Details of the Drug Combination

General Information of Drug Combination (ID: DCH070R)

• Drug Combination Name: Rigosertib + Idarubicin
• Indication: Glioblastoma?; Status: Investigative [1]
• Component Drugs:
  Rigosertib (DMOSTXF): Small molecular drug
  Idarubicin (DMM0XGL): Small molecular drug
• High-throughput Screening Result:
  Testing Cell Line: T98G
  Zero Interaction Potency (ZIP) Score: 4.18
  Bliss Independence Score: 4.18
  Loewe Additivity Score: 6.69
  LHighest Single Agent (HSA) Score: 6.77

Molecular Interaction Atlas of This Drug Combination

Indication(s) of Rigosertib

Disease Entry	ICD 11	Status	REF
Myelodysplastic syndrome	2A37	Phase 3	[2]
Solid tumour/cancer	2A00-2F9Z	Phase 3	[3]

Rigosertib Interacts with 2 DTT Molecule(s)

DTT Name	DTT ID	UniProt ID	Mode of Action	REF
Polo-like kinase 1 (PLK1)	TTIYVQP	PLK1_HUMAN	Modulator	[8]
PI3-kinase gamma (PIK3CG)	TTHBTOP	PK3CG_HUMAN	Modulator	[8]

Rigosertib Interacts with 143 DOT Molecule(s)

