Details of the Drug Combination

General Information of Drug Combination (ID: DCIALJR)

Drug Combination Name
AS602868 Bardoxolone methyl
Indication
Disease Entry Status REF
Glioblastoma Investigative [1]
Component Drugs AS602868   DMKXDOI Bardoxolone methyl   DMODA2X
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL
High-throughput Screening Result Testing Cell Line: JHH-136
Zero Interaction Potency (ZIP) Score: 19.874
Bliss Independence Score: 18.681
Loewe Additivity Score: 0.47
LHighest Single Agent (HSA) Score: 3.763

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of AS602868
Disease Entry ICD 11 Status REF
Multiple myeloma 2A83 Discontinued in Phase 1 [2]
AS602868 Interacts with 3 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Monoamine oxidase type B (MAO-B) TTGP7BY AOFB_HUMAN Inhibitor [5]
Nuclear factor NF-kappa-B (NFKB) TTSXVID NFKB1_HUMAN; NFKB2_HUMAN; TF65_HUMAN; RELB_HUMAN; REL_HUMAN Inhibitor [6]
Monoamine oxidase type A (MAO-A) TT3WG5C AOFA_HUMAN Inhibitor [5]
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AS602868 Interacts with 2 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Baculoviral IAP repeat-containing protein 5 (BIRC5) OTILXZYL BIRC5_HUMAN Decreases Expression [7]
Bcl-2-like protein 1 (BCL2L1) OTRC5K9O B2CL1_HUMAN Decreases Expression [7]
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Indication(s) of Bardoxolone methyl
Disease Entry ICD 11 Status REF
Mixed connective tissue disease 4A43.3 Phase 3 [3]
Pulmonary arterial hypertension BB01.0 Phase 2 [4]
Pulmonary hypertension BB01 Phase 2 [3]
Bardoxolone methyl Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
PPAR-gamma messenger RNA (PPARG mRNA) TTT2SVW PPARG_HUMAN Antagonist [9]
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Bardoxolone methyl Interacts with 75 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Glycogen synthase kinase-3 beta (GSK3B) OTL3L14B GSK3B_HUMAN Increases Phosphorylation [10]
Caspase-8 (CASP8) OTA8TVI8 CASP8_HUMAN Decreases Expression [10]
Nuclear factor erythroid 2-related factor 2 (NFE2L2) OT0HENJ5 NF2L2_HUMAN Increases Expression [10]
Muscarinic acetylcholine receptor M2 (CHRM2) OTUMZ2WR ACM2_HUMAN Decreases Activity [11]
Muscarinic acetylcholine receptor M1 (CHRM1) OTKW3E6B ACM1_HUMAN Decreases Activity [11]
D(2) dopamine receptor (DRD2) OTBLXKEG DRD2_HUMAN Decreases Activity [11]
Alpha-2C adrenergic receptor (ADRA2C) OT5B9RKP ADA2C_HUMAN Decreases Activity [11]
D(1A) dopamine receptor (DRD1) OTLZPBT7 DRD1_HUMAN Decreases Activity [11]
Substance-P receptor (TACR1) OTCL9OC5 NK1R_HUMAN Decreases Activity [11]
5-hydroxytryptamine receptor 2A (HTR2A) OTWXJX0M 5HT2A_HUMAN Decreases Activity [11]
5-hydroxytryptamine receptor 2C (HTR2C) OT6H8DE0 5HT2C_HUMAN Decreases Activity [11]
Histamine H1 receptor (HRH1) OT8F9FV6 HRH1_HUMAN Decreases Activity [11]
Alpha-1B adrenergic receptor (ADRA1B) OTSAYAFD ADA1B_HUMAN Decreases Activity [11]
Mu-type opioid receptor (OPRM1) OT16AAT8 OPRM_HUMAN Decreases Activity [11]
Vasopressin V1a receptor (AVPR1A) OTKR8AFL V1AR_HUMAN Decreases Activity [11]
Kappa-type opioid receptor (OPRK1) OTXCZF4L OPRK_HUMAN Decreases Activity [11]
3',5'-cyclic-AMP phosphodiesterase 4B (PDE4B) OTOA8WU2 PDE4B_HUMAN Decreases Activity [11]
Voltage-dependent L-type calcium channel subunit alpha-1C (CACNA1C) OT6KFNMS CAC1C_HUMAN Decreases Activity [11]
Aurora kinase B (AURKB) OTIY4VHU AURKB_HUMAN Decreases Activity [11]
NF-kappa-B inhibitor epsilon (NFKBIE) OTLAYEL9 IKBE_HUMAN Increases Expression [8]
Transcription factor MafG (MAFG) OTBQFUZH MAFG_HUMAN Decreases Expression [8]
SH3 domain-binding protein 5 (SH3BP5) OTOOEGUJ 3BP5_HUMAN Affects Expression [12]
Dynamin-like 120 kDa protein, mitochondrial (OPA1) OTJGNWPW OPA1_HUMAN Increases Cleavage [13]
Mitofusin-2 (MFN2) OTPYN8A3 MFN2_HUMAN Decreases Expression [13]
Urokinase-type plasminogen activator (PLAU) OTX0QGKK UROK_HUMAN Increases Expression [8]
Platelet-derived growth factor subunit B (PDGFB) OTMFMFC3 PDGFB_HUMAN Increases Expression [8]
Annexin A1 (ANXA1) OT5OFDJC ANXA1_HUMAN Affects Expression [12]
Endothelin-1 (EDN1) OTZCACEG EDN1_HUMAN Increases Expression [8]
