Co-Target(s) Information
| Target General Information | Top | ||||
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| Target ID | T85544 | Target Info | |||
| Target Name | Target of rapamycin complex 2 MAPKAP1 (MTORC2) | ||||
| Synonyms |
mSIN1; Target of rapamycin complex 2 subunit MAPKAP1; TORC2 subunit MAPKAP1; Stress-activated map kinase-interacting protein 1; SIN1; SAPK-interacting protein 1; Mitogen-activated protein kinase 2-associated protein 1; MIP1
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| Target Type | Clinical trial Target | ||||
| Gene Name | MAPKAP1 | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
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| 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) | AZD2014 | Drug Info | IC50 = 2.8 nM | [1] | ||
| 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) | VS-5584 | Drug Info | IC50 = 16 nM | [2] | ||
| 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) | VS-5584 | Drug Info | IC50 = 25 nM | [2] | ||
| 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) | VS-5584 | Drug Info | IC50 = 37 nM | [2] | ||
| 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) | VS-5584 | Drug Info | IC50 = 68 nM | [2] | ||
| 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) | AZD2014 | Drug Info | IC50 = 200 nM | [1] | ||
| References | Top | ||||
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| REF 1 | Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014. Bioorg Med Chem Lett. 2013 Mar 1;23(5):1212-6. | ||||
| REF 2 | Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring. J Med Chem. 2015 Jan 8;58(1):41-71. | ||||
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