General Information of Drug (ID: DMZA45C)

Drug Name
BX-912 Drug Info
Synonyms BX 912; BX912
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
11754511
ChEBI ID
CHEBI:91357
CAS Number
CAS 702674-56-4
TTD Drug ID
DMZA45C

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Clinical Trial Drug(s)
Investigative Drug(s)
Patented Agent(s)
Approved Drug(s)
Discontinued Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
AR-12 DM4RK6P Lymphoma 2A80-2A86 Phase 1 [3]
L-serine-O-phosphate DMTJ1NH Discovery agent N.A. Investigative [4]
PMID20005102C1 DMMESBW Discovery agent N.A. Investigative [5]
BX-795 DMRIMLJ Discovery agent N.A. Investigative [2]
PHT-427 DMI96Y3 Discovery agent N.A. Investigative [6]
PF-5177624 DMUOFT0 Solid tumour/cancer 2A00-2F9Z Investigative [7]
GSK-2334470 DM3BI7R Solid tumour/cancer 2A00-2F9Z Investigative [8]
⏷ Show the Full List of 7 Drug(s)
Drug(s) Targeting Checkpoint kinase-1 (CHK1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
LY2603618 DMCXRZF Pancreatic cancer 2C10 Phase 2 [9]
UCN-01 DMUNJZB Non-small-cell lung cancer 2C25.Y Phase 2 [10]
SCH-900776 DM67EMK Solid tumour/cancer 2A00-2F9Z Phase 2 [11]
LY2606368 DM4XMF7 Ovarian cancer 2C73 Phase 2 [12]
LY2880070 DMADEHZ Solid tumour/cancer 2A00-2F9Z Phase 1/2 [13]
RG7741 DMK6P9J Lymphoma 2A80-2A86 Phase 1 [14]
GDC-0425 DMDZ26X Lymphoma 2A80-2A86 Phase 1 [15]
AZD7762 DM1FW0C Solid tumour/cancer 2A00-2F9Z Phase 1 [16]
MK-8776 DMAS1RB Hodgkin lymphoma 2B30 Phase 1 [17]
Diamidothiazole derivative 1 DM02V5Q N. A. N. A. Patented [18]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
R-roscovitine DMSH108 Non-small-cell lung cancer 2C25.Y Phase 2 [19]
Ro 31-7453 DM83QCL Solid tumour/cancer 2A00-2F9Z Phase 2 [20]
PHA848125 DMS2Q9G Thymic cancer 2C27 Phase 2 [21]
TG02 DMZFIGQ Anaplastic astrocytoma 2A00.0 Phase 1/2 [22]
NUV-422 DMQJQNT Malignant glioma 2A00.0 Phase 1/2 [23]
RGB-286638 DMEGOQP Haematological malignancy 2B33.Y Phase 1 [24]
FN-1501 DM7BMD6 Solid tumour/cancer 2A00-2F9Z Phase 1 [25]
AG-024322 DMY4WVK Solid tumour/cancer 2A00-2F9Z Phase 1 [19]
PHA-793887 DM2Y4FG Solid tumour/cancer 2A00-2F9Z Phase 1 [26]
SNS-032 DMEITAS Solid tumour/cancer 2A00-2F9Z Phase 1 [27]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
AMO-02 DMJRU3A Myotonic dystrophy 8C71.0 Phase 2/3 [28]
LY2090314 DMTBFE4 Acute myeloid leukaemia 2A60 Phase 2 [29]
Lithium DMZ3OU6 Bipolar disorder 6A60 Phase 2 [30]
Tideglusib DME4LA1 Alzheimer disease 8A20 Phase 2 [31]
9-ING-41 DM57TY3 Myelofibrosis 2A20.2 Phase 2 [32]
Neu-120 DMXKOUC Parkinson disease 8A00.0 Phase 1/2 [33]
KENPAULLONE DMAGVXW Discovery agent N.A. Patented [34]
CHIR-99021 DMB8MNU Allergic inflammation 4A80-4A85 Patented [35]
TDZD-8 DMG6Q45 Malignant glioma 2A00.0 Patented [36]
AR-A014418 DMUPN01 Ovarian cancer 2C73 Patented [37]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [38]
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [39]
Regorafenib DMHSY1I Gastrointestinal stromal tumour 2B5B Approved [40]
Sunitinib DMCBJSR Acute undifferentiated leukemia Approved [41]
Axitinib DMGVH6N Renal cell carcinoma 2C90 Approved [42]
Vandetanib DMRICNP Solid tumour/cancer 2A00-2F9Z Approved [20]
Pazopanib HCl DM6U9CQ Renal cell carcinoma 2C90 Approved [43]
