Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T95913 Target Info
Target Name PI3-kinase gamma (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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Target Type Successful Target
Gene Name PIK3CG
Biochemical Class Kinase
UniProt ID
PK3CG_HUMAN
Co-Targets of This Target  Top
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) GSK2126458 Drug Info IC50 = 0.04 nM Click to Show More [1]
2 GDC-0032 Drug Info Ki = 0.29 nM [2]
3 PF-05212384 Drug Info IC50 = 0.4 nM [1]
4 BAY 80-6946 Drug Info IC50 = 0.5 nM [6]
5 PF-04691502 Drug Info Ki = 0.57 nM [8]
6 GDC-0084 Drug Info Ki = 2 nM [11]
7 GDC0941 Drug Info Ki = 2.6 nM [13]
8 BEZ235 Drug Info IC50 = 4 nM [1]
9 BGT226 Drug Info IC50 = 4 nM [16]
10 GDC-0980/RG7422 Drug Info IC50 = 4.8 nM [17]
11 ZSTK474 Drug Info IC50 = 6 nM [19]
12 PA-799 Drug Info IC50 = 14 nM [1]
13 VS-5584 Drug Info IC50 = 16 nM [25]
14 IPI-549 Drug Info IC50 = 17 nM [21]
15 PQR309 Drug Info Ki = 17 nM [26]
16 Buparlisib Drug Info IC50 = 20 nM [4]
17 AZD8186 Drug Info IC50 = 35 nM [24]
18 XL147 Drug Info IC50 = 39 nM [1]
19 SAR245409 Drug Info IC50 = 39 nM [6]
20 CUDC-907 Drug Info IC50 = 69 nM [4]
21 PX-866 Drug Info IC50 = 88 nM [30]
Co-Target Name PI3-kinase delta (PIK3CD) Successful Target
UniProt ID PK3CD_HUMAN
Gene Name 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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Representative Drug(s) GDC-0032 Drug Info Ki = 0.12 nM Click to Show More [2]
2 IPI-145 Drug Info IC50 < 0.5 nM [7]
3 BAY 80-6946 Drug Info IC50 < 0.7 nM [9]
4 GSK2126458 Drug Info IC50 = 2.5 nM [12]
5 ZSTK474 Drug Info IC50 = 3 nM [14]
6 GDC0941 Drug Info IC50 = 3 nM [15]
7 BEZ235 Drug Info IC50 = 5 nM [18]
8 PF-05212384 Drug Info IC50 = 6 nM [20]
9 Umbralisib Drug Info IC50 = 6.2 nM [21]
10 GDC-0980/RG7422 Drug Info IC50 = 6.7 nM [17]
11 AZD8186 Drug Info IC50 = 12 nM [24]
12 IPI-549 Drug Info IC50 = 23 nM [21]
13 XL147 Drug Info IC50 = 36 nM [1]
14 VS-5584 Drug Info IC50 = 37 nM [25]
15 SAR245409 Drug Info IC50 = 43 nM [6]
16 Buparlisib Drug Info IC50 = 110 nM [31]
17 TG100-115 Drug Info IC50 = 235 nM [32]
18 PQR309 Drug Info IC50 = 451 nM [31]
19 PA-799 Drug Info IC50 = 500 nM [34]
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) GSK2126458 Drug Info IC50 = 0.18 nM Click to Show More [3]
2 PF-05212384 Drug Info IC50 = 0.4 nM [5]
3 BEZ235 Drug Info IC50 = 1.43 nM [10]
4 GDC0941 Drug Info IC50 = 3 nM [6]
5 PF-04691502 Drug Info IC50 = 7.9 nM [23]
6 GDC-0980/RG7422 Drug Info Ki = 17 nM [17]
7 BAY 80-6946 Drug Info IC50 = 45 nM [29]
8 PQR309 Drug Info Ki = 62 nM [26]
9 GDC-0084 Drug Info Ki = 70 nM [11]
10 Buparlisib Drug Info IC50 = 94 nM [31]
11 SAR245409 Drug Info IC50 = 157 nM [6]
12 ZSTK474 Drug Info IC50 = 350 nM [33]
13 CUDC-907 Drug Info IC50 = 431 nM [4]
Co-Target Name Histone deacetylase 1 (HDAC1) Successful Target
UniProt ID HDAC1_HUMAN
Gene Name HDAC1
Synonyms
RPD3L1; HD1
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Representative Drug(s) CUDC-907 Drug Info IC50 = 0.36 nM [4]
Co-Target Name Histone deacetylase (HDAC) Successful Target
UniProt ID HDAC1_HUMAN; HDAC2_HUMAN; HDAC3_HUMAN; HDAC4_HUMAN; HDAC5_HUMAN; HDAC6_HUMAN; HDAC7_HUMAN; HDAC8_HUMAN; HDAC9_HUMAN; HDA10_HUMAN; HDA11_HUMAN
Gene Name NO-GeName
Synonyms
Human histone deacetylase
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Representative Drug(s) CUDC-907 Drug Info IC50 = 6.8 nM [22]
