Co-Target(s) Information

Content Navigation (  All   None )                                      
Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T70176 Target Info
Target Name Cyclin-dependent kinase 2 (CDK2)
Synonyms
Sin3 associated polypeptide; SIN3-associated protein; P33 protein kinase; Cell division protein kinase 2; CDKN2
    Click to Show/Hide
Target Type Clinical trial Target
Gene Name CDK2
Biochemical Class Kinase
UniProt ID
CDK2_HUMAN
Co-Targets of This Target  Top
Co-Target Name Fms-like tyrosine kinase 3 (FLT-3) Successful Target
UniProt ID FLT3_HUMAN
Gene Name FLT3
Synonyms
Stem cell tyrosine kinase 1; STK1; STK-1; Receptor-type tyrosine-protein kinase FLT3; Fetal liver kinase-2; FLT-3; FLK2; FLK-2; FL cytokine receptor; CD135
    Click to Show/Hide
Representative Drug(s) TG02 Drug Info IC50 = 21 nM [1]
Co-Target Name Tropomyosin-related kinase A (TrkA) Successful Target
UniProt ID NTRK1_HUMAN
Gene Name NTRK1
Synonyms
gp140trk; Tyrosine kinase receptor A; Tyrosine kinase receptor; Trk-A; TRKA; TRK1-transforming tyrosine kinase protein; TRK1 transforming tyrosinekinase protein; TRK; P140-TrkA; Neurotrophic tyrosine kinase receptor type 1; NGF-trk receptor type A; MTC; High affinity nerve growth factor receptor
    Click to Show/Hide
Representative Drug(s) PHA848125 Drug Info IC50 = 53 nM [2]
Co-Target Name Janus kinase 2 (JAK-2) Successful Target
UniProt ID JAK2_HUMAN
Gene Name JAK2
Synonyms
Tyrosine-protein kinase JAK2
    Click to Show/Hide
Representative Drug(s) TG02 Drug Info IC50 = 73 nM [1]
Co-Target Name Cyclin-dependent kinase 6 (CDK6) Successful Target
UniProt ID CDK6_HUMAN
Gene Name CDK6
Synonyms
Serine/threonine-protein kinase PLSTIRE; Serine/threonine protein kinase PLSTIRE; Cell division protein kinase 6; CDKN6
    Click to Show/Hide
Representative Drug(s) TG02 Drug Info IC50 ~ 100 nM [3]
Co-Target Name LCK tyrosine protein kinase (LCK) Successful Target
UniProt ID LCK_HUMAN
Gene Name LCK
Synonyms
p56-LCK; Tyrosine-protein kinase Lck; T cell-specific protein-tyrosine kinase; Proto-oncogene tyrosine-protein kinase LCK; Proto-oncogene Lck; Protein YT16; Lymphocyte cell-specific protein-tyrosine kinase; Leukocyte C-terminal Src kinase; LSK; LCK p59-Fyn; LCK Protooncogene Syn
    Click to Show/Hide
Representative Drug(s) PHA848125 Drug Info IC50 = 209 nM [2]
Co-Target Name Cyclin-dependent kinase 4 (CDK4) Successful Target
UniProt ID CDK4_HUMAN
Gene Name CDK4
Synonyms
PSK-J3; Cell division protein kinase 4
    Click to Show/Hide
Representative Drug(s) AZD-5438 Drug Info IC50 = 450 nM Click to Show More [4]
2 SNS-032 Drug Info IC50 = 925 nM [3]
Co-Target Name Tyrosine-protein kinase ABL1 (ABL) Successful Target
UniProt ID ABL1_HUMAN
Gene Name ABL1
Synonyms
p150; Proto-oncogene tyrosine-protein kinase ABL1; Proto-oncogene c-Abl; JTK7; C-ABL; Abl; Abelson tyrosine-protein kinase 1; Abelson murine leukemia viral oncogene homolog 1
    Click to Show/Hide
Representative Drug(s) PHA848125 Drug Info IC50 = 478 nM [2]
