

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

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