Co-Target Name Fms-like tyrosine kinase 3 (FLT-3) Successful Target
UniProt ID FLT3_HUMAN
Gene Name FLT3
Synonyms
Stem cell tyrosine kinase 1; STK1; STK-1; Receptor-type tyrosine-protein kinase FLT3; Fetal liver kinase-2; FLT-3; FLK2; FLK-2; FL cytokine receptor; CD135
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Representative Drug(s) VX-970 Drug Info Ki = 18 nM [27]
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) VX-970 Drug Info Ki = 33 nM [27]
Co-Target Name Tyrosine-protein kinase Kit (KIT) Successful Target
UniProt ID KIT_HUMAN
Gene Name KIT
Synonyms
v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog; p145 c-kit; Proto-oncogene tyrosine-protein kinase Kit; Proto-oncogene c-Kit; Piebald trait protein; PBT; Mast/stem cell growth factor receptor Kit; CD117 antigen; CD117; C-kit
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Representative Drug(s) VX-970 Drug Info Ki = 39 nM [27]
Co-Target Name Protein kinase C alpha (PRKCA) Successful Target
UniProt ID KPCA_HUMAN
Gene Name PRKCA
Synonyms
Protein kinase C alpha type; PRKACA; PKCalpha; PKCA; PKC-alpha; PKC-A
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Representative Drug(s) Enzastaurin Drug Info IC50 = 39 nM [28]
Co-Target Name Tyrosine-protein kinase ABL1 (ABL) Successful Target
UniProt ID ABL1_HUMAN
Gene Name ABL1
Synonyms
p150; Proto-oncogene tyrosine-protein kinase ABL1; Proto-oncogene c-Abl; JTK7; C-ABL; Abl; Abelson tyrosine-protein kinase 1; Abelson murine leukemia viral oncogene homolog 1
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Representative Drug(s) VX-970 Drug Info Ki = 59 nM [27]
Co-Target Name Protein kinase C gamma (PRKCG) Successful Target
UniProt ID KPCG_HUMAN
Gene Name PRKCG
Synonyms
PRKCG; PKCG; PKC-gamma
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Representative Drug(s) Enzastaurin Drug Info IC50 = 83 nM [28]
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) Enzastaurin Drug Info IC50 = 110 nM [28]
Co-Target Name Tyrosine-protein kinase SYK (SYK) Successful Target
UniProt ID KSYK_HUMAN
Gene Name SYK
Synonyms
p72-Syk; Spleen tyrosine kinase
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Representative Drug(s) GDC-0980/RG7422 Drug Info IC50 = 134 nM Click to Show More [17]
2 VX-970 Drug Info Ki = 190 nM [27]
Co-Target Name Janus kinase 2 (JAK-2) Successful Target
UniProt ID JAK2_HUMAN
Gene Name JAK2
Synonyms
Tyrosine-protein kinase JAK2
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Representative Drug(s) VX-970 Drug Info Ki = 150 nM [27]
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) BEZ235 Drug Info IC50 = 1000 nM [35]
Co-Target Name Serine/threonine-protein kinase ATR (FRP1) Clinical trial Target
UniProt ID ATR_HUMAN
Gene Name ATR
Synonyms
FRAP-related protein 1; Ataxia telangiectasia and Rad3-related protein
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Representative Drug(s) VX-970 Drug Info Ki = 0.165 nM [27]
Co-Target Name Mammalian target of rapamycin complex 1 (mTORC1) Clinical trial Target
UniProt ID MTOR_HUMAN-RPTOR_HUMAN-LST8_HUMAN-AKTS1_HUMAN-DPTOR_HUMAN
Gene Name MTOR-RPTORA-MLST8-KT1S1-DEPTOR
Synonyms
mTORC1; Mechanistic target of rapamycin complex 1
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Representative Drug(s) GSK2126458 Drug Info Ki = 0.18 nM Click to Show More [1]
2 BEZ235 Drug Info IC50 = 44 nM [42]
3 PQR309 Drug Info IC50 = 205 nM [44]