Amino acid transporter heavy chain SLC3A2 (SLC3A2) OTBR33M9 4F2_HUMAN Decreases Expression [8]
ATP-dependent 6-phosphofructokinase, muscle type (PFKM) OT1QY9JM PFKAM_HUMAN Decreases Expression [13]
Glutathione S-transferase A1 (GSTA1) OTA7K5XA GSTA1_HUMAN Decreases Expression [12]
Glutathione S-transferase P (GSTP1) OTLP0A0Y GSTP1_HUMAN Increases Expression [12]
Growth-regulated alpha protein (CXCL1) OT3WCTZV GROA_HUMAN Increases Expression [8]
Heme oxygenase 1 (HMOX1) OTC1W6UX HMOX1_HUMAN Decreases Expression [8]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Increases Cleavage [14]
Retinoic acid receptor alpha (RARA) OT192V9V RARA_HUMAN Affects Expression [12]
Endoplasmic reticulum chaperone BiP (HSPA5) OTFUIRAO BIP_HUMAN Increases Expression [8]
C-C motif chemokine 2 (CCL2) OTAD2HEL CCL2_HUMAN Increases Expression [8]
Pyruvate kinase PKM (PKM) OTLHHMC2 KPYM_HUMAN Decreases Expression [13]
Interleukin-1 receptor type 1 (IL1R1) OTTU8959 IL1R1_HUMAN Affects Expression [12]
Beta-1,4-galactosyltransferase 1 (B4GALT1) OTBCXEK7 B4GT1_HUMAN Increases Expression [8]
NAD(P)H dehydrogenase 1 (NQO1) OTZGGIVK NQO1_HUMAN Decreases Expression [8]
Glutathione peroxidase 2 (GPX2) OTXI2NTI GPX2_HUMAN Affects Expression [12]
C-X-C motif chemokine 2 (CXCL2) OTEJCYMY CXCL2_HUMAN Increases Expression [8]
Tumor necrosis factor alpha-induced protein 3 (TNFAIP3) OTVLI4DD TNAP3_HUMAN Increases Expression [8]
Ribosomal protein S6 kinase beta-1 (RPS6KB1) OTAELNGX KS6B1_HUMAN Decreases Phosphorylation [13]
Growth arrest and DNA damage-inducible protein GADD45 alpha (GADD45A) OTDRV63V GA45A_HUMAN Affects Expression [12]
DnaJ homolog subfamily B member 1 (DNAJB1) OTCOSEVH DNJB1_HUMAN Affects Expression [12]
DNA damage-inducible transcript 3 protein (DDIT3) OTI8YKKE DDIT3_HUMAN Increases Expression [8]
Lon protease homolog, mitochondrial (LONP1) OT665WYT LONM_HUMAN Decreases Expression [15]
Signal transducer and activator of transcription 3 (STAT3) OTAAGKYZ STAT3_HUMAN Decreases Phosphorylation [14]
Serine/threonine-protein kinase mTOR (MTOR) OTHH8KU7 MTOR_HUMAN Decreases Phosphorylation [13]
Glutamate--cysteine ligase catalytic subunit (GCLC) OTESDI4D GSH1_HUMAN Decreases Expression [8]
Glutamate--cysteine ligase regulatory subunit (GCLM) OT6CP234 GSH0_HUMAN Decreases Expression [8]
Fatty acid synthase (FASN) OTFII9KG FAS_HUMAN Decreases Expression [16]
Small ribosomal subunit protein eS6 (RPS6) OTT4D1LN RS6_HUMAN Decreases Expression [13]
Oxidized low-density lipoprotein receptor 1 (OLR1) OTS44RIC OLR1_HUMAN Increases Expression [8]
C-C motif chemokine 20 (CCL20) OTUCJY4N CCL20_HUMAN Increases Expression [8]
Heat shock factor protein 1 (HSF1) OTYNJ4KP HSF1_HUMAN Increases Activity [17]
Antigen peptide transporter 1 (TAP1) OTJL27PW TAP1_HUMAN Increases Expression [8]
Tumor necrosis factor receptor superfamily member 9 (TNFRSF9) OTNOM26L TNR9_HUMAN Increases Expression [8]
Baculoviral IAP repeat-containing protein 3 (BIRC3) OT3E95KB BIRC3_HUMAN Increases Expression [8]
Sequestosome-1 (SQSTM1) OTGY5D5J SQSTM_HUMAN Decreases Expression [8]
Kelch-like ECH-associated protein 1 (KEAP1) OTFHOD0C KEAP1_HUMAN Decreases Expression [8]
Neutral amino acid transporter B(0) (SLC1A5) OTE2H26Q AAAT_HUMAN Decreases Expression [13]
Mitofusin-1 (MFN1) OTCBXQZF MFN1_HUMAN Decreases Expression [13]
Scavenger receptor class B member 1 (SCARB1) OTAE1UA1 SCRB1_HUMAN Affects Expression [12]
Thyroid hormone-inducible hepatic protein (THRSP) OTKYE01L THRSP_HUMAN Decreases Expression [16]
Multidrug and toxin extrusion protein 1 (SLC47A1) OTZX0U5Q S47A1_HUMAN Increases Expression [18]
Bcl-2-binding component 3, isoforms 3/4 (BBC3) OTUAXDAY BBC3B_HUMAN Increases Expression [8]
Tribbles homolog 3 (TRIB3) OTG5OS7X TRIB3_HUMAN Decreases Expression [8]
Sigma non-opioid intracellular receptor 1 (SIGMAR1) OTDORW5C SGMR1_HUMAN Decreases Expression [15]
Sulfiredoxin-1 (SRXN1) OTYDBO4L SRXN1_HUMAN Decreases Expression [8]
Prolyl hydroxylase EGLN3 (EGLN3) OTXV3RYX EGLN3_HUMAN Affects Expression [12]
5'-AMP-activated protein kinase subunit gamma-2 (PRKAG2) OTHTAM54 AAKG2_HUMAN Affects Expression [8]
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⏷ Show the Full List of 75 DOT(s)

