Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T67619 Target Info
Target Name RAC-alpha serine/threonine-protein kinase (AKT1)
Synonyms
RAC-PK-alpha; RAC; Proto-oncogene c-Akt; Protein kinase B alpha; PKB alpha
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Target Type Successful Target
Gene Name AKT1
Biochemical Class Kinase
UniProt ID
AKT1_HUMAN
Co-Targets of This Target  Top
Co-Target Name Epidermal growth factor receptor (EGFR) Successful Target
UniProt ID EGFR_HUMAN
Gene Name EGFR
Synonyms
Receptor tyrosine-protein kinase erbB-1; Proto-oncogene c-ErbB-1; HER1; ERBB1; ERBB
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Representative Drug(s) CI-1033 Drug Info Ki = 0.11 nM [1]
Co-Target Name Insulin receptor (INSR) Successful Target
UniProt ID INSR_HUMAN
Gene Name INSR
Synonyms
IR; CD220 antigen; CD220
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Representative Drug(s) BMS-754807 Drug Info IC50 = 1.7 nM [2]
Co-Target Name Insulin-like growth factor I receptor (IGF1R) Successful Target
UniProt ID IGF1R_HUMAN
Gene Name IGF1R
Synonyms
Type 1 insulin-like growth factor receptor; Insulin-like growth factor 1 receptor; IGF-IR; IGF-I receptor; IGF-1R; IGF-1 receptor; CD221 antigen; CD221
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Representative Drug(s) BMS-754807 Drug Info IC50 = 1.8 nM [2]
Co-Target Name BDNF/NT-3 growth factors receptor (TrkB) Successful Target
UniProt ID NTRK2_HUMAN
Gene Name NTRK2
Synonyms
Tropomyosin-related kinase B; TrkB tyrosine kinase; Trk-B; TRKB; Neurotrophic tyrosine kinase receptor type 2; GP145-TrkB
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Representative Drug(s) BMS-754807 Drug Info IC50 = 4 nM [2]
Co-Target Name Erbb2 tyrosine kinase receptor (HER2) Successful Target
UniProt ID ERBB2_HUMAN
Gene Name ERBB2
Synonyms
p185erbB2; Tyrosine kinase-type cell surface receptor HER2; Receptor tyrosine-protein kinase erbB-2; Proto-oncogene c-ErbB-2; Proto-oncogene Neu; NGL; NEU; Metastatic lymph node gene 19 protein; MLN19; MLN 19; HER2; CD340
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Representative Drug(s) CI-1033 Drug Info IC50 = 5 nM [3]
Co-Target Name Tropomyosin-related kinase A (TrkA) Successful Target
UniProt ID NTRK1_HUMAN
Gene Name NTRK1
Synonyms
gp140trk; Tyrosine kinase receptor A; Tyrosine kinase receptor; Trk-A; TRKA; TRK1-transforming tyrosine kinase protein; TRK1 transforming tyrosinekinase protein; TRK; P140-TrkA; Neurotrophic tyrosine kinase receptor type 1; NGF-trk receptor type A; MTC; High affinity nerve growth factor receptor
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Representative Drug(s) BMS-754807 Drug Info IC50 = 7 nM [2]
Co-Target Name Erbb4 tyrosine kinase receptor (Erbb-4) Successful Target
UniProt ID ERBB4_HUMAN
Gene Name ERBB4
Synonyms
Tyrosine kinase-type cell surface receptor HER4; Receptor tyrosine-protein kinase erbB-4; Proto-oncogene-like protein c-ErbB-4; P180erbB4; HER4
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Representative Drug(s) CI-1033 Drug Info IC50 = 10 nM [3]
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 [4]
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 [4]
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 [4]
Co-Target Name Tyrosine-protein kinase BTK (ATK) Successful Target
UniProt ID BTK_HUMAN
Gene Name BTK
Synonyms
Bruton's tyrosine kinase; Bruton tyrosine kinase; BPK; B-cell progenitor kinase; B cell progenitor kinase; Agammaglobulinemia tyrosine kinase; Agammaglobulinaemia tyrosine kinase; AGMX1
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Representative Drug(s) CI-1033 Drug Info IC50 = 185 nM [5]
Co-Target Name Rho-associated protein kinase 1 (ROCK1) Successful Target
UniProt ID ROCK1_HUMAN
Gene Name ROCK1
Synonyms
Rok; Rho-associated, coiled-coil containing protein kinase 1; Rho-associated kinase 1; Rho kinase; ROCK1; ROCK; P160ROCK; P160(rock); P160 ROCK-1; Let-502 kinase
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Representative Drug(s) Capivasertib Drug Info IC50 = 470 nM [6]
Co-Target Name RAC-gamma serine/threonine-protein kinase (AKT3) Clinical trial Target
UniProt ID AKT3_HUMAN
Gene Name AKT3
Synonyms
STK-2; RAC-PK-gamma; Protein kinase B gamma; Protein kinase Akt-3; PKBG; PKB gamma
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Representative Drug(s) GSK2110183 Drug Info IC50 = 1.585 nM Click to Show More [7]
2 GDC-0068 Drug Info IC50 = 8 nM [9]
3 Capivasertib Drug Info IC50 = 8 nM [6]
Co-Target Name ERK activator kinase 1 (MEK1) Clinical trial Target
UniProt ID MP2K1_HUMAN
Gene Name MAP2K1
Synonyms
