General Information of DTT (ID: TTH6V3D)

DTT Name Cyclin-dependent kinase 1 (CDK1) DTT Info
UniProt ID
CDK1_HUMAN
Gene Name CDK1

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Patented Agent(s)
Clinical Trial Drug(s)
Investigative Drug(s)
Discontinued Drug(s)
Preclinical Drug(s)
7 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
P-276 DMMJUHD Breast cancer 2C60-2C65 Phase 2 [1]
P276-00 DM9DJL2 Mantle cell lymphoma 2A85.5 Phase 2 [2]
R-roscovitine DMSH108 Non-small-cell lung cancer 2C25.Y Phase 2 [2]
Ro 31-7453 DM83QCL Solid tumour/cancer 2A00-2F9Z Phase 2 [3]
AG-024322 DMY4WVK Solid tumour/cancer 2A00-2F9Z Phase 1 [2]
PHA-793887 DM2Y4FG Solid tumour/cancer 2A00-2F9Z Phase 1 [4]
RGB-286638 DMEGOQP Haematological malignancy 2B33.Y Phase 1 [5]
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⏷ Show the Full List of 7 Clinical Trial Drug(s)
13 Patented Agent(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
4-(thiazol-5-yl)-pyrimidine derivative 2 DMMQFCN N. A. N. A. Patented [6]
CHIR-99021 DMB8MNU Allergic inflammation 4A80-4A85 Patented [7]
Indole-based analog 13 DMV7DFM N. A. N. A. Patented [6]
Isoquinoline 1,3-dione derivative 1 DMIYUAN N. A. N. A. Patented [6]
KENPAULLONE DMAGVXW Discovery agent N.A. Patented [8]
Naphthyridine and isoquinoline derivative 1 DMTGIP7 N. A. N. A. Patented [6]
Oxazolyl methylthiothiazole derivative 1 DMZM6FW N. A. N. A. Patented [6]
PMID25991433-Compound-A1 DM89LF0 N. A. N. A. Patented [9]
Pyrazolo[1,5-a]-1,3,5-triazine derivative 1 DMOK7CW N. A. N. A. Patented [6]
Pyrrolo[2,3-d]pyrimidine derivative 10 DMRWG2E N. A. N. A. Patented [6]
Pyrrolo[2,3-d]pyrimidine derivative 9 DM0HU5O N. A. N. A. Patented [6]
Roscovitine derivative 1 DMD1G3Z N. A. N. A. Patented [6]
Tricyclic benzimidazole derivative 1 DM5SD9E N. A. N. A. Patented [6]
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⏷ Show the Full List of 13 Patented Agent(s)
6 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
SCH 727965 DMCJLD1 Acute lymphoblastic leukaemia 2A85 Discontinued in Phase 3 [2]
BAY 10-00394 DMV2DIW Small-cell lung cancer 2C25.Y Discontinued in Phase 2 [10]
R547 DMK25FU Advanced solid tumour 2A00-2F9Z Discontinued in Phase 1 [2]
ZK 304709 DMJ9R4A Advanced solid tumour 2A00-2F9Z Discontinued in Phase 1 [2]
CGP-60474 DM4TGY0 Solid tumour/cancer 2A00-2F9Z Terminated [13]
Olomoucine DMNAFG1 N. A. N. A. Terminated [14]
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⏷ Show the Full List of 6 Discontinued Drug(s)
2 Preclinical Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
L-751250 DMOERXK Obesity 5B81 Preclinical [11]
ON-01135 DMEXLU5 Solid tumour/cancer 2A00-2F9Z Preclinical [12]
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37 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
(2,6-Diamino-pyridin-3-yl)-phenyl-methanone DMWRCM1 Discovery agent N.A. Investigative [15]
10Z-Hymenialdisine DMIRSA5 Discovery agent N.A. Investigative [16]
2-(p-toluidino)-4-phenylpyrimidine-5-carbonitrile DM27YTF Discovery agent N.A. Investigative [17]
3,4-bis(indol-3-yl)maleimide derivative DMEQ1HC Discovery agent N.A. Investigative [18]
3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione DMDO175 Discovery agent N.A. Investigative [19]