DOT Name	DOT ID	UniProt ID	Mode of Action	REF
NF-kappa-B inhibitor epsilon (NFKBIE)	OTLAYEL9	IKBE_HUMAN	Affects Expression	[6]
Chloride intracellular channel protein 1 (CLIC1)	OTYLFWNG	CLIC1_HUMAN	Increases Expression	[6]
Nuclear factor 1 B-type (NFIB)	OTX94PD0	NFIB_HUMAN	Increases Expression	[6]
Transcription regulator protein BACH1 (BACH1)	OTY8004K	BACH1_HUMAN	Increases Expression	[6]
Protein Mdm4 (MDM4)	OTU10BSF	MDM4_HUMAN	Affects Expression	[6]
3-phosphoinositide-dependent protein kinase 1 (PDPK1)	OTT09ZVP	PDPK1_HUMAN	Decreases Phosphorylation	[9]
Protein MTSS 1 (MTSS1)	OT5DTDO2	MTSS1_HUMAN	Increases Expression	[6]
Bcl-2-like protein 11 (BCL2L11)	OTNQQWFJ	B2L11_HUMAN	Increases Expression	[10]
Cytohesin-interacting protein (CYTIP)	OTRJ3ZC5	CYTIP_HUMAN	Increases Expression	[6]
F-box-like/WD repeat-containing protein TBL1X (TBL1X)	OTXQ51E0	TBL1X_HUMAN	Increases Expression	[6]
Short-chain dehydrogenase/reductase 3 (DHRS3)	OTSK1DTP	DHRS3_HUMAN	Affects Expression	[6]
Serine/threonine-protein kinase Chk2 (CHEK2)	OT8ZPCNS	CHK2_HUMAN	Increases Phosphorylation	[11]
2'-5'-oligoadenylate synthase 1 (OAS1)	OT8ZLOCY	OAS1_HUMAN	Decreases Expression	[6]
Myc proto-oncogene protein (MYC)	OTPV5LUK	MYC_HUMAN	Decreases Expression	[9]
HLA class II histocompatibility antigen, DQ beta 1 chain (HLA-DQB1)	OTVVI3UI	DQB1_HUMAN	Affects Expression	[6]
Albumin (ALB)	OTVMM513	ALBU_HUMAN	Affects Binding	[12]
Glucocorticoid receptor (NR3C1)	OTCI2YDI	GCR_HUMAN	Increases Expression	[6]
Receptor tyrosine-protein kinase erbB-2 (ERBB2)	OTOAUNCK	ERBB2_HUMAN	Increases Phosphorylation	[7]
Transcription factor Jun (JUN)	OTCYBO6X	JUN_HUMAN	Increases Expression	[6]
Tyrosine-protein kinase Lck (LCK)	OT883FG9	LCK_HUMAN	Increases Phosphorylation	[7]
Tyrosine-protein kinase Fyn (FYN)	OTLSLVZS	FYN_HUMAN	Increases Phosphorylation	[7]
Cyclin-dependent kinase 1 (CDK1)	OTW1SC2N	CDK1_HUMAN	Increases Expression	[7]
Eukaryotic translation initiation factor 4E (EIF4E)	OTDAWNLA	IF4E_HUMAN	Decreases Activity	[9]
Macrophage colony-stimulating factor 1 receptor (CSF1R)	OTDYTB9C	CSF1R_HUMAN	Increases Expression	[6]
Proto-oncogene tyrosine-protein kinase receptor Ret (RET)	OTLU040A	RET_HUMAN	Increases Phosphorylation	[7]
Platelet-derived growth factor receptor beta (PDGFRB)	OTYSNK9Q	PGFRB_HUMAN	Increases Phosphorylation	[7]
Poly polymerase 1 (PARP1)	OT310QSG	PARP1_HUMAN	Increases Cleavage	[9]
Interleukin-8 (CXCL8)	OTS7T5VH	IL8_HUMAN	Increases Expression	[6]
Transcriptional activator Myb (MYB)	OTJH64IV	MYB_HUMAN	Affects Localization	[13]
Apoptosis regulator Bcl-2 (BCL2)	OT9DVHC0	BCL2_HUMAN	Decreases Expression	[7]
cAMP-dependent protein kinase type I-alpha regulatory subunit (PRKAR1A)	OT589JA2	KAP0_HUMAN	Increases Expression	[6]
Retinoic acid receptor beta (RARB)	OT367U3E	RARB_HUMAN	Increases Expression	[6]
Lysosome-associated membrane glycoprotein 2 (LAMP2)	OTLUGEJC	LAMP2_HUMAN	Affects Expression	[6]
G2/mitotic-specific cyclin-B1 (CCNB1)	OT19S7E5	CCNB1_HUMAN	Decreases Expression	[14]
Matrix metalloproteinase-9 (MMP9)	OTB2QDAV	MMP9_HUMAN	Affects Expression	[6]