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) GSK2126458 Drug Info IC50 = 1.2 nM Click to Show More [12]
2 GDC0941 Drug Info IC50 = 3 nM [6]
3 AZD8186 Drug Info IC50 = 3 nM [24]
4 BAY 80-6946 Drug Info IC50 = 3.7 nM [6]
5 ZSTK474 Drug Info IC50 = 4.8 nM [37]
6 BEZ235 Drug Info IC50 = 6 nM [16]
7 PF-05212384 Drug Info IC50 = 6 nM [20]
8 GDC-0032 Drug Info Ki = 9.1 nM [2]
9 CUDC-907 Drug Info IC50 = 16 nM [4]
10 GDC-0980/RG7422 Drug Info IC50 = 27 nM [17]
11 BGT226 Drug Info IC50 = 63 nM [16]
12 VS-5584 Drug Info IC50 = 68 nM [25]
13 IPI-549 Drug Info IC50 = 82 nM [21]
14 IPI-145 Drug Info IC50 = 85 nM [21]
15 SAR245409 Drug Info IC50 = 113 nM [6]
16 PA-799 Drug Info IC50 = 120 nM [1]
17 Buparlisib Drug Info IC50 = 165.96 nM [43]
18 XL147 Drug Info IC50 = 383 nM [1]
19 PQR309 Drug Info IC50 = 661 nM [31]
Co-Target Name Histone deacetylase 2 (HDAC2) Clinical trial Target
UniProt ID HDAC2_HUMAN
Gene Name HDAC2
Synonyms
HD2
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Representative Drug(s) CUDC-907 Drug Info IC50 = 1.6 nM [4]
Co-Target Name Histone deacetylase 3 (HDAC3) Clinical trial Target
UniProt ID HDAC3_HUMAN
Gene Name HDAC3
Synonyms
SMAP45; RPD32; RPD3-2; HD3
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Representative Drug(s) CUDC-907 Drug Info IC50 = 1.8 nM [36]
Co-Target Name Protein kinase C beta (PRKCB) Clinical trial Target
UniProt ID KPCB_HUMAN
Gene Name PRKCB
Synonyms
Protein kinase C beta type; PRKCB1; PKCB; PKC-beta; PKC-B
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Representative Drug(s) Enzastaurin Drug Info IC50 = 6 nM [28]
Co-Target Name ATM serine/threonine kinase (ATM) Clinical trial Target
UniProt ID ATM_HUMAN
Gene Name ATM
Synonyms
Serine-protein kinase ATM; Ataxia telangiectasia mutated; A-T mutated
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Representative Drug(s) BEZ235 Drug Info IC50 = 7 nM Click to Show More [38]
2 VX-970 Drug Info Ki = 44 nM [27]
Co-Target Name Vascular endothelial growth factor receptor 3 (FLT-4) Clinical trial Target
UniProt ID VGFR3_HUMAN
Gene Name FLT4
Synonyms
VEGFR3; VEGFR-3; VEGF-3 receptor; Tyrosine-protein kinase receptor FLT4; Fms-like tyrosine kinase 4
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Representative Drug(s) VX-970 Drug Info Ki = 8 nM [27]
Co-Target Name Histone deacetylase 6 (HDAC6) Clinical trial Target
UniProt ID HDAC6_HUMAN
Gene Name HDAC6
Synonyms
KIAA0901; JM21; HD6
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Representative Drug(s) CUDC-907 Drug Info IC50 = 8 nM [4]
Co-Target Name Polo-like kinase 1 (PLK1) Clinical trial Target
UniProt ID PLK1_HUMAN
Gene Name PLK1
Synonyms
Serine/threonine-protein kinase PLK1; Serine/threonine-protein kinase 13; Serine-threonine protein kinase 13; STPK13; Plk1; PLK-1; PLK; Mitoticserine-threonine kinase polo-like kinase 1
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Representative Drug(s) Rigosertib Drug Info IC50 = 9 nM [39]
Co-Target Name RAC-alpha serine/threonine-protein kinase (AKT1) Clinical trial Target
UniProt ID AKT1_HUMAN
Gene Name AKT1
Synonyms
RAC-PK-alpha; RAC; Proto-oncogene c-Akt; Protein kinase B alpha; PKB alpha
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Representative Drug(s) PF-04691502 Drug Info IC50 = 13 nM Click to Show More [40]
2 GDC0941 Drug Info IC50 = 28 nM [41]
Co-Target Name Mixed lineage kinase 1 (MAP3K9) Clinical trial Target
UniProt ID M3K9_HUMAN
