General Information of Drug (ID: DMMOFKD)

Drug Name
NU-6102 Drug Info
Synonyms
nu6102; 444722-95-6; NU 6102; O6-CYCLOHEXYLMETHOXY-2-(4'-SULPHAMOYLANILINO) PURINE; Cdk1/2 Inhibitor II, NU6102; 6-Cyclohexylmethoxy-2-(4& -sulfamoylanilino)purine; 4-{[6-(cyclohexylmethoxy)-9H-purin-2-yl]amino}benzenesulfonamide; 4SP; 1h1s; 4-[[6-(cyclohexylmethoxy)-7H-purin-2-yl]amino]benzenesulfonamide; 4-{[6-(cyclohexylmethoxy)-7h-purin-2-yl]amino}benzenesulfonamide; 4-[[6-(cyclohexylmethoxy)-9h-purin-2-yl]amino]benzenesulfonamide; 4eor; 4eok; 2iw9; 2c6o; 2iw8; AC1L1IGA; SCHEMBL2170816; CHEMBL319467
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
4566
CAS Number
CAS 444722-95-6
TTD Drug ID
DMMOFKD

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Investigative Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Approved Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
(Z)-3-((1H-pyrrol-2-yl)methylene)indolin-2-one DM27WDP Discovery agent N.A. Investigative [3]
BX-517 DMBQIEF Discovery agent N.A. Investigative [3]
ISIS 29475 DMEBQUN Discovery agent N.A. Investigative [4]
ISIS 29233 DMGV4O7 Discovery agent N.A. Investigative [4]
ISIS 29471 DMG4RMZ Discovery agent N.A. Investigative [4]
ISIS 29470 DMPCK7Y Discovery agent N.A. Investigative [4]
ISIS 29477 DMKQMXV Discovery agent N.A. Investigative [4]
ISIS 29239 DMHQF1J Discovery agent N.A. Investigative [4]
SU-6689 DMDNA23 Discovery agent N.A. Investigative [3]
ISIS 29257 DMUM2H1 Discovery agent N.A. Investigative [4]
⏷ 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 [5]
UCN-01 DMUNJZB Non-small-cell lung cancer 2C25.Y Phase 2 [6]
SCH-900776 DM67EMK Solid tumour/cancer 2A00-2F9Z Phase 2 [7]
LY2606368 DM4XMF7 Ovarian cancer 2C73 Phase 2 [8]
LY2880070 DMADEHZ Solid tumour/cancer 2A00-2F9Z Phase 1/2 [9]
RG7741 DMK6P9J Lymphoma 2A80-2A86 Phase 1 [10]
GDC-0425 DMDZ26X Lymphoma 2A80-2A86 Phase 1 [11]
AZD7762 DM1FW0C Solid tumour/cancer 2A00-2F9Z Phase 1 [12]
MK-8776 DMAS1RB Hodgkin lymphoma 2B30 Phase 1 [13]
Diamidothiazole derivative 1 DM02V5Q N. A. N. A. Patented [14]
⏷ 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 [15]
Ro 31-7453 DM83QCL Solid tumour/cancer 2A00-2F9Z Phase 2 [16]
PHA848125 DMS2Q9G Thymic cancer 2C27 Phase 2 [17]
TG02 DMZFIGQ Anaplastic astrocytoma 2A00.0 Phase 1/2 [18]
NUV-422 DMQJQNT Malignant glioma 2A00.0 Phase 1/2 [19]
RGB-286638 DMEGOQP Haematological malignancy 2B33.Y Phase 1 [20]
FN-1501 DM7BMD6 Solid tumour/cancer 2A00-2F9Z Phase 1 [21]
AG-024322 DMY4WVK Solid tumour/cancer 2A00-2F9Z Phase 1 [15]
PHA-793887 DM2Y4FG Solid tumour/cancer 2A00-2F9Z Phase 1 [22]
SNS-032 DMEITAS Solid tumour/cancer 2A00-2F9Z Phase 1 [23]
⏷ 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 [24]
LY2090314 DMTBFE4 Acute myeloid leukaemia 2A60 Phase 2 [25]
Lithium DMZ3OU6 Bipolar disorder 6A60 Phase 2 [26]
Tideglusib DME4LA1 Alzheimer disease 8A20 Phase 2 [27]
9-ING-41 DM57TY3 Myelofibrosis 2A20.2 Phase 2 [28]
Neu-120 DMXKOUC Parkinson disease 8A00.0 Phase 1/2 [29]
KENPAULLONE DMAGVXW Discovery agent N.A. Patented [30]
CHIR-99021 DMB8MNU Allergic inflammation 4A80-4A85 Patented [31]
TDZD-8 DMG6Q45 Malignant glioma 2A00.0 Patented [32]
AR-A014418 DMUPN01 Ovarian cancer 2C73 Patented [33]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Apremilast DMTWS9E Psoriasis vulgaris EA90 Approved [34]
LY2835219 DM93VBZ Breast cancer 2C60-2C65 Approved [35]
Palbociclib DMD7L94 Breast cancer 2C60-2C65 Approved [36]
Ribociclib Succinate DM9CIUW Breast cancer 2C60-2C65 Approved [37]
Trilaciclib DMP5A4T Small-cell lung cancer 2C25.Y Approved [38]
LEE011 DMMX75K Breast cancer 2C60-2C65 Phase 3 [39]
Ro 31-7453 DM83QCL Solid tumour/cancer 2A00-2F9Z Phase 2 [16]
P276-00 DM9DJL2 Mantle cell lymphoma 2A85.5 Phase 2 [15]
P-276 DMMJUHD Breast cancer 2C60-2C65 Phase 2 [40]
G1T38 DMQO2IT Breast cancer 2C60-2C65 Phase 2 [8]
⏷ 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 [1]
Cyclin-dependent kinase 4 (CDK4) TT0PG8F CDK4_HUMAN Inhibitor [1]
Glycogen synthase kinase-3 beta (GSK-3B) TTRSMW9 GSK3B_HUMAN Inhibitor [2]
PDK-1 messenger RNA (PDK-1 mRNA) TTYMGWX PDPK1_HUMAN Inhibitor [2]