Fatty acid-binding protein, adipocyte (FABP4)	OT3DKFOU	FABP4_HUMAN	Affects Expression	[6]
Ezrin (EZR)	OTHBPF1Z	EZRI_HUMAN	Increases Expression	[6]
Nucleoside diphosphate kinase A (NME1)	OT0NELQ1	NDKA_HUMAN	Decreases Expression	[6]
CD44 antigen (CD44)	OT9TTJ41	CD44_HUMAN	Increases Expression	[6]
Histone H2AX (H2AX)	OT18UX57	H2AX_HUMAN	Increases Expression	[15]
Cytotoxic T-lymphocyte protein 4 (CTLA4)	OTYQR611	CTLA4_HUMAN	Increases Expression	[6]
Transcription factor JunD (JUND)	OTNKACJD	JUND_HUMAN	Increases Expression	[6]
Early growth response protein 1 (EGR1)	OTCP6XGZ	EGR1_HUMAN	Affects Expression	[6]
Transcription factor E3 (TFE3)	OTM99ZWH	TFE3_HUMAN	Affects Expression	[6]
Lamin-B1 (LMNB1)	OT100T3P	LMNB1_HUMAN	Increases Cleavage	[11]
Ephrin type-A receptor 1 (EPHA1)	OTGJMRZ0	EPHA1_HUMAN	Increases Phosphorylation	[7]
Fibroblast growth factor receptor 2 (FGFR2)	OTLOPACK	FGFR2_HUMAN	Decreases Phosphorylation	[7]
B-cell differentiation antigen CD72 (CD72)	OTPOJID2	CD72_HUMAN	Decreases Expression	[6]
G1/S-specific cyclin-D1 (CCND1)	OT8HPTKJ	CCND1_HUMAN	Decreases Expression	[9]
Tyrosine-protein phosphatase non-receptor type 6 (PTPN6)	OT33XNZM	PTN6_HUMAN	Decreases Expression	[6]
G1/S-specific cyclin-D2 (CCND2)	OTDULQF9	CCND2_HUMAN	Decreases Expression	[9]
M-phase inducer phosphatase 3 (CDC25C)	OTPQI71S	MPIP3_HUMAN	Decreases Expression	[16]
RAC-alpha serine/threonine-protein kinase (AKT1)	OT8H2YY7	AKT1_HUMAN	Decreases Phosphorylation	[9]
RAC-beta serine/threonine-protein kinase (AKT2)	OTBB632K	AKT2_HUMAN	Decreases Phosphorylation	[17]
Mannosyl-oligosaccharide 1,2-alpha-mannosidase IA (MAN1A1)	OT6LIGJP	MA1A1_HUMAN	Increases Expression	[6]
Tyrosine-protein kinase RYK (RYK)	OTZ3WWZH	RYK_HUMAN	Decreases Phosphorylation	[7]
Catenin beta-1 (CTNNB1)	OTZ932A3	CTNB1_HUMAN	Decreases Phosphorylation	[7]
DNA damage-inducible transcript 3 protein (DDIT3)	OTI8YKKE	DDIT3_HUMAN	Increases Expression	[6]
Vascular endothelial growth factor receptor 2 (KDR)	OT15797V	VGFR2_HUMAN	Decreases Phosphorylation	[7]
Cyclin-dependent kinase inhibitor 1 (CDKN1A)	OTQWHCZE	CDN1A_HUMAN	Increases Expression	[6]
Interleukin-6 receptor subunit beta (IL6ST)	OT1N9C70	IL6RB_HUMAN	Increases Expression	[6]
Signal transducer and activator of transcription 3 (STAT3)	OTAAGKYZ	STAT3_HUMAN	Decreases Phosphorylation	[7]
ETS translocation variant 5 (ETV5)	OTE2OBM4	ETV5_HUMAN	Increases Expression	[6]
Regulator of G-protein signaling 2 (RGS2)	OT0FSRW7	RGS2_HUMAN	Increases Expression	[6]
Protein kinase C iota type (PRKCI)	OTKBAVT3	KPCI_HUMAN	Increases Expression	[6]
Serine/threonine-protein kinase mTOR (MTOR)	OTHH8KU7	MTOR_HUMAN	Decreases Phosphorylation	[9]
Caspase-3 (CASP3)	OTIJRBE7	CASP3_HUMAN	Increases Activity	[10]
Tyrosine-protein kinase FRK (FRK)	OTEKV1SC	FRK_HUMAN	Increases Phosphorylation	[7]
Nuclear receptor subfamily 4 group A member 2 (NR4A2)	OT3F9IR2	NR4A2_HUMAN	Increases Expression	[6]
Tyrosine-protein kinase SYK (SYK)	OTQID87L	KSYK_HUMAN	Increases Phosphorylation	[7]
Mitogen-activated protein kinase 9 (MAPK9)	OTCEVJ9E	MK09_HUMAN	Increases Phosphorylation	[7]