Fruquintinib DMHOSCQ Colorectal cancer 2B91.Z Approved [44]
Cabozantinib DMIYDT4 Medullary thyroid gland carcinoma Approved [45]
Tivozanib DMUKC5L Renal cell carcinoma 2C90 Approved [46]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
BALANOL DMDLN9E N. A. N. A. Terminated [47]
4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol DMSKJ1X Discovery agent N.A. Investigative [48]
Ro-4396686 DM5DMCH Discovery agent N.A. Investigative [49]
PMID20005102C1 DMMESBW Discovery agent N.A. Investigative [5]
[3H]cAMP DMZRQU7 Discovery agent N.A. Investigative [50]
PMID19364658C33 DMSE1C3 Discovery agent N.A. Investigative [51]
BX-795 DMRIMLJ Discovery agent N.A. Investigative [2]
chelerythrine DMCP1G9 Discovery agent N.A. Investigative [52]
PMID21742770C1 DME3JMH Discovery agent N.A. Investigative [53]
Rp-adenosine 3',5'-cyclic monophosphothioate triethylamine (Rp-cAMPS) DM1JWGH Discovery agent N.A. Investigative [54]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Checkpoint kinase-1 (CHK1) TTTU902 CHK1_HUMAN Inhibitor [2]
Cyclin-dependent kinase 2 (CDK2) TT7HF4W CDK2_HUMAN Inhibitor [2]
Fungal Protein kinase A (Fung ypkA) TTYVI76 Q56921_YEREN Inhibitor [2]
Glycogen synthase kinase-3 beta (GSK-3B) TTRSMW9 GSK3B_HUMAN Inhibitor [2]
Phosphoinositide dependent protein kinase-1 (PDPK1) TT9QBI6 PDPK1_HUMAN Inhibitor [2]
Vascular endothelial growth factor receptor 2 (KDR) TTUTJGQ VGFR2_HUMAN Inhibitor [2]

References

1 Role of Akt signaling in vascular homeostasis and angiogenesis. Circ Res. 2002 Jun 28;90(12):1243-50.
2 Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74.
3 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
4 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
5 2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles. Bioorg Med Chem Lett. 2010 Jan 15;20(2):679-83.
6 Molecular pharmacology and antitumor activity of PHT-427, a novel Akt/phosphatidylinositide-dependent protein kinase 1 pleckstrin homology domain inhibitor. Mol Cancer Ther. 2010 Mar;9(3):706-17.
7 Targeting 3-phosphoinoside-dependent kinase-1 to inhibit insulin-like growth factor-I induced AKT and p70 S6 kinase activation in breast cancer cells. PLoS One. 2012;7(10):e48402.
8 Genetic inactivation or pharmacological inhibition of Pdk1 delays development and inhibits metastasis of Braf(V600E)::Pten(-/-) melanoma. Oncogene. 2014 Aug 21;33(34):4330-9.
9 Characterization and preclinical development of LY2603618: a selective and potent Chk1 inhibitor. Invest New Drugs. 2014 Apr;32(2):213-26.
10 Characterization of an inhibitory dynamic pharmacophore for the ERCC1-XPA interaction using a combined molecular dynamics and virtual screening app... J Mol Graph Model. 2009 Sep;28(2):113-30.
11 Targeting the replication checkpoint using SCH 900776, a potent and functionally selective CHK1 inhibitor identified via high content screening. Mol Cancer Ther. 2011 Apr;10(4):591-602.
12 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
13 A phase Ib study of oral Chk1 inhibitor LY2880070 in combination with gemcitabine in patients with advanced or metastatic cancer. Journal of Clinical Oncology 38, no. 15_suppl (May 20, 2020) 3581-3581.
