Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T44458 | Target Info | |||
Target Name | Cyclin-dependent kinase 9 (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
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Target Type | Clinical trial Target | ||||
Gene Name | CDK9 | ||||
Biochemical Class | Kinase | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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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
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Representative Drug(s) | Flavopiridol | Drug Info | Ki = 40 nM | Click to Show More | [1] | |
2 | SNS-032 | Drug Info | IC50 = 925 nM | [4] | ||
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
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Representative Drug(s) | Flavopiridol | Drug Info | IC50 = 80 nM | [2] | ||
Co-Target Name | Protein kinase C epsilon (PRKCE) | Successful Target | ||||
UniProt ID | KPCE_HUMAN | |||||
Gene Name | PRKCE | |||||
Synonyms |
Protein kinase C epsilon type; PKCE; PKC epsilon; NPKC-epsilon
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Representative Drug(s) | Flavopiridol | Drug Info | IC50 = 480 nM | [3] | ||
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
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Representative Drug(s) | Flavopiridol | Drug Info | IC50 = 30 nM | Click to Show More | [5] | |
2 | SNS-032 | Drug Info | IC50 = 480 nM | [4] | ||
Co-Target Name | Cyclin-dependent kinase 2 (CDK2) | Clinical trial Target | ||||
UniProt ID | CDK2_HUMAN | |||||
Gene Name | CDK2 | |||||
Synonyms |
Sin3 associated polypeptide; SIN3-associated protein; P33 protein kinase; Cell division protein kinase 2; CDKN2
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Representative Drug(s) | SNS-032 | Drug Info | IC50 = 38 nM | Click to Show More | [6] | |
2 | Flavopiridol | Drug Info | IC50 = 40 nM | [7] | ||
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
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Representative Drug(s) | SNS-032 | Drug Info | IC50 = 62 nM | Click to Show More | [8] | |
2 | Flavopiridol | Drug Info | IC50 = 110 nM | [8] | ||
Co-Target Name | Protein kinase C delta (PRKCD) | Clinical trial Target | ||||
UniProt ID | KPCD_HUMAN | |||||
Gene Name | PRKCD | |||||
Synonyms |
nPKC-delta; Tyrosine-protein kinase PRKCD; SDK1; Protein kinase C delta type catalytic subunit; Protein kinase C delta type; PKC-delta
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Representative Drug(s) | Flavopiridol | Drug Info | IC50 = 890 nM | [3] | ||
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
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Representative Drug(s) | CYC065 | Drug Info | IC50 = 23 nM | Click to Show More | [9] | |
2 | Flavopiridol | Drug Info | IC50 = 170 nM | [8] | ||
Co-Target Name | La-related protein 7 (LARP7) | Co-Target | ||||
UniProt ID | LARP7_HUMAN | |||||
Gene Name | LARP7 | |||||
Synonyms |
La ribonucleoprotein domain family member 7; hLARP7; P-TEFb-interaction protein for 7SK stability; PIP7S
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Representative Drug(s) | Flavopiridol | Drug Info | Ki = 3 nM | [1] | ||
Co-Target Name | Cyclin dependent kinase 2-Cyclin A2 complex (CDK2-CCNA2) | Co-Target | ||||
UniProt ID | CDK2_HUMAN-CCNA2_HUMAN | |||||
Gene Name | CDK2-CCNA2 | |||||
Representative Drug(s) | CYC065 | Drug Info | IC50 = 5 nM | Click to Show More | [10] | |
2 | SNS-032 | Drug Info | IC50 = 38 nM | [10] | ||
3 | Flavopiridol | Drug Info | IC50 = 100 nM | [1] | ||
Co-Target Name | Cyclin dependent kinase 2-G1/S specific cyclin E1 complex (CDK2-CCNE1) | Co-Target | ||||
UniProt ID | CDK2_HUMAN-CCNE1_HUMAN | |||||
Gene Name | CDK2-CCNE1 | |||||
Representative Drug(s) | CYC065 | Drug Info | IC50 = 5 nM | Click to Show More | [9] | |
2 | SNS-032 | Drug Info | IC50 = 38 nM | [4] | ||
3 | Flavopiridol | Drug Info | IC50 = 100 nM | [1] | ||
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) | Flavopiridol | Drug Info | IC50 = 20 nM | Click to Show More | [1] | |