Ran GTPase-activating protein 1 (RANGAP1)	OTZGD3LJ	RAGP1_HUMAN	Increases Phosphorylation	[18]
Crk-like protein (CRKL)	OTOYSD1R	CRKL_HUMAN	Decreases Phosphorylation	[19]
Glioma pathogenesis-related protein 1 (GLIPR1)	OT0FGQK7	GLIP1_HUMAN	Increases Expression	[6]
Max-interacting protein 1 (MXI1)	OTUQ9E0D	MXI1_HUMAN	Increases Expression	[6]
Tyrosine-protein kinase Blk (BLK)	OT1EB8MT	BLK_HUMAN	Increases Phosphorylation	[7]
Protein FosB (FOSB)	OTW6C05J	FOSB_HUMAN	Decreases Expression	[6]
Epithelial membrane protein 1 (EMP1)	OTSZHUHQ	EMP1_HUMAN	Increases Expression	[6]
Caspase-7 (CASP7)	OTAPJ040	CASP7_HUMAN	Increases Activity	[10]
Caspase-9 (CASP9)	OTD4RFFG	CASP9_HUMAN	Increases Cleavage	[9]
BH3-interacting domain death agonist (BID)	OTOSHSHU	BID_HUMAN	Decreases Expression	[9]
Claudin-15 (CLDN15)	OT9K0KI7	CLD15_HUMAN	Affects Expression	[6]
Leukocyte immunoglobulin-like receptor subfamily A member 4 (LILRA4)	OTKC3PA6	LIRA4_HUMAN	Decreases Expression	[6]
Actin, cytoplasmic 1 (ACTB)	OT1MCP2F	ACTB_HUMAN	Increases Expression	[6]
Rho-related GTP-binding protein RhoB (RHOB)	OTHQFQF7	RHOB_HUMAN	Increases Expression	[6]
Small ribosomal subunit protein eS6 (RPS6)	OTT4D1LN	RS6_HUMAN	Decreases Phosphorylation	[20]
Actin, cytoplasmic 2 (ACTG1)	OTH4V7VQ	ACTG_HUMAN	Increases Expression	[6]
Tropomyosin alpha-4 chain (TPM4)	OTN4YLYR	TPM4_HUMAN	Increases Expression	[6]
Histone H3.3 (H3-3B)	OT9XHQ3C	H33_HUMAN	Increases Expression	[6]
DNA-binding protein inhibitor ID-2 (ID2)	OT0U1D53	ID2_HUMAN	Increases Expression	[6]
Angiopoietin-1 receptor (TEK)	OT78YN57	TIE2_HUMAN	Decreases Phosphorylation	[7]
cAMP-responsive element modulator (CREM)	OTJIJ5AL	CREM_HUMAN	Increases Expression	[6]
Histone-lysine N-methyltransferase 2A (KMT2A)	OT9GLJI6	KMT2A_HUMAN	Increases Expression	[6]
Dual specificity protein phosphatase 2 (DUSP2)	OTH54FMR	DUS2_HUMAN	Decreases Expression	[6]
3',5'-cyclic-AMP phosphodiesterase 4B (PDE4B)	OTOA8WU2	PDE4B_HUMAN	Increases Expression	[6]
Bcl-2-like protein 1 (BCL2L1)	OTRC5K9O	B2CL1_HUMAN	Decreases Expression	[9]
Induced myeloid leukemia cell differentiation protein Mcl-1 (MCL1)	OT2YYI1A	MCL1_HUMAN	Decreases Expression	[9]
Son of sevenless homolog 2 (SOS2)	OTV3XRE5	SOS2_HUMAN	Increases Expression	[6]
Forkhead box protein O1 (FOXO1)	OTPJRB6D	FOXO1_HUMAN	Affects Phosphorylation	[9]
Inositol 1,4,5-triphosphate receptor associated 2 (IRAG2)	OTLUTKJQ	IRAG2_HUMAN	Affects Expression	[6]
Dual specificity protein phosphatase 4 (DUSP4)	OT6WAO12	DUS4_HUMAN	Increases Expression	[6]
Non-receptor tyrosine-protein kinase TNK1 (TNK1)	OTXG5RWQ	TNK1_HUMAN	Increases Phosphorylation	[7]
Sequestosome-1 (SQSTM1)	OTGY5D5J	SQSTM_HUMAN	Affects Expression	[6]
Eukaryotic translation initiation factor 4E-binding protein 1 (EIF4EBP1)	OTHBQVD5	4EBP1_HUMAN	Decreases Phosphorylation	[9]
Phorbol-12-myristate-13-acetate-induced protein 1 (PMAIP1)	OTXEE550	APR_HUMAN	Increases Expression	[6]
Krueppel-like factor 5 (KLF5)	OT1ABI9N	KLF5_HUMAN	Increases Expression	[6]
Protein-tyrosine kinase 2-beta (PTK2B)	OTGAS0I8	FAK2_HUMAN	Increases Phosphorylation	[7]
Genetic suppressor element 1 (GSE1)	OT3J7CJB	GSE1_HUMAN	Affects Expression	[6]