14 National Cancer Institute Drug Dictionary (drug id 730054).
15 Quantitative assessment of BCL-2:BIM complexes as a pharmacodynamic marker for venetoclax (ABT-199).
16 Clinical pipeline report, company report or official report of AstraZeneca (2009).
17 Chk1 Inhibitor MK-8776 Restores the Sensitivity of Chemotherapeutics in P-glycoprotein Overexpressing Cancer Cells. Int J Mol Sci. 2019 Aug 22;20(17):4095.
18 Cyclin-dependent kinase inhibitors for cancer therapy: a patent review (2009 - 2014).Expert Opin Ther Pat. 2015;25(9):953-70.
19 Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
20 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.
21 Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor. J Med Chem. 2009 Aug 27;52(16):5152-63.
22 Preclinical metabolism and pharmacokinetics of SB1317 (TG02), a potent CDK/JAK2/FLT3 inhibitor. Drug Metab Lett. 2012 Mar;6(1):33-42.
23 ClinicalTrials.gov (NCT04541225) Phase 1/2 Dose Escalation, Safety, Pharmacokinetics, and Efficacy Study of NUV-422 in Adults With Recurrent or Refractory High-grade Gliomas and Solid Tumors. U.S.National Institutes of Health.
24 Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs. Leukemia. 2013 Dec;27(12):2366-75.
25 Discovery of 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide (FN-1501), an FLT3- and CDK-Kinase Inhibitor with Potentially High Efficiency against Acute Myelocytic Leukemia. J Med Chem. 2018 Feb 22;61(4):1499-1518.
26 A first in man, phase I dose-escalation study of PHA-793887, an inhibitor of multiple cyclin-dependent kinases (CDK2, 1 and 4) reveals unexpected h... Cell Cycle. 2011 Mar 15;10(6):963-70.
27 Mechanism of action of SNS-032, a novel cyclin-dependent kinase inhibitor, in chronic lymphocytic leukemia. Blood. 2009 May 7;113(19):4637-45.
28 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
29 Glycogen synthase kinase 3 (GSK-3) inhibitors: a patent update (2014-2015).Expert Opin Ther Pat. 2017 Jun;27(6):657-666.
30 The GSK3 kinase inhibitor lithium produces unexpected hyperphosphorylation of -catenin, a GSK3 substrate, in human glioblastoma cells. Biol Open. 2018 Jan 26;7(1):bio030874.
31 Evidence for irreversible inhibition of glycogen synthase kinase-3beta by tideglusib. J Biol Chem. 2012 Jan 6;287(2):893-904.
32 9-ING-41, a small molecule inhibitor of GSK-3beta, potentiates the effects of anticancer therapeutics in bladder cancer. Sci Rep. 2019 Dec 27;9(1):19977.
33 Company report (Neurim Pharmaceuticals)
34 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta. Bioorg Med Chem Lett. 2004 Jan 19;14(2):413-6.
35 Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003 Mar;52(3):588-95.
36 Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3beta inhibitors through virtual screening. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7232-6.
37 Fragment and knowledge-based design of selective GSK-3beta inhibitors using virtual screening models. Eur J Med Chem. 2009 Jun;44(6):2361-71.
38 Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling.Mol Cancer Ther.2008 Oct;7(10):3129-40.
39 Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
40 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
41 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
42 Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
43 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
44 Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014;15(12):1635-45.
45 Clinical pipeline report, company report or official report of Exelixis (2011).
46 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services
47 Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry. J Med Chem. 2005 Sep 8;48(18):5613-38. Address;
48 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. J Med Chem. 2006 Nov 2;49(22):6500-9.
49 Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3.
50 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: 1694).
51 Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2). Bioorg Med Chem. 2009 May 1;17(9):3342-51.
52 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8.
53 A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells. ACS Med Chem Lett. 2012 Dec 13;3(12):1034-1038.
54 Inhibition of protein kinase A activity interferes with long-term, but not short-term, memory of conditioned taste aversions. Behav Neurosci. 2002 Dec;116(6):1070-4.