Co-Target Name Tyrosine-protein kinase Kit (KIT) Successful Target
UniProt ID KIT_HUMAN
Gene Name KIT
Synonyms
v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog; p145 c-kit; Proto-oncogene tyrosine-protein kinase Kit; Proto-oncogene c-Kit; Piebald trait protein; PBT; Mast/stem cell growth factor receptor Kit; CD117 antigen; CD117; C-kit
    Click to Show/Hide
Representative Drug(s) PHA848125 Drug Info IC50 = 668 nM [2]
Co-Target Name Debrisoquine 4-hydroxylase (CYP2D6) Successful Target
UniProt ID CP2D6_HUMAN
Gene Name CYP2D6
Synonyms
P450-DB1; Cytochrome P450-DB1; Cytochrome P450 2D6; CYPIID6; CYP2DL1
    Click to Show/Hide
Representative Drug(s) TG02 Drug Info IC50 = 950 nM [5]
Co-Target Name Cyclin-dependent kinase 1 (CDK1) Clinical trial Target
UniProt ID CDK1_HUMAN
Gene Name CDK1
Synonyms
P34CDC2; P34 protein kinase; CDKN1; CDC28A; CDC2
    Click to Show/Hide
Representative Drug(s) TG02 Drug Info IC50 = 3 nM Click to Show More [1]
2 AZD-5438 Drug Info IC50 = 62 nM [7]
3 R-roscovitine Drug Info IC50 = 200 nM [10]
4 SNS-032 Drug Info IC50 = 480 nM [3]
Co-Target Name Cyclin-dependent kinase 9 (CDK9) Clinical trial Target
UniProt ID CDK9_HUMAN
Gene Name CDK9
Synonyms
Tat-associated kinase complex catalytic subunit; TAK; Similar to cyclin-dependent kinase 9; Serine/threonine-protein kinase PITALRE; Cyclin-dependent protein kinase Cdk9; Cell division protein kinase 9; Cell division cycle 2-like protein kinase 4; CDC2L4; CDC2-related kinase; C-2K
    Click to Show/Hide
Representative Drug(s) TG02 Drug Info IC50 = 3 nM Click to Show More [1]
2 SNS-032 Drug Info IC50 = 4 nM [6]
3 AT7519 Drug Info IC50 = 10 nM [6]
4 R-roscovitine Drug Info IC50 = 230 nM [13]
Co-Target Name Positive transcription elongation factor b (P-TEFb) Clinical trial Target
UniProt ID CDK9_HUMAN-CCNT1_HUMAN
Gene Name CDK9-CCNT1
Synonyms
P-TEFb
    Click to Show/Hide
Representative Drug(s) SNS-032 Drug Info IC50 = 4 nM Click to Show More [1]
2 AT7519 Drug Info IC50 < 10 nM [1]
3 CYC065 Drug Info IC50 = 26 nM [1]
4 PHA-793887 Drug Info IC50 = 138 nM [9]
5 R-roscovitine Drug Info IC50 = 220 nM [12]
Co-Target Name Cyclin-dependent kinase 7 (CDK7) Clinical trial Target
UniProt ID CDK7_HUMAN
Gene Name CDK7
Synonyms
TFIIH basal transcription factor complex kinase subunit; Serine/threonine-protein kinase 1; P39 Mo15; MO15; Cell division protein kinase 7; CDKN7; CDK-activating kinase 1; CDK-activating kinase; CAK1; CAK; 39 kDa protein kinase
    Click to Show/Hide
Representative Drug(s) SNS-032 Drug Info IC50 = 62 nM Click to Show More [8]
2 R-roscovitine Drug Info IC50 = 480 nM [8]
Co-Target Name Glycogen synthase kinase-3 beta (GSK-3B) Clinical trial Target
UniProt ID GSK3B_HUMAN
Gene Name GSK3B
Synonyms
Serine/threonine-protein kinase GSK3B; GSK-3 beta
    Click to Show/Hide
Representative Drug(s) PHA-793887 Drug Info IC50 = 79 nM Click to Show More [9]
2 AT7519 Drug Info IC50 < 200 nM [11]
Co-Target Name Vascular endothelial growth factor receptor 3 (FLT-4) Clinical trial Target