Nuclear mitotic apparatus protein 1 (NUMA1)	OTTKAVG4	NUMA1_HUMAN	Affects Localization	[21]
Astrocytic phosphoprotein PEA-15 (PEA15)	OTKCKTSX	PEA15_HUMAN	Increases Expression	[6]
Interferon regulatory factor 4 (IRF4)	OT1DHQ1P	IRF4_HUMAN	Affects Expression	[6]
Microtubule-associated protein RP/EB family member 1 (MAPRE1)	OTCVQD60	MARE1_HUMAN	Affects Localization	[21]
Exostosin-1 (EXT1)	OTRPALJK	EXT1_HUMAN	Increases Expression	[6]
Serine/arginine-rich splicing factor 7 (SRSF7)	OTRS4W4S	SRSF7_HUMAN	Increases Expression	[6]
Pleckstrin homology-like domain family A member 2 (PHLDA2)	OTMV9DPP	PHLA2_HUMAN	Increases Expression	[6]
Muscleblind-like protein 2 (MBNL2)	OTF7CF1F	MBNL2_HUMAN	Increases Expression	[6]
Histone H2A.V (H2AZ2)	OT0I5H2P	H2AV_HUMAN	Increases Expression	[6]
Syntaxin-12 (STX12)	OT5IBQ62	STX12_HUMAN	Increases Expression	[6]
Polycomb group protein ASXL1 (ASXL1)	OTX931AW	ASXL1_HUMAN	Increases Expression	[6]
DDB1- and CUL4-associated factor 11 (DCAF11)	OTNSGYK1	DCA11_HUMAN	Increases Expression	[6]
Protein NDRG1 (NDRG1)	OTVO66BO	NDRG1_HUMAN	Increases Expression	[6]
Estrogen receptor beta (ESR2)	OTXNR2WQ	ESR2_HUMAN	Increases Expression	[6]
TRAF family member-associated NF-kappa-B activator (TANK)	OTZSGFIK	TANK_HUMAN	Increases Expression	[6]
Proline-rich AKT1 substrate 1 (AKT1S1)	OT4JHN4Y	AKTS1_HUMAN	Decreases Phosphorylation	[15]
MAP/microtubule affinity-regulating kinase 4 (MARK4)	OT6Z2TGV	MARK4_HUMAN	Increases Expression	[6]
Tribbles homolog 1 (TRIB1)	OTPEO17G	TRIB1_HUMAN	Increases Expression	[6]
Krueppel-like factor 6 (KLF6)	OTQY9S7F	KLF6_HUMAN	Increases Expression	[6]
Mitogen-activated protein kinase kinase kinase 3 (MAP3K3)	OT53LJGW	M3K3_HUMAN	Affects Expression	[6]
Calsyntenin-3 (CLSTN3)	OTPUFK4C	CSTN3_HUMAN	Affects Expression	[6]
Reticulon-4 (RTN4)	OTIH85O3	RTN4_HUMAN	Affects Expression	[6]
DNA damage-inducible transcript 4 protein (DDIT4)	OTHY8SY4	DDIT4_HUMAN	Increases Expression	[6]
Bcl-2-associated transcription factor 1 (BCLAF1)	OT7T8H6A	BCLF1_HUMAN	Increases Expression	[6]
Eukaryotic translation initiation factor 2-alpha kinase 3 (EIF2AK3)	OT0DZGY4	E2AK3_HUMAN	Increases Expression	[6]
ADP-ribosylation factor-binding protein GGA2 (GGA2)	OT43HO27	GGA2_HUMAN	Increases Expression	[6]
F-box only protein 2 (FBXO2)	OTF3677S	FBX2_HUMAN	Affects Expression	[6]
Transcription factor MafF (MAFF)	OT9B7MX0	MAFF_HUMAN	Increases Expression	[6]
Disheveled-associated activator of morphogenesis 1 (DAAM1)	OT0VHIYZ	DAAM1_HUMAN	Increases Expression	[6]
TNF receptor-associated factor 6 (TRAF6)	OTA5GO5K	TRAF6_HUMAN	Affects Localization	[13]
Krueppel-like factor 12 (KLF12)	OTVH4KD4	KLF12_HUMAN	Increases Expression	[6]
Dual specificity protein phosphatase 10 (DUSP10)	OTNG467B	DUS10_HUMAN	Increases Expression	[6]
Cyclic AMP-dependent transcription factor ATF-3 (ATF3)	OTC1UOHP	ATF3_HUMAN	Increases Response To Substance	[6]
Cellular tumor antigen p53 (TP53)	OTIE1VH3	P53_HUMAN	Affects Response To Substance	[20]
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PIK3CA)	OTTOMI8J	PK3CA_HUMAN	Affects Response To Substance	[20]

