DGIdb - ENTINOSTAT Drug Record

ENTINOSTAT chembl:CHEMBL27759 Antineoplastic

Alternate Names:

MS-275
MS-27-275
ENTINOSTAT
MS-275-27
SNDX-275
BAY 86-5274
MS 27-275
N-[[4-[(2-AMINOANILINO)-OXOMETHYL]PHENYL]METHYL]CARBAMIC ACID 3-PYRIDINYLMETHYL ESTER
SNDX 275
BAY86-5274
MS 275
N-(2-AMINOPHENYL)-4-(N-(PYRIDIN-3-YLMETHOXYCARBONYL)AMINOMETHYL)BENZAMIDE
chemidplus:209783-80-2
chembl:CHEMBL27759
pubchem.compound:4261
drugbank:11841

Drug Info:

FDA Approval	not approved
Drug Class	Small molecule
Drug Indications	antineoplastic agent

(4 More Sources)

Publications:

Dalgard et al., 2008, Evaluation of the in vitro and in vivo antitumor activity of histone deacetylase inhibitors for the therapy of retinoblastoma., Clin. Cancer Res.
Rushlow et al., 2013, Characterisation of retinoblastomas without RB1 mutations: genomic, gene expression, and clinical studies., Lancet Oncol.
Hutt DM et al., 2010, Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis., Nat Chem Biol
Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem
Kemp MM et al., 2011, A novel HDAC inhibitor with a hydroxy-pyrimidine scaffold., Bioorg Med Chem Lett
Kiyokawa S et al., 2010, New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group., Bioorg Med Chem
Mai A et al., 2008, Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities., Bioorg Med Chem Lett
Hirata Y et al., 2012, Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain., Bioorg Med Chem Lett
He et al., 2013, Mcl-1 and FBW7 control a dominant survival pathway underlying HDAC and Bcl-2 inhibitor synergy in squamous cell carcinoma., Cancer Discov

ENTINOSTAT FBXW7

Interaction Score: 0.79

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type hematologic cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
23274910

Sources:
JAX-CKB
ENTINOSTAT HDAC1

Interaction Score: 0.65

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name entinostat, SNDX-275, MS-275

Notes

PMIDs:
20452226 19966789 18381238 20491440 22321215

Sources:
DTC TdgClinicalTrial TTD TALC GuideToPharmacology ChemblInteractions
ENTINOSTAT HDAC3

Interaction Score: 0.53

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
19966789 20491440

Sources:
DTC TdgClinicalTrial TALC GuideToPharmacology ChemblInteractions
ENTINOSTAT HDAC2

Interaction Score: 0.42

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Mechanism of Interaction Histone deacetylase inhibitor

Direct Interaction yes

PMIDs:
19966789 20491440 22321215

Sources:
DTC TALC GuideToPharmacology ChemblInteractions
ENTINOSTAT RB1

Interaction Score: 0.41

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type retinoblastoma

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
18483379 23498719

Sources:
JAX-CKB
ENTINOSTAT HDAC11

Interaction Score: 0.41

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Histone deacetylase inhibitor

PMIDs:
19966789 20491440

Sources:
DTC ChemblInteractions
ENTINOSTAT HDAC4

Interaction Score: 0.38

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Histone deacetylase inhibitor

Direct Interaction yes

PMIDs:
19966789 18381238 20491440

Sources:
DTC ChemblInteractions
ENTINOSTAT HDAC9

Interaction Score: 0.37

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
19966789 20491440

Sources:
DTC GuideToPharmacology
ENTINOSTAT HDAC10

Interaction Score: 0.36

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Histone deacetylase inhibitor

Direct Interaction yes

PMIDs:
19966789 20491440

Sources:
DTC ChemblInteractions
ENTINOSTAT HDAC6

Interaction Score: 0.36

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Histone deacetylase inhibitor

PMIDs:
21696956 19966789 20491440

Sources:
DTC ChemblInteractions
ENTINOSTAT HDAC7

Interaction Score: 0.34

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Histone deacetylase inhibitor

Direct Interaction yes

PMIDs:
19966789 20491440

Sources:
DTC ChemblInteractions
ENTINOSTAT HDAC5

Interaction Score: 0.33

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Histone deacetylase inhibitor

PMIDs:
19966789 20491440

Sources:
DTC ChemblInteractions
ENTINOSTAT HDAC8

Interaction Score: 0.33

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Histone deacetylase inhibitor

Direct Interaction yes

Notes

PMIDs:
19966789 20491440

Sources:
DTC TALC ChemblInteractions
ENTINOSTAT CFTR

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19966789

Sources:
DTC
ENTINOSTAT ERBB2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Entinostat + Lapatinib + Trastuzumab

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

PMIDs:
None found

Sources:
JAX-CKB
ENTINOSTAT HTT

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
ENTINOSTAT YES1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ENTINOSTAT ATAD5

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

TdgClinicalTrial: ENTINOSTAT
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Publications:

DTC: ENTINOSTAT

Version: 02-September-2020

Alternate Names:

CHEMBL27759 ChEMBL Drug ID

Drug Info:

Publications:

Hutt DM et al., 2010, Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis., Nat Chem Biol

Mai A et al., 2008, Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities., Bioorg Med Chem Lett

Souto JA et al., 2010, Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues., J Med Chem

JAX-CKB: Entinostat

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

He et al., 2013, Mcl-1 and FBW7 control a dominant survival pathway underlying HDAC and Bcl-2 inhibitor synergy in squamous cell carcinoma., Cancer Discov

Dalgard et al., 2008, Evaluation of the in vitro and in vivo antitumor activity of histone deacetylase inhibitors for the therapy of retinoblastoma., Clin. Cancer Res.

