Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T71266 Target Info
Target Name RAC-gamma serine/threonine-protein kinase (AKT3)
Synonyms
STK-2; RAC-PK-gamma; Protein kinase B gamma; Protein kinase Akt-3; PKBG; PKB gamma
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Target Type Successful Target
Gene Name AKT3
Biochemical Class Kinase
UniProt ID
AKT3_HUMAN
Co-Targets of This Target  Top
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) GSK690693 Drug Info IC50 = 21 nM [1]
Co-Target Name Human immunodeficiency virus Reverse transcriptase (HIV RT) Successful Target
UniProt ID POL_HV1B1
Gene Name HIV RT
Synonyms
HIV p66 RT; HIV Exoribonuclease H
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Representative Drug(s) TCN-P Drug Info IC50 = 40 nM [2]
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) GSK2141795 Drug Info IC50 = 125 nM Click to Show More [3]
2 Capivasertib Drug Info IC50 = 470 nM [4]
3 GSK690693 Drug Info IC50 = 890 nM [1]
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) GSK2110183 Drug Info Ki = 0.08 nM Click to Show More [5]
2 GSK690693 Drug Info IC50 = 0.6 nM [6]
3 XL418 Drug Info IC50 = 1 nM [7]
4 Capivasertib Drug Info IC50 = 3 nM [4]
5 GSK2141795 Drug Info IC50 = 4.7 nM [3]
6 MK-2206 Drug Info IC50 = 8 nM [8]
Co-Target Name Protein kinase C theta (PRKCQ) Clinical trial Target
UniProt ID KPCT_HUMAN
Gene Name PRKCQ
Synonyms
Protein kinase C theta type; PRKCT; NPKC-theta
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Representative Drug(s) GSK690693 Drug Info IC50 = 2 nM [1]
Co-Target Name Ribosomal protein S6 kinase beta-1 (S6K1) Clinical trial Target
UniProt ID KS6B1_HUMAN
Gene Name RPS6KB1
Synonyms
p70-S6K 1; p70 ribosomal S6 kinase alpha; p70 S6KA; p70 S6K-alpha; p70 S6 kinase alpha; Serine/threonine-protein kinase 14A; STK14A; S6K-beta-1; S6K; Ribosomal protein S6 kinase I; P70S6K1; P70-S6K; 70 kDa ribosomal protein S6 kinase 1
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Representative Drug(s) XL418 Drug Info IC50 = 2 nM Click to Show More [7]
2 GSK2141795 Drug Info IC50 = 60 nM [3]
Co-Target Name PAK-4 protein kinase (PAK4) Clinical trial Target
UniProt ID PAK4_HUMAN
Gene Name PAK4
Synonyms
p21-activated kinase 4; Serine/threonine-protein kinase PAK 4; PAK-4; KIAA1142
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Representative Drug(s) GSK690693 Drug Info IC50 = 10 nM [1]
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) GSK690693 Drug Info IC50 = 14 nM [1]
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) GSK690693 Drug Info IC50 = 19 nM [1]
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 [4]
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) GSK690693 Drug Info IC50 = 138 nM [9]
Co-Target Name Serine/threonine-protein kinase Sgk1 (SGK1) Clinical trial Target
UniProt ID SGK1_HUMAN
Gene Name SGK1
Synonyms
Serum/glucocorticoid-regulated kinase 1; SGK1
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Representative Drug(s) GSK2141795 Drug Info IC50 = 211 nM [3]
Co-Target Name Protein kinase C (PRKC) Clinical trial Target
UniProt ID KPCA_HUMAN; KPCB_HUMAN; KPCD1_HUMAN; KPCD3_HUMAN; KPCD_HUMAN; KPCE_HUMAN; KPCG_HUMAN; KPCI_HUMAN; KPCL_HUMAN; KPCT_HUMAN; KPCZ_HUMAN
Gene Name NO-GeName
Representative Drug(s) GSK2141795 Drug Info IC50 = 753 nM [3]
Co-Target Name Ribosomal protein S6 kinase alpha-1 (RSK1) