Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T85799 | Target Info | |||
| Target Name | Cyclin-dependent kinase 4 (CDK4) | ||||
| Synonyms |
PSK-J3; Cell division protein kinase 4
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| Target Type | Successful Target | ||||
| Gene Name | CDK4 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
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| 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) | LY2835219 | Drug Info | IC50 = 1.9 nM | Click to Show More | [1] | |
| 2 | LEE011 | Drug Info | IC50 = 6 nM | [2] | ||
| 3 | Palbociclib | Drug Info | IC50 = 15 nM | [3] | ||
| 4 | P1446A-05 | Drug Info | IC50 < 100 nM | [7] | ||
| Co-Target Name | Phosphodiesterase 4D (PDE4D) | Successful Target | ||||
| UniProt ID | PDE4D_HUMAN | |||||
| Gene Name | PDE4D | |||||
| Synonyms |
cAMP-specific 3',5'-cyclic phosphodiesterase 4D; PDE43; DPDE3
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| Representative Drug(s) | Apremilast | Drug Info | IC50 = 33 nM | [4] | ||
| Co-Target Name | Janus kinase 3 (JAK-3) | Successful Target | ||||
| UniProt ID | JAK3_HUMAN | |||||
| Gene Name | JAK3 | |||||
| Synonyms |
Tyrosine-protein kinase JAK3; Leukocyte janus kinase; L-JAK
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| Representative Drug(s) | Palbociclib | Drug Info | IC50 = 63.1 nM | [5] | ||
| Co-Target Name | Phosphodiesterase 4 (PDE4) | Successful Target | ||||
| UniProt ID | PDE4A_HUMAN; PDE4B_HUMAN; PDE4C_HUMAN; PDE4D_HUMAN | |||||
| Gene Name | NO-GeName | |||||
| Synonyms |
PDE-4
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| Representative Drug(s) | Apremilast | Drug Info | IC50 = 74 nM | [6] | ||
| Co-Target Name | Serine/threonine-protein kinase pim-1 (PIM1) | Clinical trial Target | ||||
| UniProt ID | PIM1_HUMAN | |||||
| Gene Name | PIM1 | |||||
| Synonyms |
Pim-1 proto-oncogene, serine/threonine kinase; PIM
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| Representative Drug(s) | LY2835219 | Drug Info | Ki < 10 nM | [3] | ||
| 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 | [8] | |
| 2 | P1446A-05 | Drug Info | IC50 = 22 nM | [8] | ||
| 3 | LY2835219 | Drug Info | IC50 = 57 nM | [10] | ||
| 4 | PHA-793887 | Drug Info | IC50 = 138 nM | [11] | ||
| 5 | LEE011 | Drug Info | IC50 = 197 nM | [12] | ||
| 6 | Palbociclib | Drug Info | Ki = 364 nM | [13] | ||
| Co-Target Name | Phosphodiesterase 4B (PDE4B) | Clinical trial Target | ||||
| UniProt ID | PDE4B_HUMAN | |||||
| Gene Name | PDE4B | |||||
| Synonyms |
cAMP-specific 3',5'-cyclic phosphodiesterase 4B; Type 4B cAMP phosphodiesterase; Type 4 cyclic adenosine monophosphate phosphodiesterase (type 4 PDE); PDE32; DPDE4
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| Representative Drug(s) | Apremilast | Drug Info | IC50 = 24 nM | [9] | ||
| 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) | LY2835219 | Drug Info | IC50 = 57 nM | Click to Show More | [3] | |
| 2 | P1446A-05 | Drug Info | IC50 < 100 nM | [7] | ||
| 3 | Palbociclib | Drug Info | IC50 = 794.33 nM | [5] | ||
| 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 | [11] | ||
| 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) | P1446A-05 | Drug Info | IC50 < 100 nM | Click to Show More | [7] | |
| 2 | LY2835219 | Drug Info | IC50 ~ 1000 nM | [3] | ||