Gene Name MAP3K9
Synonyms
PRKE1; Mitogen-activated protein kinase kinase kinase 9; MLK1
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Representative Drug(s) VX-970 Drug Info Ki = 15 nM Click to Show More [27]
2 GDC-0980/RG7422 Drug Info IC50 = 232 nM [17]
Co-Target Name Tyrosine-protein kinase Mer (MERTK) Clinical trial Target
UniProt ID MERTK_HUMAN
Gene Name MERTK
Synonyms
Receptor tyrosine kinase MerTK; Proto-oncogene c-Mer
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Representative Drug(s) VX-970 Drug Info Ki = 30 nM [27]
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) VX-970 Drug Info Ki = 140 nM [27]
Co-Target Name Histone deacetylase 4 (HDAC4) Clinical trial Target
UniProt ID HDAC4_HUMAN
Gene Name HDAC4
Synonyms
KIAA0288; HD4
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Representative Drug(s) CUDC-907 Drug Info IC50 = 191 nM [36]
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) Enzastaurin Drug Info IC50 = 1000 nM [45]
Co-Target Name Histone deacetylase 8 (HDAC8) Patented-recorded Target
UniProt ID HDAC8_HUMAN
Gene Name HDAC8
Synonyms
Histone deacetylase-8; HDACL1; HD8; CDA07
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Representative Drug(s) CUDC-907 Drug Info IC50 = 1.4 nM [4]
Co-Target Name Histone deacetylase 10 (HDAC10) Patented-recorded Target
UniProt ID HDA10_HUMAN
Gene Name HDAC10
Synonyms
Polyamine deacetylase HDAC10; HD10
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Representative Drug(s) CUDC-907 Drug Info IC50 = 2.8 nM [46]
Co-Target Name Histone deacetylase 11 (HDAC11) Patented-recorded Target
UniProt ID HDA11_HUMAN
Gene Name HDAC11
Synonyms
HD11
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Representative Drug(s) CUDC-907 Drug Info IC50 = 5.4 nM [22]
Co-Target Name Dual-specificity tyrosine-phosphorylation regulated kinase 2 (DYRK2) Patented-recorded Target
UniProt ID DYRK2_HUMAN
Gene Name DYRK2
Synonyms
Dual specificity tyrosine-phosphorylation-regulated kinase 2
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Representative Drug(s) VX-970 Drug Info Ki = 26 nM [27]
Co-Target Name Histone deacetylase 7 (HDAC7) Patented-recorded Target
UniProt ID HDAC7_HUMAN
Gene Name HDAC7
Synonyms
Histone deacetylase 7A; HDAC7A; HD7a; HD7
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Representative Drug(s) CUDC-907 Drug Info IC50 = 27 nM [36]
Co-Target Name Histone deacetylase 5 (HDAC5) Patented-recorded Target
UniProt ID HDAC5_HUMAN
Gene Name HDAC5
Synonyms
KIAA0600; HD5; Antigen NY-CO-9
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Representative Drug(s) CUDC-907 Drug Info IC50 = 406 nM [36]
Co-Target Name Histone deacetylase 9 (HDAC9) Patented-recorded Target
UniProt ID HDAC9_HUMAN
Gene Name HDAC9
Synonyms
MITR; MEF2-interacting transcription repressor MITR; KIAA0744; Histone deacetylase-related protein; Histone deacetylase 7B; HDRP; HDAC7B; HDAC7; HD9; HD7b
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Representative Drug(s) CUDC-907 Drug Info IC50 = 554 nM [22]
Co-Target Name Tyrosine-protein kinase Fgr (FGR) Literature-reported Target
UniProt ID FGR_HUMAN
Gene Name FGR
Synonyms
p58c-Fgr; p58-Fgr; p55-Fgr; SRC2; Proto-oncogene c-Fgr; Gardner-Rasheed feline sarcoma viral (v-fgr) oncogene homolog
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Representative Drug(s) GDC-0980/RG7422 Drug Info IC50 = 697 nM [17]