UniProt ID VGFR3_HUMAN
Gene Name FLT4
Synonyms
VEGFR3; VEGFR-3; VEGF-3 receptor; Tyrosine-protein kinase receptor FLT4; Fms-like tyrosine kinase 4
    Click to Show/Hide
Representative Drug(s) PHA848125 Drug Info IC50 = 920 nM [2]
Co-Target Name Cyclin-dependent kinase 5 (CDK5) Patented-recorded Target
UniProt ID CDK5_HUMAN
Gene Name CDK5
Synonyms
Tau protein kinase II catalytic subunit; TPKII catalytic subunit; Serine/threonine-protein kinase PSSALRE; Serine/threonine protein kinase PSSALRE; Proline-directed protein kinase F(A) (PDPK F(A)); Proline-directed protein kinase 33 kDa subunit; PDPK; Cyclin-dependent-like kinase 5; Cyclin-dependent kinase 5 (CDK5); Cell division protein kinase 5; CDKN5
    Click to Show/Hide
Representative Drug(s) TG02 Drug Info IC50 = 3 nM Click to Show More [1]
2 CYC065 Drug Info IC50 = 23 nM [14]
3 R-roscovitine Drug Info IC50 = 160 nM [15]
Co-Target Name G2/mitotic-specific cyclin B1 (CCNB1) Patented-recorded Target
UniProt ID CCNB1_HUMAN
Gene Name CCNB1
Synonyms
G2/mitotic-specific cyclin-B1; Cyclin B1; CCNB
    Click to Show/Hide
Representative Drug(s) AZD-5438 Drug Info IC50 = 16 nM [4]
Co-Target Name G1/S-specific cyclin-E1 (CCNE1) Literature-reported Target
UniProt ID CCNE1_HUMAN
Gene Name CCNE1
Synonyms
G1/S-specific cyclin E; Cyclin E; CCNE
    Click to Show/Hide
Representative Drug(s) AZD-5438 Drug Info IC50 = 6 nM [4]
Co-Target Name Cyclin D (CCND3) Literature-reported Target
UniProt ID CCND3_HUMAN
Gene Name CCND3
Synonyms
G1/S-specific cyclin-D3
    Click to Show/Hide
Representative Drug(s) AZD-5438 Drug Info IC50 = 21 nM [4]
Co-Target Name Cyclin A2 (CCNA2) Literature-reported Target
UniProt ID CCNA2_HUMAN
Gene Name CCNA2
Synonyms
Cyclin-A2; Cyclin-A; Cyclin A; CCNA
    Click to Show/Hide
Representative Drug(s) AZD-5438 Drug Info IC50 = 45 nM [4]
Co-Target Name Cyclin dependent kinase 1-G2/mitotic specific cyclin B1 complex (CDK1-CCNB1) Co-Target
UniProt ID CDK1_HUMAN-CCNB1_HUMAN
Gene Name CDK1-CCNB1
Representative Drug(s) AG-024322 Drug Info IC50 = 2.3 nM Click to Show More [3]
2 TG02 Drug Info IC50 = 9 nM [3]
3 PHA848125 Drug Info IC50 = 9 nM [3]
4 PHA-793887 Drug Info IC50 = 60 nM [9]
5 AT7519 Drug Info IC50 = 190 nM [18]
6 R-roscovitine Drug Info IC50 = 350 nM [22]
7 SNS-032 Drug Info IC50 = 480 nM [26]
8 CYC065 Drug Info IC50 = 578 nM [1]
Co-Target Name Cyclin dependent kinase 9-Cyclin K complex (CDK9-CCNK) Co-Target
UniProt ID CDK9_HUMAN-CCNK_HUMAN
Gene Name CDK9-CCNK
Representative Drug(s) TG02 Drug Info IC50 = 3 nM [3]
Co-Target Name Cyclin dependent kinase 3-G1/Sspecific cyclin E1 complex (CDK3-CCNE1) Co-Target
UniProt ID CDK3_HUMAN-CCNE1_HUMAN
Gene Name CDK3-CCNE1
Representative Drug(s) TG02 Drug Info IC50 = 3 nM Click to Show More [1]
2 AT7519 Drug Info IC50 = 360 nM [3]
Co-Target Name CDK7-Cyclin H-CDK activating kinase assembly factor MAT1 complex (CDK7-CCNH-MNAT1) Co-Target
UniProt ID CDK7_HUMAN-CCNH_HUMAN-MAT1_HUMAN
Gene Name CDK7-CCNH-MNAT1
