General Information of Drug (ID: DM0CSH8)

Drug Name
2-(1H-indazol-3-yl)-1H-benzo[d]imidazole Drug Info
Synonyms
3-(1H-BENZIMIDAZOL-2-YL)-1H-INDAZOLE; CHEMBL383990; 3-(1H-1,3-benzodiazol-2-yl)-2H-indazole; 2-(2H-indazol-3-yl)-1H-1,3-benzodiazole; IDZ; 1097816-83-5; Indazole Compound 2; 2c3l; AC1Q4XAS; AC1NS1P1; SCHEMBL311148; BDBM16590; 3-benzimidazol-2-yl-1h-indazole; JTKFRFMSUBOCIQ-UHFFFAOYSA-N; MolPort-016-542-829; ZINC14961821; AKOS009356321; NE25942; MCULE-6782886882; DB07959; 2-(1H-indazol-3-yl)-1H-benzimidazole; 3-(1H-benzoimidazol-2-yl)-1H-indazole; 2-(1H-Indazole-3-yl)-1H-benzoimidazole; EN300-70692
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
135464491
TTD Drug ID
DM0CSH8

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Investigative Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [3]
Intedanib DMSTA36 Colorectal cancer 2B91.Z Approved [4]
Pemigatinib DM819JF Cholangiocarcinoma 2C12.10 Approved [5]
Infigratinib DMNKBEC Cholangiocarcinoma 2C12.10 Approved [6]
E-3810 DM42PFT Solid tumour/cancer 2A00-2F9Z Phase 3 [7]
Sulfatinib DMPOTM4 Neuroendocrine cancer 2B72.1 Phase 3 [8]
ARQ-087 DM02BVQ Intrahepatic cholangiocarcinoma 2C12.10 Phase 3 [9]
AZD4547 DM3827C Solid tumour/cancer 2A00-2F9Z Phase 2/3 [10]
Debio 1347 DMZW50O Solid tumour/cancer 2A00-2F9Z Phase 2 [11]
AM-001 DMGVQI8 Actinic keratosis EK90.0 Phase 2 [12]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [13]
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [14]
Becaplermin DM1R5X4 Diabetic complication 5A2Y Approved [15]
E-3810 DM42PFT Solid tumour/cancer 2A00-2F9Z Phase 3 [7]
Famitinib DMSFWT7 Solid tumour/cancer 2A00-2F9Z Phase 2 [16]
XL-820 DMMHX9K Solid tumour/cancer 2A00-2F9Z Phase 2 [17]
MK-2461 DM21WBH Alzheimer disease 8A20 Phase 1/2 [18]
SNN-0031 DM2X3BR Brain injury NA07.Z Phase 1/2 [19]
TAK-593 DMNFZOT Solid tumour/cancer 2A00-2F9Z Phase 1 [20]
Pyridine derivative 18 DMBZMYT N. A. N. A. Patented [21]
⏷ Show the Full List of 10 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 [22]
UCN-01 DMUNJZB Non-small-cell lung cancer 2C25.Y Phase 2 [23]
SCH-900776 DM67EMK Solid tumour/cancer 2A00-2F9Z Phase 2 [24]
LY2606368 DM4XMF7 Ovarian cancer 2C73 Phase 2 [11]
LY2880070 DMADEHZ Solid tumour/cancer 2A00-2F9Z Phase 1/2 [25]
RG7741 DMK6P9J Lymphoma 2A80-2A86 Phase 1 [26]
GDC-0425 DMDZ26X Lymphoma 2A80-2A86 Phase 1 [27]
AZD7762 DM1FW0C Solid tumour/cancer 2A00-2F9Z Phase 1 [28]
MK-8776 DMAS1RB Hodgkin lymphoma 2B30 Phase 1 [29]
Diamidothiazole derivative 1 DM02V5Q N. A. N. A. Patented [30]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [31]
VATALANIB DMY0UEQ Solid tumour/cancer 2A00-2F9Z Phase 2 [32]
MK-2461 DM21WBH Alzheimer disease 8A20 Phase 1/2 [18]
Sirna-027 DMZTQD8 Exudative age-related macular degeneration 9B78.3Z Phase 1/2 [33]
PMID22765894C8h DMH5RFU Discovery agent N.A. Investigative [34]
AAL-993 DM35RFH Discovery agent N.A. Investigative [32]
PMID17935989C25 DML8ZBR Discovery agent N.A. Investigative [35]
2-(5-Phenyl-oxazol-2-ylamino)-benzonitrile DMX6QMT Discovery agent N.A. Investigative [36]
4-Chloro-N-(3-chloro-benzoyl)-benzenesulfonamide DMI3OR9 Discovery agent N.A. Investigative [37]
(2-Methoxy-phenyl)-(5-phenyl-oxazol-2-yl)-amine DMQWD75 Discovery agent N.A. Investigative [36]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [13]
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [3]
Regorafenib DMHSY1I Gastrointestinal stromal tumour 2B5B Approved [38]
Sunitinib DMCBJSR Acute undifferentiated leukemia Approved [39]
Axitinib DMGVH6N Renal cell carcinoma 2C90 Approved [40]
Vandetanib DMRICNP Solid tumour/cancer 2A00-2F9Z Approved [41]
Pazopanib HCl DM6U9CQ Renal cell carcinoma 2C90 Approved [42]
Fruquintinib DMHOSCQ Colorectal cancer 2B91.Z Approved [43]
Cabozantinib DMIYDT4 Medullary thyroid gland carcinoma Approved [44]
Tivozanib DMUKC5L Renal cell carcinoma 2C90 Approved [45]
⏷ 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 [1]
Fibroblast growth factor receptor 1 (FGFR1) TTRLW2X FGFR1_HUMAN Inhibitor [2]
Platelet-derived growth factor receptor beta (PDGFRB) TTI7421 PGFRB_HUMAN Inhibitor [2]
Vascular endothelial growth factor receptor 2 (KDR) TTUTJGQ VGFR2_HUMAN Inhibitor [2]
VEGFR1 messenger RNA (VEGFR1 mRNA) TT1VAUK VGFR1_HUMAN Inhibitor [2]

