MK-0557

Summary

Mk-0557 (CHEMBL595573) is a phase-3 clinical-stage small molecule; indicated across 2 conditions including obesity disorder.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 2 conditions
• Clinical trials: 5
• Chemistry: 406.4 Da · C22H19FN4O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL595573
Name	MK-0557
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	11491176
Molecular formula	C22H19FN4O3
Molecular weight	406.4
InChIKey	RMYZIRFUCOMQRH-UHFFFAOYSA-N

SMILES: C1CC2(CCC1C(=O)NC3=NN(C=C3)C4=CC=CC=C4F)C5=C(C=CN=C5)C(=O)O2

IUPAC name: N-[1-(2-fluorophenyl)pyrazol-3-yl]-1’-oxospiro[cyclohexane-4,3’-furo[3,4-c]pyridine]-1-carboxamide

Also known as: Mk-0557, Mk0557, MK0557, MK-0557

Patent coverage: 17 distinct patent families (31 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: 3 (assay-derived). Sample: D(3) dopamine receptor, Neuropeptide Y receptor type 5, Neuropeptide Y receptor type 5.

Bioactivity

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

Target	pChembl	Type	Value	Unit	Activity ID
NPY5R	8.9	IC50	1.26	nM	CHEMBL_ACT_3597643
NPY5R	8.89	IC50	1.3	nM	CHEMBL_ACT_3066640
NPY5R	8.8	Ki	1.6	nM	CHEMBL_ACT_10857907
Q63634	8.68	IC50	2.1	nM	CHEMBL_ACT_3066786
DRD3	5.45	Ki	3566	nM	CHEMBL_ACT_25741228

Target pathways

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

Indications & clinical

Indications

2 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
obesity disorder	3	MONDO:0011122	EFO:0001073

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 5.

Phase distribution

Phase	Trials
PHASE2	3
PHASE3	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00092859	PHASE3	COMPLETED	A 2-Year Study of an Investigational Drug in Obese Patients (0557-011)
NCT00092872	PHASE3	COMPLETED	A 1-Year Study of an Investigational Drug in Obese Patients (0557-012)(COMPLETED)
NCT00482430	PHASE2	COMPLETED	MK0557 for the Treatment of Cognitive Impairment in Patients With Schizophrenia (0557-027)
NCT00533481	PHASE2	COMPLETED	Efficacy of MK0557 in Combination With Sibutramine or Orlistat (0557-015)(COMPLETED)
NCT00533598	PHASE2	COMPLETED	A Study to Determine the Effects of MK0557 in Obese Subjects (0557-006)(COMPLETED)

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).