2 | SNS-032 | Drug Info | IC50 = 925 nM | [15] | ||
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) | CYC065 | Drug Info | IC50 = 21 nM | Click to Show More | [10] | |
2 | Flavopiridol | Drug Info | IC50 = 60 nM | [12] | ||
3 | SNS-032 | Drug Info | IC50 = 340 nM | [10] | ||
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) | Flavopiridol | Drug Info | IC50 = 27 nM | Click to Show More | [10] | |
2 | SNS-032 | Drug Info | IC50 = 480 nM | [15] | ||
3 | CYC065 | Drug Info | IC50 = 578 nM | [10] | ||
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) | Flavopiridol | Drug Info | IC50 = 30 nM | Click to Show More | [3] | |
2 | SNS-032 | Drug Info | IC50 = 480 nM | [11] | ||
Co-Target Name | Cyclin dependent kinase 2-G1/S specific cyclin E complex (CDK2-CCNE) | Co-Target | ||||
UniProt ID | CDK2_HUMAN-CCNE1_HUMAN/CCNE2_HUMAN | |||||
Gene Name | CDK2-CCNE1/CCNE2 | |||||
Representative Drug(s) | SNS-032 | Drug Info | IC50 = 48 nM | Click to Show More | [11] | |
2 | Flavopiridol | Drug Info | IC50 = 170 nM | [14] | ||
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) | SNS-032 | Drug Info | IC50 = 62 nM | Click to Show More | [6] | |
2 | Flavopiridol | Drug Info | IC50 = 110 nM | [1] | ||
3 | CYC065 | Drug Info | IC50 = 193 nM | [10] | ||
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) | SNS-032 | Drug Info | IC50 = 62 nM | Click to Show More | [10] | |
2 | Flavopiridol | Drug Info | IC50 = 514 nM | [10] | ||
Co-Target Name | Cyclin dependent kinase 2-Cyclin A complex (CDK2-CCNA2) | Co-Target | ||||
UniProt ID | CDK2_HUMAN-CCNA1_HUMAN/CCNA2_HUMAN | |||||
Gene Name | CDK2-CCNA1/CCNA2 | |||||
Representative Drug(s) | Flavopiridol | Drug Info | IC50 = 70 nM | [13] | ||
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) | Flavopiridol | Drug Info | IC50 = 100 nM | Click to Show More | [14] | |
2 | SNS-032 | Drug Info | IC50 = 925 nM | [11] | ||
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 | [10] | ||
Co-Target Name | Cyclin dependent kinase 6-G1/S specific cyclin D3 complex (CDK6-CCND2) | Co-Target | ||||
UniProt ID | CDK6_HUMAN-CCND3_HUMAN | |||||
Gene Name | CDK6-CCND3 | |||||
Representative Drug(s) | Flavopiridol | Drug Info | IC50 = 395 nM | [10] |
References | Top | ||||
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REF 1 | A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs. Bioorg Med Chem. 2019 Mar 1;27(5):677-685. | ||||
REF 2 | Molecular docking study on anticancer activity of plant-derived natural products. Med Chem Res. 2009 Jul 28;19:817-35. | ||||
REF 3 | Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities. J Med Chem. 2002 Aug 29;45(18):3905-27. | ||||
REF 4 | Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update. J Med Chem. 2019 May 9;62(9):4233-4251. | ||||
REF 5 | 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 6 | A diaminocyclohexyl analog of SNS-032 with improved permeability and bioavailability properties. Bioorg Med Chem Lett. 2008 Nov 1;18(21):5763-5. | ||||
REF 7 | A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. Nat Chem Biol. 2008 Jun;4(6):357-65. | ||||
REF 8 | Recent advances in the development of cyclin-dependent kinase 7 inhibitors. Eur J Med Chem. 2019 Dec 1;183:111641. | ||||
REF 9 | Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019). Bioorg Med Chem Lett. 2019 Oct 15;29(20):126637. | ||||
REF 10 | Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. J Med Chem. 2016 Oct 13;59(19):8667-84. | ||||
REF 11 | 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 12 | Synthesis, biological evaluation, and molecular modeling of natural and unnatural flavonoidal alkaloids, inhibitors of kinases. J Med Chem. 2012 Mar 22;55(6):2811-9. | ||||
REF 13 | Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects. J Med Chem. 2000 Nov 2;43(22):4126-34. | ||||
REF 14 | Synthesis and biological activity of N-aryl-2-aminothiazoles: potent pan inhibitors of cyclin-dependent kinases. Bioorg Med Chem Lett. 2004 Jun 7;14(11):2973-7. | ||||
REF 15 | 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. |
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