Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMFGYKS)

Drug Name

MK-5108 Drug Info

Synonyms

1010085-13-8; VX-689; MK 5108; MK5108; MK-5108 (VX-689); UNII-H8J407531S; VX689; VX 689; CHEMBL3600873; H8J407531S; 4-(3-chloro-2-fluorophenoxy)-1-[[6-(1,3-thiazol-2-ylamino)pyridin-2-yl]methyl]cyclohexane-1-carboxylic acid; 4-(3-Chloranyl-2-Fluoranyl-Phenoxy)-1-[[6-(1,3-Thiazol-2-Ylamino)pyridin-2-Yl]methyl]cyclohexane-1-Carboxylic Acid; (1r,4r)-4-(3-chloro-2-fluorophenoxy)-1-((6-(thiazol-2-ylamino)pyridin-2-yl)methyl)cyclohexane-1-carboxylic acid; Cyclohexanecarboxylic acid,; MK-5108/VX-689

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Phase 1	[1]

Cross-matching ID

PubChem CID: 24748204
ChEBI ID: CHEBI:125340
CAS Number: CAS 1010085-13-8
TTD Drug ID: DMFGYKS

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Clinical Trial Drug(s)

Download the Complete Related Drug List

Drug(s) Targeting Aurora kinase B (AURKB)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AT9283	DMQ94CT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[3]
PHA-739358	DMGYBZI	Prostate cancer	2C82.0	Phase 2	[4]
VX-680	DM93YKJ	Solid tumour/cancer	2A00-2F9Z	Phase 2	[5]
ABT-348	DMMZOYN	Haematological malignancy	2B33.Y	Phase 2	[6]
HPP-607	DM5VSZR	Solid tumour/cancer	2A00-2F9Z	Phase 1	[7]
CYC116	DMUMHXT	Solid tumour/cancer	2A00-2F9Z	Phase 1	[8]
AMG 900	DMASGXJ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[9]
SNS-314	DMAC5F2	Solid tumour/cancer	2A00-2F9Z	Phase 1	[10]
BI-847325	DMY4B6J	Solid tumour/cancer	2A00-2F9Z	Phase 1	[11]
R763	DME0CJ9	Haematological malignancy	2B33.Y	Phase 1	[12]
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Drug(s) Targeting Aurora kinase A (AURKA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AT9283	DMQ94CT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[3]
MLN8237	DMO8PT9	Solid tumour/cancer	2A00-2F9Z	Phase 3	[13]
PHA-739358	DMGYBZI	Prostate cancer	2C82.0	Phase 2	[4]
VX-680	DM93YKJ	Solid tumour/cancer	2A00-2F9Z	Phase 2	[5]
ABT-348	DMMZOYN	Haematological malignancy	2B33.Y	Phase 2	[6]
ENMD-2076	DMJZVPB	Acute myeloid leukaemia	2A60	Phase 2	[4]
LY3295668	DM8RJTB	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[14]
HPP-607	DM5VSZR	Solid tumour/cancer	2A00-2F9Z	Phase 1	[7]
MLN8054	DMUANF3	Solid tumour/cancer	2A00-2F9Z	Phase 1	[5]
CYC116	DMUMHXT	Solid tumour/cancer	2A00-2F9Z	Phase 1	[8]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Aurora kinase A (AURKA)	TTPS3C0	AURKA_HUMAN	Inhibitor	[2]
Aurora kinase B (AURKB)	TT5LS6T	AURKB_HUMAN	Inhibitor	[2]

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References

1	ClinicalTrials.gov (NCT00543387) Treatment of Participants With Advanced and/or Refractory Solid Tumors (MK-5108-001 AM4). U.S. National Institutes of Health.
2	A novel c-Met inhibitor, MK8033, synergizes with carboplatin plus paclitaxel to inhibit ovarian cancer cell growth. Oncol Rep. 2013 May;29(5):2011-8.
3	A phase I trial of AT9283 (a selective inhibitor of aurora kinases) in children and adolescents with solid tumors: a Cancer Research UK study. Clin Cancer Res. 2015 Jan 15;21(2):267-73.
4	Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
5	A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
6	Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families. J Pharmacol Exp Ther. 2012 Dec;343(3):617-27.
7	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1936).
8	Clinical pipeline report, company report or official report of Cyclacel.
9	Preclinical evaluation of AMG 900, a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines. Cancer Res. 2010 Dec 1;70(23):9846-54.
10	SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo. Cancer Chemother Pharmacol. 2010 Mar;65(4):707-17.
11	doi: 10.1158/1535-7163.TARG-13-B281
12	Preclinical characterization of Aurora kinase inhibitor R763/AS703569 identified through an image-based phenotypic screen. J Cancer Res Clin Oncol. 2010 Jan;136(1):99-113.
13	Effect of Aurora A kinase inhibitor MLN8237 combined with rituximab on antitumor activity in preclinical B-cell non-Hodgkin's lymphoma models. Journal of Clinical Oncology, 2009:8553.
14	Aurora A-Selective Inhibitor LY3295668 Leads to Dominant Mitotic Arrest, Apoptosis in Cancer Cells, and Shows Potent Preclinical Antitumor Efficacy. Mol Cancer Ther. 2019 Dec;18(12):2207-2219.