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phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha

Target Id 2153
缩写名 PI3Kα
家族 Phosphatidylinositol-4,5-bisphosphate 3-kinase family

基因和蛋白信息

Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 1068 3q26.32 PIK3CA phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha
Mouse 2 1068 3 15.7 cM Pik3ca phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha
Rat 2 1068 2 q25 Pik3ca phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit alpha

作用于该靶标的配体

Ligand Id Ligand Ligand Type Action on Target 对应产品货号 产品名称
7743 izorlisib Synthetic organic Inhibition C127596 CH5132799
7794 taselisib Synthetic organic Inhibition T413710 Taselisib (GDC 0032)
7795 duvelisib Synthetic organic Inhibition I126464 Duvelisib (IPI-145, INK1197),P100δ抑制剂
6004 LY 294002 Synthetic organic Inhibition L276596 LY 294002（DMSO溶液）
6023 PI 3-Kg inhibitor Synthetic organic Inhibition A127765 AS-605240,PI3Kγ抑制剂
6024 PI 3-Kg inhibitor II Synthetic organic Inhibition A129517 AS-604850,ATP竞争性PI3Kγ抑制剂
6060 wortmannin Natural product Inhibition W100984 渥曼青霉素
5715 TG-100-115 Synthetic organic Inhibition T127783 TG100-115,PI3Kγ/δ抑制剂
7878 buparlisib Synthetic organic Inhibition N127553 BKM120,体外PI3K抑制剂
7888 apitolisib Synthetic organic Inhibition G126387 GDC-0980 (RG7422)
7933 sapanisertib Synthetic organic Inhibition I128086 INK 128 (MLN0128),mTOR抑制剂
7936 PF-04691502 Synthetic organic Inhibition P126369 PF-04691502,双重PI 3-K / mTOR抑制剂
7940 gedatolisib Synthetic organic Inhibition P129530 Gedatolisib (PF-05212384, PKI-587),双重PI 3-K / mTOR抑制剂
7950 dactolisib Synthetic organic Inhibition B126286 BEZ235,有效的PI3K和mTOR抑制剂
7951 BGT-226 Synthetic organic Inhibition B608036 BGT-226
8011 KU-0060648 Synthetic organic Inhibition K129743 KU-0060648,DNA-PK和PI 3-K双重抑制剂
5701 PI-103 Synthetic organic Inhibition P125961 PI-103,PI3K 和 mTOR 抑制剂
8012 PIK-75 Synthetic organic Inhibition P333866 PIK-75，游离
8012 PIK-75 Synthetic organic Inhibition P333866 PIK-75，游离
8013 PP121 Synthetic organic Inhibition P126419 PP121,酪氨酸和磷酸肌醇激酶的双重抑制剂
7955 alpelisib Synthetic organic Inhibition B127311 阿培利司
6741 idelalisib Synthetic organic Inhibition C127044 CAL-101,P110δ抑制剂
5682 pictilisib Synthetic organic Inhibition G126357 GDC-0941,有效的PI3K抑制剂
8059 AZD6482 Synthetic organic Inhibition A129523 AZD6482,PI3-Kβ抑制剂
8243 HS-173 Synthetic organic Inhibition H351992 HS-173
8382 VS-5584 Synthetic organic Inhibition V125616 VS-5584(SB2343),PI3K/mTOR双重抑制剂
8383 bimiralisib Synthetic organic Inhibition B414146 Bimiralisib (PQR309)
8527 AZD8186 Synthetic organic Inhibition A174656 azd-8186
8793 SAR260301 Synthetic organic Inhibition S613412 2-[2-[(2S)-2-methyl-2,3-dihydroindol-1-yl]-2-oxoethyl]-6-morpholin-4-yl-1H-pyrimidin-4-one
8805 compound 82 [PMID: 21332118] Synthetic organic Inhibition N609439 N-[6-[6-chloro-5-[(4-fluorophenyl)sulfonylamino]pyridin-3-yl]-1,3-benzothiazol-2-yl]acetamide
8827 compound 11j [PMID: 23021994] Synthetic organic Inhibition C608659 1-[4-[4-[2-[4-chloro-3-(diethylsulfamoyl)anilino]pyrimidin-4-yl]pyridin-2-yl]phenyl]-3-methylurea
8915 AZD8835 Synthetic organic Inhibition A413893 AZD8835
8917 AMG319 Synthetic organic Inhibition A413839 AMG319
8918 samotolisib Synthetic organic Inhibition S413971 Samotolisib (LY3023414)
8952 fimepinostat Synthetic organic Inhibition C126527 非美诺司他
8968 PIK-108 Synthetic organic Negative P612834 PIK-108
7963 pilaralisib Synthetic organic Inhibition X129499 XL147,PI3K抑制剂
7965 ZSTK474 Synthetic organic Inhibition Z126804 ZSTK474,PI3K抑制剂
8969 serabelisib Synthetic organic Inhibition S276459 Serabelisib,抑制剂
8974 omipalisib Synthetic organic Inhibition G127233 GSK2126458(GSK458),PI3激酶抑制剂
8978 quinostatin Synthetic organic Inhibition Q613055 quinostatin
8978 quinostatin Synthetic organic Inhibition Q613055 quinostatin