3,4-diphenyl-1H-pyrrole-2,5-dione DMPK6YT Discovery agent N.A. Investigative [19]
3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione DMGC7RY Discovery agent N.A. Investigative [19]
3-(indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione DM3EV9N Discovery agent N.A. Investigative [19]
4-(Quinolin-3-yl)-N-p-tolylpyrimidin-2-amine DM4YFU5 Discovery agent N.A. Investigative [20]
4-(Quinolin-4-yl)-N-p-tolylpyrimidin-2-amine DMDW3SX Discovery agent N.A. Investigative [20]
4-phenyl-2-(phenylamino)pyrimidine-5-carbonitrile DMONKDQ Discovery agent N.A. Investigative [17]
9-Nitropaullone DM8LUYM Discovery agent N.A. Investigative [11]
aloisine A DM5U1LN Discovery agent N.A. Investigative [21]
alsterpaullone 2-cyanoethyl DMDI2KH Discovery agent N.A. Investigative [22]
aminopurvalanol A DMKLC3O N. A. N. A. Investigative [22]
AZAKENPAULLONE DM61H07 Discovery agent N.A. Investigative [23]
Bisindolylmaleimide-I DMOQJZC Discovery agent N.A. Investigative [18]
BMS-265246 DM6LPIG Discovery agent N.A. Investigative [24]
Cdk1 inhibitor DMNW12R Discovery agent N.A. Investigative [22]
Cdk1/2 inhibitor III DMS62T0 Discovery agent N.A. Investigative [25]
CGP74514A DMU5984 Discovery agent N.A. Investigative [26]
CVT-313 DMSEK5W Discovery agent N.A. Investigative [22]
IN1535 DMKFE6X Discovery agent N.A. Investigative [27]
Indirubin-3'-monoxime DMLRQH0 Discovery agent N.A. Investigative [28]
Indirubin-5-sulfonate DM08VHZ Discovery agent N.A. Investigative [29], [30]
JNJ-7706621 DMHTYBS Discovery agent N.A. Investigative [31]
K00024 DMP8M9Q Discovery agent N.A. Investigative [32]
Microxine DM7Y9AD Pain MG30-MG3Z Investigative [33]
NU6140 DMCUSG3 Discovery agent N.A. Investigative [34]
PF-228 DM32FKD Discovery agent N.A. Investigative [35]
PMID18986805C9b DMFU6AI Discovery agent N.A. Investigative [36]
PMID19115845C89S DMB9F2L Discovery agent N.A. Investigative [37]
Purvalanol A DMNQ7TM Discovery agent N.A. Investigative [11]
Quinoxaline1 DMRWXH4 Discovery agent N.A. Investigative [22]
RO-316233 DMAGLPW Discovery agent N.A. Investigative [18]
SU9516 DMQHG0R Discovery agent N.A. Investigative [38]
Thieno analogue of kenpaullone DMIOTHG Discovery agent N.A. Investigative [23]
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⏷ Show the Full List of 37 Investigative Drug(s)
Molecule Interaction Atlas

References

1 P276-00, a novel cyclin-dependent inhibitor induces G1-G2 arrest, shows antitumor activity on cisplatin-resistant cells and significant in vivo efficacy in tumor models. Mol Cancer Ther. 2007 Mar;6(3):926-34.
2 Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
3 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.
4 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.
5 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.
6 Cyclin-dependent kinase inhibitors for cancer therapy: a patent review (2009 - 2014).Expert Opin Ther Pat. 2015;25(9):953-70.
7 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.
8 Discovery of novel CDK1 inhibitors by combining pharmacophore modeling, QSAR analysis and in silico screening followed by in vitro bioassay. Eur J Med Chem. 2010 Sep;45(9):4316-30.