Representative Drug(s) TG02 Drug Info IC50 = 3 nM Click to Show More [1]
2 SNS-032 Drug Info IC50 = 62 nM [1]
3 PHA848125 Drug Info IC50 = 270 nM [21]
Co-Target Name Cyclin dependent kinase 5-CDK5 activator 1 complex (CDK5-CDK5R1) Co-Target
UniProt ID CDK5_HUMAN-CD5R1_HUMAN
Gene Name CDK5-CDK5R1
Representative Drug(s) TG02 Drug Info IC50 = 4 nM Click to Show More [3]
2 PHA848125 Drug Info IC50 = 4 nM [3]
3 PHA-793887 Drug Info IC50 = 5 nM [9]
4 AT7519 Drug Info IC50 = 13 nM [11]
5 CYC065 Drug Info IC50 = 21 nM [1]
6 R-roscovitine Drug Info IC50 = 160 nM [20]
7 SNS-032 Drug Info IC50 = 340 nM [1]
Co-Target Name Cyclin dependent kinase 7-Cyclin H complex (CDK7-CCNH) Co-Target
UniProt ID CDK7_HUMAN-CCNH_HUMAN
Gene Name CDK7-CCNH
Representative Drug(s) PHA-793887 Drug Info IC50 = 10 nM Click to Show More [9]
2 SNS-032 Drug Info IC50 = 62 nM [17]
3 PHA848125 Drug Info IC50 = 150 nM [3]
4 CYC065 Drug Info IC50 = 193 nM [1]
5 R-roscovitine Drug Info IC50 = 360 nM [23]
Co-Target Name Cyclin dependent kinase 14-Cyclin Y complex (CDK14-CCNY) Co-Target
UniProt ID CDK14_HUMAN-CCNY_HUMAN
Gene Name CDK14-CCNY
Representative Drug(s) AT7519 Drug Info IC50 = 19.8 nM [16]
Co-Target Name Cyclin T1 Co-Target
UniProt ID CCNT1_HUMAN
Gene Name CCNT1
Synonyms
Cyclin-T1; CycT1; Cyclin-T
    Click to Show/Hide
Representative Drug(s) AZD-5438 Drug Info IC50 = 20 nM [4]
Co-Target Name Cyclin dependent kinase 4-G1/S specific cyclin D1 complex (CDK4-CCND1) Co-Target
UniProt ID CDK4_HUMAN-CCND1_HUMAN
Gene Name CDK4-CCND1
Representative Drug(s) PHA-793887 Drug Info IC50 = 62 nM Click to Show More [9]
2 AT7519 Drug Info IC50 = 67 nM [18]
3 PHA848125 Drug Info IC50 ~ 100 nM [3]
4 SNS-032 Drug Info IC50 = 925 nM [26]
Co-Target Name Cyclin dependent like kinase 5-Cyclin T1 complex (CDK5-CCNT1) Co-Target
UniProt ID CDK5_HUMAN-CCNT1_HUMAN
Gene Name CDK5-CCNT1
Representative Drug(s) R-roscovitine Drug Info IC50 = 160 nM [19]
Co-Target Name Cyclin dependent kinase 6-G1/S specific cyclin D3 complex (CDK6-CCND3) Co-Target
UniProt ID CDK6_HUMAN-CCND3_HUMAN
Gene Name CDK6-CCND3
Representative Drug(s) AT7519 Drug Info IC50 = 170 nM [3]
Co-Target Name Cyclin dependent kinase 4-G1/S specific cyclin E1 (CDK4-CCNE1) Co-Target
UniProt ID CDK4_HUMAN-CCNE1_HUMAN
Gene Name CDK4-CCNE1
Representative Drug(s) CYC065 Drug Info IC50 = 232 nM [1]
Co-Target Name Cyclin dependent kinase 1-G2/mitotic specific cyclin B complex (CDK1-CCNB) Co-Target
UniProt ID CDK1_HUMAN-CCNB1_HUMAN/CCNB2_HUMAN/CCNB3_HUMAN
Gene Name CDK1-CCNB1/CCNB2/CCNB3
Representative Drug(s) R-roscovitine Drug Info IC50 = 450 nM Click to Show More [24]
2 SNS-032 Drug Info IC50 = 480 nM [25]
Co-Target Name Cyclin dependent kinase 4-G1/S specific cyclin D complex (CDK4-CCND) Co-Target
UniProt ID CDK4_HUMAN-CCND1_HUMAN/CCND2_HUMAN/CCND3_HUMAN
Gene Name CDK4-CCND1-CCND2/CCND3
Representative Drug(s) SNS-032 Drug Info IC50 = 925 nM [25]
References  Top
REF 1 Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. J Med Chem. 2016 Oct 13;59(19):8667-84.