Indication(s) of Idarubicin

Disease Entry	ICD 11	Status	REF
Acute myelogenous leukaemia	2A41	Approved	[4]
Acute myeloid leukaemia	2A60	Approved	[5]
Adult acute monocytic leukemia	N.A.	Approved	[4]
Childhood acute megakaryoblastic leukemia	N.A.	Approved	[4]
Leukemia	N.A.	Approved	[4]

Idarubicin Interacts with 1 DTT Molecule(s)

DTT Name	DTT ID	UniProt ID	Mode of Action	REF
DNA topoisomerase II (TOP2)	TT0IHXV	TOP2A_HUMAN; TOP2B_HUMAN	Modulator	[23]

Idarubicin Interacts with 3 DTP Molecule(s)

DTP Name	DTP ID	UniProt ID	Mode of Action	REF
Multidrug resistance-associated protein 1 (ABCC1)	DTSYQGK	MRP1_HUMAN	Substrate	[24]
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Substrate	[25]
Breast cancer resistance protein (ABCG2)	DTI7UX6	ABCG2_HUMAN	Substrate	[25]

Idarubicin Interacts with 2 DME Molecule(s)

DME Name	DME ID	UniProt ID	Mode of Action	REF
Cytochrome P450 2D6 (CYP2D6)	DECB0K3	CP2D6_HUMAN	Metabolism	[26]
Cytochrome P450 2C9 (CYP2C9)	DE5IED8	CP2C9_HUMAN	Metabolism	[26]

Idarubicin Interacts with 9 DOT Molecule(s)

DOT Name	DOT ID	UniProt ID	Mode of Action	REF
Estrogen receptor (ESR1)	OTKLU61J	ESR1_HUMAN	Decreases Activity	[22]
Heme oxygenase 1 (HMOX1)	OTC1W6UX	HMOX1_HUMAN	Increases Expression	[27]
Androgen receptor (AR)	OTUBKAZZ	ANDR_HUMAN	Increases Activity	[22]
Natriuretic peptides B (NPPB)	OTSN2IPY	ANFB_HUMAN	Increases Expression	[28]
Peroxisome proliferator-activated receptor gamma (PPARG)	OTHMARHO	PPARG_HUMAN	Decreases Activity	[22]
Caspase-3 (CASP3)	OTIJRBE7	CASP3_HUMAN	Increases Activity	[29]
Peroxisome proliferator-activated receptor delta (PPARD)	OTI4WTOP	PPARD_HUMAN	Decreases Activity	[22]
Potassium voltage-gated channel subfamily H member 2 (KCNH2)	OTZX881H	KCNH2_HUMAN	Decreases Activity	[30]
Bile acid receptor (NR1H4)	OTWZLPTB	NR1H4_HUMAN	Decreases Activity	[22]

References

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