9424 leniolisib Synthetic organic Inhibition L414153 leniolisib (CDZ 173)
9425 nemiralisib Synthetic organic Inhibition N413878 Nemiralisib (GSK2269557)
9563 eganelisib Synthetic organic Inhibition E413975 Eganelisib (IPI-549)
9571 eCF309 Synthetic organic Inhibition E610057 eCF309
9636 inavolisib Synthetic organic Inhibition G419993 GDC-0077
7794 taselisib Synthetic organic Inhibition T413710 Taselisib (GDC 0032)
5682 pictilisib Synthetic organic Inhibition G126357 GDC-0941,有效的PI3K抑制剂
9728 dezapelisib Synthetic organic Inhibition D609853 dezapelisib
9800 seletalisib Synthetic organic Inhibition S414058 Seletalisib (UCB-5857)
9826 GSK1059615 Synthetic organic Inhibition G127955 GSK1059615,PI 3-激酶抑制剂
9907 tenalisib Synthetic organic Inhibition T414107 Tenalisib (RP6530)
9916 panulisib Synthetic organic Inhibition P612623 panulisib
9928 puquitinib Synthetic organic Inhibition P613018 puquitinib
9997 AZD3458 Synthetic organic Inhibition A607864 AZD3458
10001 compound 52 [PMID: 28541707] Synthetic organic Inhibition A609297 2-(4-acetyl-3,3-dimethyl-2-oxopiperazin-1-yl)-4-[4-amino-5-(trifluoromethyl)pyrrolo[2,1-f][1,2,4]triazin-7-yl]benzonitrile
10096 acalisib Synthetic organic Inhibition A413341 acalisib (GS-9820)
10097 paxalisib Synthetic organic Inhibition P413923 Paxalisib (GDC-0084)
10142 PQR620 Synthetic organic Inhibition P612909 PQR620
10142 PQR620 Synthetic organic Inhibition P612909 PQR620
10151 neolymphostin A Synthetic organic Inhibition N612219 neolymphostin A
6060 wortmannin Natural product Inhibition W100984 渥曼青霉素
10162 RV1729 Synthetic organic Inhibition R613336 RV1729
10163 RV6153 Synthetic organic Inhibition R613337 RV6153
10233 AZ2 Synthetic organic Inhibition A607838 AZ2
10234 compound 22 [PMID: 24754609] Synthetic organic Inhibition M608958 1-[6-(5-methoxypyridin-3-yl)-1,3-benzothiazol-2-yl]-3-[2-(1-propylimidazol-4-yl)ethyl]urea
10365 compound 2q [PMID: 30986068] Synthetic organic Inhibition S609091 [(3S)-3-[8-(1-ethyl-5-methylpyrazol-4-yl)-9-methylpurin-6-yl]oxypyrrolidin-1-yl]-(oxan-4-yl)methanone
10441 compound 5d [PMID: 31335136] Synthetic organic Inhibition D609327 2,4-difluoro-N-[2-methoxy-5-[4-methyl-8-[(3-methyloxetan-3-yl)methoxy]quinazolin-6-yl]pyridin-3-yl]benzenesulfonamide
10489 compound 12b [PMID: 31465220] Synthetic organic Inhibition R608674 5-((R)-4-((R)-3-Methylmorpholino)-5a,6,8,9-tetrahydro-5H-pyrimido[5',4':4,5]pyrrolo[2,1-c][1,4]oxazin-2-yl)pyrazin-2-amine
10578 AS-252424 Synthetic organic Inhibition A129503 AS-252424,PI3Kγ抑制剂
10598 compound 41 [PMID: 31855425] Synthetic organic Inhibition R609220 (R)-2-Methoxy-N-(2-methoxy-5-(7-((4-(oxetan-3-yl)morpholin-2-yl)methoxy)-1,3-dihydroisobenzofuran-5-yl)pyridin-3-yl)ethanesulfonamide
10601 AZD7648 Synthetic organic Inhibition A414215 AZD7648
10627 zandelisib Synthetic organic Inhibition Z413033 Zandelisib
10649 compound 7 [PMID: 31955578] Synthetic organic Inhibition S609431 (S)-3-Methyl-4-(7-((R)-3-methylmorpholino)-2-(1H-pyrazol-3-yl)thiazolo[5,4-d]pyrimidin-5-yl)morpholine
10702 compound 15a [PMID: 32069401] Synthetic organic Inhibition D608737 2,4-Difluoro-N-(2-methoxy-5-(3-(5-(2-(4-methylpiperazin-1-yl)ethyl)-1,3,4-oxadiazol-2-yl)imidazo[1,2-a]pyridin-6-yl)pyridin-3-yl)benzenesulfonamide
7875 copanlisib Synthetic organic Inhibition B129540 库潘尼西
11204 AZD8154 Synthetic organic Inhibition A607886 AZD8154
11876 gilmelisib Synthetic organic Inhibition G610557 gilmelisib
12062 compound 27 [PMID: 35834807] Synthetic organic Inhibition D609025 6-(4,6-Dimorpholino-1,3,5-triazin-2-yl)benzo[d]oxazol-2-amine
12075 vulolisib Synthetic organic Inhibition V614824 vulolisib
12119 NVP-CLR457 Synthetic organic Inhibition N612440 NVP-CLR457
12382 risovalisib Synthetic organic Inhibition R613205 risovalisib
12616 DS-7423 Synthetic organic Inhibition D609983 DS-7423
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