| 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) | LY2835219 | Drug Info | IC50 = 300 nM | [3] | ||
| 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) | LY2835219 | Drug Info | IC50 ~ 500 nM | [3] | ||
| Co-Target Name | Dual-specificity tyrosine-phosphorylation regulated kinase 1A (DYRK1A) | Patented-recorded Target | ||||
| UniProt ID | DYR1A_HUMAN | |||||
| Gene Name | DYRK1A | |||||
| Synonyms |
hMNB; Protein kinase minibrain homolog; MNBH; MNB; HP86; Dual specificity tyrosine-phosphorylation-regulated kinase 1A; Dual specificity YAK1-related kinase; DYRK
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| Representative Drug(s) | LY2835219 | Drug Info | Ki < 10 nM | [3] | ||
| 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 | [14] | |
| 2 | P1446A-05 | Drug Info | IC50 = 25 nM | [8] | ||
| 3 | PHA-793887 | Drug Info | IC50 = 60 nM | [11] | ||
| 4 | P-276 | Drug Info | IC50 = 79 nM | [8] | ||
| 5 | LY2835219 | Drug Info | IC50 = 371 nM | [21] | ||
| 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 | [14] | |
| 2 | LY2835219 | Drug Info | IC50 = 46 nM | [20] | ||
| 3 | P-276 | Drug Info | IC50 = 224 nM | [8] | ||
| 4 | Palbociclib | Drug Info | IC50 = 230 nM | [15] | ||
| Co-Target Name | Cyclin dependent kinase 6-G1/S specific cyclin D1 complex (CDK6-CCND1) | Co-Target | ||||
| UniProt ID | CDK6_HUMAN-CCND1_HUMAN | |||||
| Gene Name | CDK6-CCND1 | |||||
| Representative Drug(s) | Palbociclib | Drug Info | IC50 = 3.76 nM | Click to Show More | [15] | |
| 2 | LY2835219 | Drug Info | IC50 = 10 nM | [19] | ||
| 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) | Trilaciclib | Drug Info | IC50 = 4 nM | Click to Show More | [16] | |
| 2 | LY2835219 | Drug Info | IC50 = 5 nM | [17] | ||
| 3 | Palbociclib | Drug Info | IC50 = 19 nM | [17] | ||
| 4 | LEE011 | Drug Info | IC50 = 28 nM | [17] | ||
| 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 | [11] | |
| 2 | LY2835219 | Drug Info | IC50 = 405 nM | [20] | ||
| 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 | [11] | ||
| 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 | [11] | |
| 2 | Trilaciclib | Drug Info | EC50 < 100 nM | [16] | ||
| 3 | G1T38 | Drug Info | EC50 < 100 nM | [16] | ||
| 4 | LY2835219 | Drug Info | IC50 = 347 nM | [20] | ||
| Co-Target Name | Cyclin dependent kinase 6-G1/S specific cyclin D2 complex (CDK6-CCND2) | Co-Target | ||||
| UniProt ID | CDK6_HUMAN-CCND2_HUMAN | |||||
| Gene Name | CDK6-CCND2 | |||||
| Representative Drug(s) | Palbociclib | Drug Info | IC50 = 9 nM | [18] | ||
| Co-Target Name | CaM kinase I alpha (CAMK1) | Co-Target | ||||
| UniProt ID | KCC1A_HUMAN | |||||
| Gene Name | CAMK1 | |||||
| Synonyms |
Calcium/calmodulin-dependent protein kinase type 1; CaM kinase I; CaM-KI; CaMKI-alpha
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| Representative Drug(s) | LY2835219 | Drug Info | Ki < 10 nM | [3] | ||
| Co-Target Name | Homeodomain-interacting protein kinase 1 (HIPK1) | Co-Target | ||||
| UniProt ID | HIPK1_HUMAN | |||||
| Gene Name | HIPK1 | |||||
| Synonyms |
Nuclear body-associated kinase 2
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| Representative Drug(s) | LY2835219 | Drug Info | Ki < 10 nM | [3] | ||
| 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 | [11] | ||
| Co-Target Name | Cyclin dependent kinase 1-G1/S specific cyclin D3 complex (CDK1-CCND3) | Co-Target | ||||
| UniProt ID | CDK1_HUMAN-CCND3_HUMAN | |||||