REF 2 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.
REF 3 Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update. J Med Chem. 2019 May 9;62(9):4233-4251.
REF 4 Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5487-92.
REF 5 Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinase-3 (FLT3) for the treatment of cancer. J Med Chem. 2012 Jan 12;55(1):169-96.
REF 6 Structural insights of cyclin dependent kinases: Implications in design of selective inhibitors. Eur J Med Chem. 2017 Dec 15;142:424-58.
REF 7 The discovery of AZD5597, a potent imidazole pyrimidine amide CDK inhibitor suitable for intravenous dosing. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6369-73.
REF 8 Recent advances in the development of cyclin-dependent kinase 7 inhibitors. Eur J Med Chem. 2019 Dec 1;183:111641.
REF 9 Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing. Bioorg Med Chem. 2010 Mar 1;18(5):1844-53.
REF 10 Microxine, a new cdc2 kinase inhibitor from the Australian marine sponge Microxina species. J Nat Prod. 2001 Apr;64(4):525-6.
REF 11 Cyclin dependent kinase (CDK) inhibitors as anticancer drugs. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3420-35.
REF 12 A beta-glucuronidase-responsive albumin-binding prodrug for potential selective kinase inhibitor-based cancer chemotherapy. Eur J Med Chem. 2018 Oct 5;158:1-6.
REF 13 Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. Eur J Med Chem. 2019 Jun 15;172:143-153.
REF 14 Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019). Bioorg Med Chem Lett. 2019 Oct 15;29(20):126637.
REF 15 Design, synthesis, and testing of an 6-O-linked series of benzimidazole based inhibitors of CDK5/p25. Bioorg Med Chem. 2011 Jan 1;19(1):359-73.
REF 16 Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14. Bioorg Med Chem Lett. 2019 Aug 1;29(15):1985-1993.
REF 17 A diaminocyclohexyl analog of SNS-032 with improved permeability and bioavailability properties. Bioorg Med Chem Lett. 2008 Nov 1;18(21):5763-5.
REF 18 Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design. J Med Chem. 2008 Aug 28;51(16):4986-99.
REF 19 A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. J Med Chem. 2010 Dec 23;53(24):8508-22.
REF 20 Novel 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitrile derivatives as dual cyclin-dependent kinase 1 (CDK1)/glycogen synthase kinase-3 (GSK-3) inhibitors: synthesis, biological evaluation and molecular modeling studies. Eur J Med Chem. 2008 Jul;43(7):1469-77.
REF 21 How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?. J Med Chem. 2018 Oct 25;61(20):9105-9120.
REF 22 Potent inhibitors of CDK5 derived from roscovitine: synthesis, biological evaluation and molecular modelling. Bioorg Med Chem Lett. 2013 Jan 1;23(1):125-31.
REF 23 Seliciclib (CYC202, R-Roscovitine) induces cell death in multiple myeloma cells by inhibition of RNA polymerase II-dependent transcription and down-regulation of Mcl-1. Cancer Res. 2005 Jun 15;65(12):5399-407.
REF 24 Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum. Bioorg Med Chem Lett. 2004 Apr 5;14(7):1703-7.
REF 25 N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent. J Med Chem. 2004 Mar 25;47(7):1719-28.
REF 26 Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). J Med Chem. 2014 Feb 13;57(3):578-99.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.