Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T67849 | Target Info | |||
Target Name | PI3-kinase delta (PIK3CD) | ||||
Synonyms |
PtdIns-3-kinase subunit p110-delta; PtdIns-3-kinase subunit delta; Phosphoinositide 3-kinase delta; Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit, delta isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit delta; PI3Kdelta; PI3K-delta; PI3-kinase subunit delta; PI3-kinase p110 subunit delta; P110delta
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Target Type | Successful Target | ||||
Gene Name | PIK3CD | ||||
Biochemical Class | Kinase | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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Co-Target Name | PI3-kinase alpha (PIK3CA) | Successful Target | ||||
UniProt ID | PK3CA_HUMAN | |||||
Gene Name | PIK3CA | |||||
Synonyms |
p110alpha; Serine/threonine protein kinase PIK3CA; PtdIns3kinase subunit p110alpha; PtdIns3kinase subunit alpha; PtdIns-3-kinase subunit p110-alpha; PtdIns-3-kinase subunit alpha; Phosphoinositide3kinase catalytic alpha polypeptide; Phosphoinositide-3-kinase catalytic alpha polypeptide; Phosphatidylinositol 4,5bisphosphate 3kinase catalytic subunit alpha isoform; Phosphatidylinositol 4,5bisphosphate 3kinase 110 kDa catalytic subunit alpha; Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit alpha; PI3kinase subunit alpha; PI3Kalpha; PI3K-alpha; PI3-kinase subunit alpha
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Representative Drug(s) | BAY 80-6946 | Drug Info | IC50 = 0.5 nM | Click to Show More | [1] | |
2 | PA-799 | Drug Info | IC50 = 14 nM | [3] | ||
3 | Buparlisib | Drug Info | IC50 = 20 nM | [4] | ||
4 | Idelalisib | Drug Info | IC50 = 177.2 nM | [10] | ||
Co-Target Name | PI3-kinase gamma (PIK3CG) | Successful Target | ||||
UniProt ID | PK3CG_HUMAN | |||||
Gene Name | PIK3CG | |||||
Synonyms |
p120-PI3K; p110gamma; Serine/threonine protein kinase PIK3CG; PtdIns-3-kinase subunit p110-gamma; PtdIns-3-kinase subunit gamma; PtdIns-3-kinase p110; Phosphoinositol-3 kinase; Phosphoinositide-3-kinase catalytic gamma polypeptide; Phosphoinositide 3-Kinase gamma; Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit, gamma isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit gamma; PI3Kgamma; PI3K-gamma; PI3K; PI3-kinase subunit gamma; PI3-kinase p110 subunit gamma
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Representative Drug(s) | BAY 80-6946 | Drug Info | IC50 = 0.7 nM | Click to Show More | [1] | |
2 | IPI-145 | Drug Info | IC50 = 2 nM | [2] | ||
3 | RP6530 | Drug Info | IC50 = 33 nM | [5] | ||
4 | PA-799 | Drug Info | IC50 = 36 nM | [6] | ||
5 | Idelalisib | Drug Info | IC50 = 60 nM | [8] | ||
6 | Umbralisib | Drug Info | IC50 ~ 120 nM | [5] | ||
7 | Buparlisib | Drug Info | IC50 = 256 nM | [1] | ||
8 | AMG 319 | Drug Info | IC50 = 850 nM | [11] | ||
Co-Target Name | Serine/threonine-protein kinase mTOR (mTOR) | Successful Target | ||||
UniProt ID | MTOR_HUMAN | |||||
Gene Name | MTOR | |||||
Synonyms |
Target of rapamycin; TOR kinase; Rapamycin target protein 1; Rapamycin target protein; Rapamycin and FKBP12 target 1; RAPT1; RAFT1; Mechanistic target of rapamycin; Mammalian target of rapamycin; FRAP2; FRAP1; FRAP; FKBP12-rapamycin complex-associated protein; FKBP-rapamycin associated protein; FK506-binding protein 12-rapamycin complex-associated protein 1
