Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T49898 | Target Info | |||
| Target Name | Cyclin-dependent kinase 1 (CDK1) | ||||
| Synonyms |
P34CDC2; P34 protein kinase; CDKN1; CDC28A; CDC2
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| Target Type | Clinical trial Target | ||||
| Gene Name | CDK1 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| 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) | P-276 | Drug Info | IC50 = 20 nM | Click to Show More | [1] | |
| 2 | PHA-793887 | Drug Info | IC50 = 138 nM | [2] | ||
| 3 | R-roscovitine | Drug Info | IC50 = 220 nM | [4] | ||
| 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) | PHA-793887 | Drug Info | IC50 = 79 nM | [2] | ||
| 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) | R-roscovitine | Drug Info | IC50 = 90 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
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| Representative Drug(s) | R-roscovitine | Drug Info | IC50 = 230 nM | [5] | ||
| 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) | R-roscovitine | Drug Info | IC50 = 480 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) | R-roscovitine | Drug Info | IC50 = 160 nM | [6] | ||
| 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) | AG-024322 | Drug Info | IC50 = 3 nM | Click to Show More | [7] | |
| 2 | R-roscovitine | Drug Info | IC50 = 72 nM | [4] | ||
| 3 | P-276 | Drug Info | IC50 = 224 nM | [1] | ||
| 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) | PHA-793887 | Drug Info | IC50 = 5 nM | Click to Show More | [2] | |
| 2 | R-roscovitine | Drug Info | IC50 = 160 nM | [13] | ||
| 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) | PHA-793887 | Drug Info | IC50 = 8 nM | Click to Show More | [2] | |
| 2 | R-roscovitine | Drug Info | IC50 = 100 nM | [9] | ||
| 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) | PHA-793887 | Drug Info | IC50 = 8 nM | Click to Show More | [2] | |
| 2 | R-roscovitine | Drug Info | IC50 = 100 nM | [11] | ||
| 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 | [2] | |
| 2 | R-roscovitine | Drug Info | IC50 = 360 nM | [10] | ||
| 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 | [2] | |
| 2 | P-276 | Drug Info | IC50 = 63 nM | [8] | ||
| 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) | R-roscovitine | Drug Info | IC50 = 100 nM | [10] | ||
| 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 | [12] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. J Med Chem. 2016 Oct 13;59(19):8667-84. | ||||
| REF 2 | 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 3 | Recent advances in the development of cyclin-dependent kinase 7 inhibitors. Eur J Med Chem. 2019 Dec 1;183:111641. | ||||
| REF 4 | 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 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 | 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 7 | Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update. J Med Chem. 2019 May 9;62(9):4233-4251. | ||||
| REF 8 | Discovery and Preclinical Development of IIIM-290, an Orally Active Potent Cyclin-Dependent Kinase Inhibitor. J Med Chem. 2018 Feb 22;61(4):1664-1687. | ||||
| REF 9 | Substituted 4-(thiazol-5-yl)-2-(phenylamino)pyrimidines are highly active CDK9 inhibitors: synthesis, X-ray crystal structures, structure-activity relationship, and anticancer activities. J Med Chem. 2013 Feb 14;56(3):640-59. | ||||
| REF 10 | 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 11 | 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. | ||||
| REF 12 | 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 13 | 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. | ||||
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