Rushlow et al., 2013, Characterisation of retinoblastomas without RB1 mutations: genomic, gene expression, and clinical studies., Lancet Oncol.

TTD: SNDX-275
- Version: 2020.06.01
Alternate Names:

D0M8FD TTD Drug ID

Drug Info:

Publications:
GuideToPharmacology: 178103586
- Version: 29-September-2020
Alternate Names:

ENTINOSTAT GuideToPharmacology Ligand Name

Drug Info:

Publications:
TALC: ENTINOSTAT
- Version: 12-May-2016
Alternate Names:

ENTINOSTAT Primary Drug Name

ENTINOSTAT Drug Generic Name

MS-275 Drug Synonym

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL27759
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL27759
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Indication/Tumor Type	hematologic cancer
Response Type	sensitive
Approval Status	Preclinical

Novel drug target	Established target
Trial Name	entinostat, SNDX-275, MS-275
Notes

Specific Action of the Ligand	Inhibition
Endogenous Drug?	False
Direct Interaction?	False

Notes
Mechanism of Interaction	Histone deacetylase inhibitor
Direct Interaction	yes

Indication/Tumor Type	retinoblastoma
Response Type	sensitive
Approval Status	Preclinical - Cell line xenograft

combination therapy	Entinostat + Lapatinib + Trastuzumab
Indication/Tumor Type	Her2-receptor positive breast cancer
Response Type	sensitive

ENTINOSTAT	Primary Drug Name
ENTINOSTAT	Drug Generic Name
MS-275	Drug Synonym

ENTINOSTAT Drug Record

ENTINOSTAT chembl:CHEMBL27759 Antineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type hematologic cancer Response Type sensitive Approval Status Preclinical

PMIDs: 23274910

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Novel drug target Established target Trial Name entinostat, SNDX-275, MS-275 Notes

PMIDs: 20452226 19966789 18381238 20491440 22321215

Sources: DTC TdgClinicalTrial TTD TALC GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: 19966789 20491440

Sources: DTC TdgClinicalTrial TALC GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Notes Mechanism of Interaction Histone deacetylase inhibitor Direct Interaction yes

PMIDs: 19966789 20491440 22321215

Sources: DTC TALC GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type retinoblastoma Response Type sensitive Approval Status Preclinical - Cell line xenograft

PMIDs: 18483379 23498719

Sources: JAX-CKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Histone deacetylase inhibitor

PMIDs: 19966789 20491440

Sources: DTC ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Histone deacetylase inhibitor Direct Interaction yes

PMIDs: 19966789 18381238 20491440

Sources: DTC ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: 19966789 20491440

Sources: DTC GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Histone deacetylase inhibitor Direct Interaction yes

PMIDs: 19966789 20491440

Sources: DTC ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Histone deacetylase inhibitor

PMIDs: 21696956 19966789 20491440

Sources: DTC ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Histone deacetylase inhibitor Direct Interaction yes

PMIDs: 19966789 20491440

Sources: DTC ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Histone deacetylase inhibitor

PMIDs: 19966789 20491440

Sources: DTC ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Histone deacetylase inhibitor Direct Interaction yes Notes

PMIDs: 19966789 20491440

Sources: DTC TALC ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19966789

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Entinostat + Lapatinib + Trastuzumab Indication/Tumor Type Her2-receptor positive breast cancer Response Type sensitive

PMIDs: None found

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

TdgClinicalTrial: ENTINOSTAT

Alternate Names:

Drug Info: Drug Indications antineoplastic agent Drug Class Small molecule FDA Approval not approved

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type hematologic cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
23274910

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name entinostat, SNDX-275, MS-275

Notes

PMIDs:
20452226 19966789 18381238 20491440 22321215

Sources:
DTC TdgClinicalTrial TTD TALC GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
19966789 20491440

Sources:
DTC TdgClinicalTrial TALC GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Mechanism of Interaction Histone deacetylase inhibitor

Direct Interaction yes

PMIDs:
19966789 20491440 22321215

Sources:
DTC TALC GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type retinoblastoma

Response Type sensitive

Approval Status Preclinical - Cell line xenograft

PMIDs:
18483379 23498719

Sources:
JAX-CKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Histone deacetylase inhibitor

PMIDs:
19966789 20491440

Sources:
DTC ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Histone deacetylase inhibitor

Direct Interaction yes

PMIDs:
19966789 18381238 20491440

Sources:
DTC ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
19966789 20491440

Sources:
DTC GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Histone deacetylase inhibitor

Direct Interaction yes

PMIDs:
19966789 20491440

Sources:
DTC ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Histone deacetylase inhibitor

PMIDs:
21696956 19966789 20491440

Sources:
DTC ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Histone deacetylase inhibitor

Direct Interaction yes

PMIDs:
19966789 20491440

Sources:
DTC ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Histone deacetylase inhibitor

PMIDs:
19966789 20491440

Sources:
DTC ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Histone deacetylase inhibitor

Direct Interaction yes

Notes

PMIDs:
19966789 20491440

Sources:
DTC TALC ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
19966789

Sources:
DTC

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Entinostat + Lapatinib + Trastuzumab

Indication/Tumor Type Her2-receptor positive breast cancer

Response Type sensitive

PMIDs:
None found

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small molecule

FDA Approval not approved

Alternate Names:

CHEMBL27759 ChEMBL Drug ID

Alternate Names:

D0M8FD TTD Drug ID

Alternate Names:

ENTINOSTAT GuideToPharmacology Ligand Name

Alternate Names:

ENTINOSTAT Primary Drug Name

ENTINOSTAT Drug Generic Name

MS-275 Drug Synonym