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Representative Drug(s) | BAY 80-6946 | Drug Info | IC50 = 45 nM | Click to Show More | [7] | |
2 | Buparlisib | Drug Info | IC50 = 94 nM | [9] | ||
3 | Idelalisib | Drug Info | IC50 ~ 1000 nM | [12] | ||
Co-Target Name | PI3-kinase beta (PIK3CB) | Clinical trial Target | ||||
UniProt ID | PK3CB_HUMAN | |||||
Gene Name | PIK3CB | |||||
Synonyms |
p110beta; PtdIns3kinase subunit p110beta; PtdIns3kinase subunit beta; PtdIns-3-kinase subunit p110-beta; PtdIns-3-kinase subunit beta; Phosphatidylinositol 4,5bisphosphate 3kinase catalytic subunitbeta isoform; Phosphatidylinositol 4,5bisphosphate 3kinase 110 kDa catalyticsubunit beta; Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit beta; PIK3C1; PI3kinase subunit beta; PI3Kbeta; PI3K-beta; PI3-kinase subunit beta
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Representative Drug(s) | BAY 80-6946 | Drug Info | IC50 = 3.7 nM | Click to Show More | [1] | |
2 | IPI-145 | Drug Info | IC50 = 85 nM | [13] | ||
3 | PA-799 | Drug Info | IC50 = 120 nM | [3] | ||
4 | Idelalisib | Drug Info | IC50 = 120.1 nM | [14] | ||
5 | Buparlisib | Drug Info | IC50 = 165.96 nM | [15] | ||
Co-Target Name | PI3K p110 alpha/p85 alpha (PIK3CA/PIK3R1) | Co-Target | ||||
UniProt ID | PK3CA_HUMAN-P85A_HUMAN | |||||
Gene Name | PIK3CA-PIK3R1 | |||||
Representative Drug(s) | BAY 80-6946 | Drug Info | IC50 = 0.11 nM | Click to Show More | [16] | |
2 | Buparlisib | Drug Info | IC50 = 11 nM | [17] | ||
3 | IPI-145 | Drug Info | IC50 = 400 nM | [19] | ||
4 | Idelalisib | Drug Info | IC50 = 800 nM | [13] | ||
Co-Target Name | PI3K p110 beta/p85 alpha (PIK3CB/PIK3R1) | Co-Target | ||||
UniProt ID | PK3CB_HUMAN-P85A_HUMAN | |||||
Gene Name | PIK3CB-PIK3R1 | |||||
Representative Drug(s) | BAY 80-6946 | Drug Info | IC50 = 4.57 nM | Click to Show More | [16] | |
2 | IPI-145 | Drug Info | IC50 = 8 nM | [2] | ||
3 | Buparlisib | Drug Info | IC50 = 234 nM | [17] | ||
4 | Idelalisib | Drug Info | IC50 = 293 nM | [2] | ||
Co-Target Name | PI3K-gamma/PI3K regulatory subunit 5 (PIK3CG-PIK3R5) | Co-Target | ||||
UniProt ID | PK3CG_HUMAN-PI3R5_HUMAN | |||||
Gene Name | PIK3CG-PIK3R5 | |||||
Representative Drug(s) | Buparlisib | Drug Info | IC50 = 129 nM | [18] | ||
Co-Target Name | PI3 kinase subunit beta-PI3 kinase regulatory subunit beta (PIK3CB-PIK3R2) | Co-Target | ||||
UniProt ID | PK3CB_HUMAN-P85B_HUMAN | |||||
Gene Name | PIK3CB-PIK3R2 | |||||
Representative Drug(s) | Idelalisib | Drug Info | IC50 = 579 nM | [20] | ||
Co-Target Name | Phosphatidylinositol 3-kinase catalytic subunit type 3 (PIK3C3) | Co-Target | ||||
UniProt ID | PK3C3_HUMAN | |||||
Gene Name | PIK3C3 | |||||
Synonyms |
PI3-kinase type 3; PI3K type 3; PtdIns-3-kinase type 3; Phosphatidylinositol 3-kinase p100 subunit; Phosphoinositide-3-kinase class 3; hVps34
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Representative Drug(s) | Idelalisib | Drug Info | IC50 = 980 nM | [5] | ||
Co-Target Name | Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta (PIK3C2B) | Co-Target | ||||
UniProt ID | P3C2B_HUMAN | |||||
Gene Name | PIK3C2B | |||||
Synonyms |
PI3K-C2-beta; PtdIns-3-kinase C2 subunit beta; C2-PI3K; Phosphoinositide 3-kinase-C2-beta