| Gene Name | CDK1-CCND3 | |||||
| Representative Drug(s) | LY2835219 | Drug Info | IC50 = 56 nM | [19] | ||
| Co-Target Name | Cyclin dependent kinase 9-Cyclin H complex (CDK9-CCNH) | Co-Target | ||||
| UniProt ID | CDK9_HUMAN-CCNH_HUMAN | |||||
| Gene Name | CDK9-CCNH | |||||
| Representative Drug(s) | G1T38 | Drug Info | IC50 = 280 nM | Click to Show More | [16] | |
| 2 | G1T38 | Drug Info | IC50 = 280 nM | [16] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of a class of diheteroaromatic amines as orally bioavailable CDK1/4/6 inhibitors. Bioorg Med Chem Lett. 2017 Dec 1;27(23):5332-6. | ||||
| REF 2 | Structural insights of cyclin dependent kinases: Implications in design of selective inhibitors. Eur J Med Chem. 2017 Dec 15;142:424-58. | ||||
| REF 3 | 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 4 | InCl 3 mediated heteroarylation of indoles and their derivatization via CH activation strategy: Discovery of 2-(1H-indol-3-yl)-quinoxaline derivatives as a new class of PDE4B selective inhibitors for arthritis and/or multiple sclerosis. Eur J Med Chem. 2019 Jul 15;174:198-215. | ||||
| REF 5 | Selectivity data: assessment, predictions, concordance, and implications. J Med Chem. 2013 Sep 12;56(17):6991-7002. | ||||
| REF 6 | Discovery of (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl] acetamide (apremilast), a potent and orally active phosphodiesterase 4 and tumor necrosis factor-alpha inhibitor. J Med Chem. 2009 Mar 26;52(6):1522-4. | ||||
| REF 7 | A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs. Bioorg Med Chem. 2019 Mar 1;27(5):677-685. | ||||
| REF 8 | Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. J Med Chem. 2016 Oct 13;59(19):8667-84. | ||||
| REF 9 | Design and Synthesis of Selective Phosphodiesterase 4D (PDE4D) Allosteric Inhibitors for the Treatment of Fragile X Syndrome and Other Brain Disorders. J Med Chem. 2019 May 23;62(10):4884-4901. | ||||
| REF 10 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. Eur J Med Chem. 2018 Mar 25;148:140-153. | ||||
| REF 11 | 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 12 | Novel cyclin-dependent kinase 9 (CDK9) inhibitor with suppression of cancer stemness activity against non-small-cell lung cancer. Eur J Med Chem. 2019 Nov 1;181:111535. | ||||
| REF 13 | Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. J Med Chem. 2017 Mar 9;60(5):1892-915. | ||||
| REF 14 | Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update. J Med Chem. 2019 May 9;62(9):4233-4251. | ||||
| 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. | ||||
| REF 16 | Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019). Bioorg Med Chem Lett. 2019 Oct 15;29(20):126637. | ||||
| REF 17 | A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy. Eur J Med Chem. 2018 Jan 20;144:1-28. | ||||
| REF 18 | Cyclin dependent kinase (CDK) inhibitors as anticancer drugs. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3420-35. | ||||
| REF 19 | Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity relationships. Bioorg Med Chem Lett. 2018 Mar 1;28(5):974-8. | ||||
| REF 20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?. J Med Chem. 2018 Oct 25;61(20):9105-9120. | ||||
| REF 21 | Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors. Eur J Med Chem. 2016 Jan 27;108:701-719. | ||||
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