9 c-Jun N-terminal kinase inhibitors: a patent review (2010 - 2014).Expert Opin Ther Pat. 2015;25(8):849-72.
10 National Cancer Institute Drug Dictionary (drug id 770319).
11 Down-regulation of survivin in nitric oxide-induced cell growth inhibition and apoptosis of the human lung carcinoma cells. J Biol Chem. 2004 May 7;279(19):20267-76.
12 Phase 1 study of intravenous rigosertib (ON 01910.Na), a novel benzyl styryl sulfone structure producing G2/M arrest and apoptosis, in adult patients with advanced cancer. Am J Cancer Res. 2013; 3(3): 323-338.
13 Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors. J Med Chem. 2005 Mar 24;48(6):1886-900.
14 Antiproliferative activity of olomoucine II, a novel 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitor. Cell Mol Life Sci. 2005 Aug;62(15):1763-71.
15 3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: synthesis and biological evaluation. Bioorg Med Chem Lett. 2005 May 2;15(9):2221-4.
16 DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6.
17 4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: synthesis and biological evaluation. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3266-70.
18 Design of new inhibitors for cdc2 kinase based on a multiple pseudosubstrate structure. Bioorg Med Chem Lett. 1998 May 5;8(9):1019-22.
19 Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors. J Med Chem. 2006 Feb 23;49(4):1271-81.
20 Synthesis and cytotoxic activity of 2-methylimidazo[1,2-a]pyridine- and quinoline-substituted 2-aminopyrimidine derivatives. Eur J Med Chem. 2010 Jan;45(1):379-86.
21 Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects. J Med Chem. 2003 Jan 16;46(2):222-36.
22 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.
23 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta. Bioorg Med Chem Lett. 2004 Jan 19;14(2):413-6.
24 A robust high-content imaging approach for probing the mechanism of action and phenotypic outcomes of cell-cycle modulators. Mol Cancer Ther. 2011 Feb;10(2):242-54.
25 1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities. J Med Chem. 2005 Jun 30;48(13):4208-11.
26 2,6,9-trisubstituted purines: optimization towards highly potent and selective CDK1 inhibitors. Bioorg Med Chem Lett. 1999 Jan 4;9(1):91-6.
27 M-phase regulation of the recruitment of mRNAs onto polysomes using the CDK1/cyclin B inhibitor aminopurvalanol. Biochem Biophys Res Commun. 2003 Jul 11;306(4):880-6.
28 The kinase inhibitor indirubin-3'-oxime prevents germinal vesicle breakdown and reduces parthenogenetic development of pig oocytes. Theriogenology. 2006 Mar 1;65(4):744-56.
29 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
30 Binding of the potential antitumour agent indirubin-5-sulphonate at the inhibitor site of rabbit muscle glycogen phosphorylase b. Comparison with ligand binding to pCDK2-cyclin A complex. Eur J Biochem. 2004 Jun;271(11):2280-90.
31 Synthesis and evaluation of N-acyl sulfonamides as potential prodrugs of cyclin-dependent kinase inhibitor JNJ-7706621. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3639-41.
32 Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors. J Med Chem. 2003 May 22;46(11):2027-30.
33 Microxine, a new cdc2 kinase inhibitor from the Australian marine sponge Microxina species. J Nat Prod. 2001 Apr;64(4):525-6.
34 Potentiation of paclitaxel-induced apoptosis by the novel cyclin-dependent kinase inhibitor NU6140: a possible role for survivin down-regulation. Mol Cancer Ther. 2005 Sep;4(9):1328-37.
35 Cellular characterization of a novel focal adhesion kinase inhibitor. J Biol Chem. 2007 May 18;282(20):14845-52.
36 Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6486-9.
37 First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery. J Med Chem. 2009 Jan 22;52(2):293-307.
38 SU9516: biochemical analysis of cdk inhibition and crystal structure in complex with cdk2. Biochem Biophys Res Commun. 2003 Oct 24;310(3):1026-31.