References

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2 Design and structure-activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3595-9.
3 Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
4 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
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6 Pharmacological inhibition of fibroblast growth factor (FGF) receptor signaling ameliorates FGF23-mediated hypophosphatemic rickets. J Bone Miner Res. 2013 Apr;28(4):899-911.
7 E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405.
8 Clinical pipeline report, company report or official report of Hutchison Medi Pharma.
9 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: 1808).
10 AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res. 2012 Apr 15;72(8):2045-56.
11 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
12 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029917)
13 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.
14 Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel... J Med Chem. 2003 Mar 27;46(7):1116-9.
15 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
16 Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
17 National Cancer Institute Drug Dictionary (drug id 452042).
18 MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
19 Company report (Neuronova)
20 Biochemical characterization of TAK-593, a novel VEGFR/PDGFR inhibitor with a two-step slow binding mechanism. Biochemistry. 2011 Feb 8;50(5):738-51.
21 RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99.
22 Characterization and preclinical development of LY2603618: a selective and potent Chk1 inhibitor. Invest New Drugs. 2014 Apr;32(2):213-26.
23 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.
24 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.
25 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.
26 National Cancer Institute Drug Dictionary (drug id 730054).
27 Quantitative assessment of BCL-2:BIM complexes as a pharmacodynamic marker for venetoclax (ABT-199).
28 Clinical pipeline report, company report or official report of AstraZeneca (2009).
29 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.
30 Cyclin-dependent kinase inhibitors for cancer therapy: a patent review (2009 - 2014).Expert Opin Ther Pat. 2015;25(9):953-70.
31 New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven a... J Med Chem. 2000 Jun 15;43(12):2310-23.
32 Inhibitors of VEGF receptors-1 and -2 based on the 2-((pyridin-4-yl)ethyl)pyridine template. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1913-9.
33 2011 Pipeline of Sirna Therapeutics.
34 The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4979-85.
35 Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and prelimina... Bioorg Med Chem Lett. 2007 Dec 1;17(23):6593-601.
36 Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors. J Med Chem. 2005 Mar 10;48(5):1610-9.
37 Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents. J Med Chem. 2004 Oct 21;47(22):5367-80.
38 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
39 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
40 Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
41 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.
42 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
43 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.
44 Clinical pipeline report, company report or official report of Exelixis (2011).
45 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services