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Representative Drug(s) | Idelalisib | Drug Info | IC50 ~ 1000 nM | [21] |
References | Top | ||||
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REF 1 | Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer. Eur J Med Chem. 2019 Dec 1;183:111718. | ||||
REF 2 | Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kgamma-PI3Kdelta Dual Inhibitors. J Med Chem. 2019 May 23;62(10):4936-4948. | ||||
REF 3 | Small molecules targeting phosphoinositide 3-kinases. Medchemcomm. 2012;3:1337-55. | ||||
REF 4 | Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases. J Med Chem. 2019 Aug 8;62(15):6992-7014. | ||||
REF 5 | Evolution of PI3Kgamma and delta Inhibitors for Inflammatory and Autoimmune Diseases. J Med Chem. 2019 May 23;62(10):4783-4814. | ||||
REF 6 | Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1767-72. | ||||
REF 7 | Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective. J Med Chem. 2019 May 23;62(10):4815-4850. | ||||
REF 8 | Conformationally restricted quinazolone derivatives as PI3Kdelta-selective inhibitors: the design, synthesis and biological evaluation. Med. Chem. Commun. 2019;10:413-420. | ||||
REF 9 | 5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology. J Med Chem. 2017 Sep 14;60(17):7524-7538. | ||||
REF 10 | Synthesis and biological evaluation of 4-(piperid-3-yl)amino substituted 6-pyridylquinazolines as potent PI3Kdelta inhibitors. Bioorg Med Chem. 2019 Oct 1;27(19):115035. | ||||
REF 11 | Discovery and in Vivo Evaluation of the Potent and Selective PI3Kdelta Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-5-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-1430). J Med Chem. 2016 Aug 11;59(15):7252-67. | ||||
REF 12 | Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kdelta selective inhibitors. Bioorg Med Chem Lett. 2019 Jun 1;29(11):1313-1319. | ||||
REF 13 | Targeting the immunity protein kinases for immuno-oncology. Eur J Med Chem. 2019 Feb 1;163:413-427. | ||||
REF 14 | Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kdelta) inhibitors. Bioorg Med Chem. 2018 May 1;26(8):2028-40. | ||||
REF 15 | Discovery of Novel Dual Poly(ADP-ribose)polymerase and Phosphoinositide 3-Kinase Inhibitors as a Promising Strategy for Cancer Therapy. J Med Chem. 2020 Jan 9;63(1):122-139. | ||||
REF 16 | Design, Synthesis, and Biological Evaluation of Imidazo[1,2- a]pyridine Derivatives as Novel PI3K/mTOR Dual Inhibitors. J Med Chem. 2020 Mar 26;63(6):3028-3046. | ||||
REF 17 | Discovery of an Orally Bioavailable Dual PI3K/mTOR Inhibitor Based on Sulfonyl-Substituted Morpholinopyrimidines. ACS Med Chem Lett. 2018 Jun 25;9(7):719-724. | ||||
REF 18 | Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors. J Med Chem. 2016 Aug 11;59(15):7268-74. | ||||
REF 19 | Piperidinyl-embeded chalcones possessing anti PI3Kdelta inhibitory properties exhibit anti-atopic properties in preclinical models. Eur J Med Chem. 2018 Oct 5;158:405-413. | ||||
REF 20 | Discovery of fluoroquinolone derivatives as potent, selective inhibitors of PI3K gamma. Med. Chem. Commun. 2015;6:2029-2035 | ||||
REF 21 | Class II Phosphoinositide 3-Kinases as Novel Drug Targets. J Med Chem. 2017 Jan 12;60(1):47-65. |
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