PRKMK1; Mitogen-activated protein kinase kinase 1; MKK1; MEK 1; MAPKK 1; MAPK/ERKkinase 1; MAPK/ERK kinase 1; MAP kinase kinase 1; Dual specificity mitogen-activated protein kinase kinase 1
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Representative Drug(s) CI-1040 Drug Info IC50 = 2 nM [8]
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 [4]
Co-Target Name Proto-oncogene c-RAF (c-RAF) Clinical trial Target
UniProt ID RAF1_HUMAN
Gene Name RAF1
Synonyms
cRaf; Raf-1; RAF proto-oncogene serine/threonine-protein kinase; RAF
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Representative Drug(s) CI-1040 Drug Info IC50 = 12 nM [10]
Co-Target Name Casein kinase II alpha (CSNK2A1) Clinical trial Target
UniProt ID CSK21_HUMAN
Gene Name CSNK2A1
Synonyms
Protein kinase CK2; Casein kinase II subunit alpha; CK2A1; CK II alpha; CK II
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Representative Drug(s) CI-1040 Drug Info IC50 = 17 nM [11]
Co-Target Name Rho-associated protein kinase 2 (ROCK2) Successful Target
UniProt ID ROCK2_HUMAN
Gene Name ROCK2
Synonyms
p164 ROCK-2; Rho-associated, coiled-coil-containing protein kinase II; Rho-associated, coiled-coil-containing protein kinase 2; Rho kinase 2; ROCK-II; KIAA0619
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Representative Drug(s) Capivasertib Drug Info IC50 = 56 nM [6]
Co-Target Name Casein kinase II (CSNK2) Clinical trial Target
UniProt ID CSK21_HUMAN; CSK22_HUMAN; CSK23_HUMAN; CSK2B_HUMAN
Gene Name NO-GeName
Representative Drug(s) CI-1040 Drug Info EC50 = 100 nM [11]
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 [12]
Co-Target Name B lymphocyte kinase (BLK) Patented-recorded Target
UniProt ID BLK_HUMAN
Gene Name BLK
Synonyms
p55-Blk; Tyrosine-protein kinase Blk
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Representative Drug(s) CI-1033 Drug Info IC50 = 29 nM [5]
Co-Target Name Tyrosine-protein kinase BMX (BMX) Patented-recorded Target
UniProt ID BMX_HUMAN
Gene Name BMX
Synonyms
NTK38; Epithelial and endothelial tyrosine kinase; ETK; Cytoplasmic tyrosine-protein kinase BMX; Bone marrow tyrosine kinase gene in chromosome X protein
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Representative Drug(s) CI-1033 Drug Info IC50 = 62 nM [5]
Co-Target Name RAC-beta serine/threonine-protein kinase (AKT2) Literature-reported Target
UniProt ID AKT2_HUMAN
Gene Name AKT2
Synonyms
RAC-PK-beta; Protein kinase B beta; Protein kinase Akt-2; PKB beta
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Representative Drug(s) Capivasertib Drug Info IC50 = 8 nM Click to Show More [6]
2 GSK2110183 Drug Info IC50 = 10 nM [7]
3 GDC-0068 Drug Info IC50 = 18 nM [9]
Co-Target Name Protein kinase G1 (PRKG1) Literature-reported Target
UniProt ID KGP1_HUMAN
Gene Name PRKG1
Synonyms
cGMP-dependent protein kinase I; cGMP-dependent protein kinase 1; cGKI; cGK1; cGK 1; PRKGR1B; PRKGR1A; PRKG1B
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Representative Drug(s) GDC-0068 Drug Info IC50 = 69 nM [9]
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 [12]
References  Top
REF 1 Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants. J Med Chem. 2016 Mar 10;59(5):2005-24.
REF 2 Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application. J Med Chem. 2019 Feb 28;62(4):1731-1760.
REF 3 Irreversible protein kinase inhibitors: balancing the benefits and risks. J Med Chem. 2012 Jul 26;55(14):6243-62.
REF 4 Synthesis and anticancer activity of novel bisindolylhydroxymaleimide derivatives with potent GSK-3 kinase inhibition. Bioorg Med Chem. 2018 Aug 7;26(14):4209-24.
REF 5 Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. Bioorg Med Chem Lett. 2008 Nov 15;18(22):5916-9.
REF 6 Discovery of 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an orally bioavailable, potent inhibitor of Akt kinases. J Med Chem. 2013 Mar 14;56(5):2059-73.
REF 7 US patent application no. 20110071182A1, Inhibitors of AKT Activity
REF 8 Synthesis and evaluation of 4-anilino-6,7-dialkoxy-3-quinolinecarbonitriles as inhibitors of kinases of the Ras-MAPK signaling cascade. Bioorg Med Chem Lett. 2003 Sep 15;13(18):3031-4.
REF 9 Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors. J Med Chem. 2012 Sep 27;55(18):8110-27.
REF 10 Pharmacophore identification of Raf-1 kinase inhibitors. Bioorg Med Chem Lett. 2008 Apr 1;18(7):2346-50.
REF 11 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action. J Med Chem. 2019 Feb 28;62(4):1817-1836.
REF 12 Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta. Bioorg Med Chem Lett. 2003 Jun 2;13(11):1857-9.

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