References

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11 Characterization of the potent, selective Nrf2 activator, 3-(pyridin-3-ylsulfonyl)-5-(trifluoromethyl)-2H-chromen-2-one, in cellular and in vivo models of pulmonary oxidative stress. J Pharmacol Exp Ther. 2017 Oct;363(1):114-125.
12 Fluorescent tagging of endogenous Heme oxygenase-1 in human induced pluripotent stem cells for high content imaging of oxidative stress in various differentiated lineages. Arch Toxicol. 2021 Oct;95(10):3285-3302. doi: 10.1007/s00204-021-03127-8. Epub 2021 Sep 4.
13 Synthetic oleanane triterpenoid derivative CDDO-Me disrupts cellular bioenergetics to suppress pancreatic ductal adenocarcinoma via targeting SLC1A5. J Biochem Mol Toxicol. 2022 Nov;36(11):e23192. doi: 10.1002/jbt.23192. Epub 2022 Aug 5.
14 The synthetic triterpenoids CDDO-methyl ester and CDDO-ethyl amide prevent lung cancer induced by vinyl carbamate in A/J mice. Cancer Res. 2007 Mar 15;67(6):2414-9. doi: 10.1158/0008-5472.CAN-06-4534.
15 Lonp1 and Sig-1R contribute to the counteraction of ursolic acid against ochratoxin A-induced mitochondrial apoptosis. Food Chem Toxicol. 2023 Feb;172:113592. doi: 10.1016/j.fct.2022.113592. Epub 2022 Dec 29.
16 Fatty acid synthesis is a therapeutic target in human liposarcoma. Int J Oncol. 2010 May;36(5):1309-14. doi: 10.3892/ijo_00000616.
17 A Gene Expression Biomarker Predicts Heat Shock Factor 1 Activation in a Gene Expression Compendium. Chem Res Toxicol. 2021 Jul 19;34(7):1721-1737. doi: 10.1021/acs.chemrestox.0c00510. Epub 2021 Jun 25.
18 Bardoxolone methyl modulates efflux transporter and detoxifying enzyme expression in cisplatin-induced kidney cell injury. Toxicol Lett. 2016 Sep 30;259:52-59. doi: 10.1016/j.toxlet.2016.07.021. Epub 2016 Jul 29.