Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T95399 | Target Info | |||
| Target Name | Myophosphorylase (PYGM) | ||||
| Synonyms |
Glycogen phosphorylase, muscle form; Myophosphorylase
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| Target Type | Discontinued Target | ||||
| Gene Name | PYGM | ||||
| 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 | [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
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| Representative Drug(s) | Flavopiridol | Drug Info | IC50 = 80 nM | [2] | ||
| Co-Target Name | Glycogen synthase kinase-3 alpha (GSK-3A) | Successful Target | ||||
| UniProt ID | GSK3A_HUMAN | |||||
| Gene Name | GSK3A | |||||
| Synonyms |
Serine/threonineprotein kinase GSK3A; Serine/threonine-protein kinase GSK3A; Glycogen synthase kinase3 alpha; Glycogen synthase kinase 3; GSK3 alpha; GSK-3 alpha; GSK-3
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| Representative Drug(s) | Flavopiridol | Drug Info | IC50 = 280 nM | [3] | ||
| 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 | [4] | ||
| 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
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| Representative Drug(s) | Flavopiridol | Drug Info | IC50 = 2.5 nM | [5] | ||
| 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
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| Representative Drug(s) | Flavopiridol | Drug Info | Ki = 3 nM | [6] | ||
| 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 | [7] | ||
| 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) | Flavopiridol | Drug Info | IC50 = 40 nM | [8] | ||
| 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) | Flavopiridol | Drug Info | IC50 = 110 nM | [9] | ||
| 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
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| Representative Drug(s) | Flavopiridol | Drug Info | IC50 = 280 nM | [3] | ||
| 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 | [4] | ||
| 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) | Flavopiridol | Drug Info | IC50 = 170 nM | [9] | ||
| 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 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 | [1] | ||
| 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 | [5] | ||
| 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 | [4] | ||
| 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) | Flavopiridol | Drug Info | IC50 = 60 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 | [11] | ||
| 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) | Flavopiridol | Drug Info | IC50 = 100 nM | [1] | ||
| 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 | [12] | ||
| 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) | Flavopiridol | Drug Info | IC50 = 100 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) | Flavopiridol | Drug Info | IC50 = 110 nM | [1] | ||
| 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) | Flavopiridol | Drug Info | IC50 = 170 nM | [12] | ||
| 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 | [5] | ||
| 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) | Flavopiridol | Drug Info | IC50 = 514 nM | [5] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| 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 | Crystal structure of a human cyclin-dependent kinase 6 complex with a flavonol inhibitor, fisetin. J Med Chem. 2005 Feb 10;48(3):737-43. | ||||
| REF 4 | 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 5 | Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. J Med Chem. 2016 Oct 13;59(19):8667-84. | ||||
| REF 6 | Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity. J Med Chem. 2013 Feb 14;56(3):660-70. | ||||
| REF 7 | 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 8 | A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. Nat Chem Biol. 2008 Jun;4(6):357-65. | ||||
| REF 9 | Recent advances in the development of cyclin-dependent kinase 7 inhibitors. Eur J Med Chem. 2019 Dec 1;183:111641. | ||||
| REF 10 | 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 11 | Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects. J Med Chem. 2000 Nov 2;43(22):4126-34. | ||||
| REF 12 | 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. | ||||
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