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) GSK2126458 Drug Info IC50 = 0.019 nM Click to Show More [3]
2 BAY 80-6946 Drug Info IC50 = 0.11 nM [47]
3 BEZ235 Drug Info IC50 = 4 nM [50]
4 GDC0941 Drug Info IC50 = 4.8 nM [49]
5 ZSTK474 Drug Info IC50 = 5 nM [9]
6 Buparlisib Drug Info IC50 = 11 nM [51]
7 PQR309 Drug Info Ki = 17 nM [44]
8 CUDC-907 Drug Info IC50 = 19 nM [36]
9 VX-970 Drug Info Ki = 140 nM [27]
10 IPI-145 Drug Info IC50 = 400 nM [54]
Co-Target Name PI3K p110 delta/p85 alpha (PIK3CD/PIK3R1) Co-Target
UniProt ID PK3CD_HUMAN-P85A_HUMAN
Gene Name PIK3CD-PIK3R1
Representative Drug(s) BAY 80-6946 Drug Info IC50 = 0.18 nM Click to Show More [47]
2 IPI-145 Drug Info IC50 = 1 nM [48]
3 GDC0941 Drug Info IC50 = 3.3 nM [49]
4 ZSTK474 Drug Info IC50 = 3.9 nM [9]
5 BEZ235 Drug Info IC50 = 22 nM [16]
6 CUDC-907 Drug Info IC50 = 39 nM [46]
7 Buparlisib Drug Info IC50 = 125 nM [51]
Co-Target Name Histone deacetylase 3-Nuclear receptor corepressor 2 complex (HDAC3-NCOR2) Co-Target
UniProt ID HDAC3_HUMAN-NCOR2_HUMAN
Gene Name HDAC3-NCOR2
Representative Drug(s) CUDC-907 Drug Info IC50 = 1.8 nM [22]
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 [47]
2 IPI-145 Drug Info IC50 = 8 nM [48]
3 BEZ235 Drug Info IC50 = 16.23 nM [52]
4 GDC0941 Drug Info IC50 = 54 nM [46]
5 CUDC-907 Drug Info IC50 = 54 nM [46]
6 Buparlisib Drug Info IC50 = 234 nM [51]
Co-Target Name Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alpha (PIK3C2A) Co-Target
UniProt ID P3C2A_HUMAN
Gene Name PIK3C2A
Synonyms
PI3K-C2-alpha; PtdIns-3-kinase C2 subunit alpha; Phosphoinositide 3-kinase-C2-alpha
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Representative Drug(s) BEZ235 Drug Info IC50 = 34 nM [53]
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) BEZ235 Drug Info IC50 = 44 nM Click to Show More [53]
2 ZSTK474 Drug Info IC50 = 180 nM [53]
3 GDC-0032 Drug Info IC50 = 292 nM [2]
4 GDC0941 Drug Info IC50 = 590 nM [53]
5 GDC-0980/RG7422 Drug Info IC50 = 794 nM [17]
Co-Target Name mTORC2 Co-Target
UniProt ID MTOR_HUMAN; RICTR_HUMAN; SIN1_HUMAN; LST8_HUMAN
Gene Name MTOR; RICTOR; MAPKAP1; MLST8
Synonyms
mTOR Complex 2; Mechanistic target of Rapamycin 2
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Representative Drug(s) PQR309 Drug Info IC50 = 139 nM [44]
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) GDC-0032 Drug Info IC50 = 374 nM Click to Show More [2]
2 BEZ235 Drug Info IC50 = 450 nM [53]
Co-Target Name Protein kinase C eta (PRKCH) Co-Target
UniProt ID KPCL_HUMAN
Gene Name PRKCH
Synonyms
Protein kinase C eta type; PKC-L; nPKC-eta
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Representative Drug(s) Enzastaurin Drug Info IC50 = 400 nM [45]
References  Top
REF 1 Small molecules targeting phosphoinositide 3-kinases. Medchemcomm. 2012;3:1337-55.
REF 2 Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a beta-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity. J Med Chem. 2013 Jun 13;56(11):4597-610.
REF 3 Design, synthesis and SAR of new-di-substituted pyridopyrimidines as ATP-competitive dual PI3Kalpha/mTOR inhibitors. Bioorg Med Chem Lett. 2017 Jul 15;27(14):3117-22.
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 Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors. Bioorg Med Chem Lett. 2011 Aug 15;21(16):4773-8.
REF 6 Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer. Eur J Med Chem. 2019 Dec 1;183:111718.
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