References

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2 Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1353-7.
3 Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3814-8.
4 US patent application no. 6,124,272, Antisense modulation of PDK-1 expression.
5 Characterization and preclinical development of LY2603618: a selective and potent Chk1 inhibitor. Invest New Drugs. 2014 Apr;32(2):213-26.
6 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.
7 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.
8 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
9 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.
10 National Cancer Institute Drug Dictionary (drug id 730054).
11 Quantitative assessment of BCL-2:BIM complexes as a pharmacodynamic marker for venetoclax (ABT-199).
12 Clinical pipeline report, company report or official report of AstraZeneca (2009).
13 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.
14 Cyclin-dependent kinase inhibitors for cancer therapy: a patent review (2009 - 2014).Expert Opin Ther Pat. 2015;25(9):953-70.
15 Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
16 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.
17 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.
18 Preclinical metabolism and pharmacokinetics of SB1317 (TG02), a potent CDK/JAK2/FLT3 inhibitor. Drug Metab Lett. 2012 Mar;6(1):33-42.
19 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.
20 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.
21 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.
22 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.
23 Mechanism of action of SNS-032, a novel cyclin-dependent kinase inhibitor, in chronic lymphocytic leukemia. Blood. 2009 May 7;113(19):4637-45.
24 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
25 Glycogen synthase kinase 3 (GSK-3) inhibitors: a patent update (2014-2015).Expert Opin Ther Pat. 2017 Jun;27(6):657-666.
26 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.
27 Evidence for irreversible inhibition of glycogen synthase kinase-3beta by tideglusib. J Biol Chem. 2012 Jan 6;287(2):893-904.
28 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.
29 Company report (Neurim Pharmaceuticals)
30 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta. Bioorg Med Chem Lett. 2004 Jan 19;14(2):413-6.
31 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.
32 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.
33 Fragment and knowledge-based design of selective GSK-3beta inhibitors using virtual screening models. Eur J Med Chem. 2009 Jun;44(6):2361-71.
34 Agreement signed with Prostagenics to develop prostate cancer treatment. Innovate Oncology, Inc. 2005.
35 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
36 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2017
37 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
38 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2021
39 Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma. Clin Cancer Res. 2013 Nov 15;19(22):6173-82.
40 Liposarcoma: molecular genetics and therapeutics. Sarcoma. 2011;2011:483154.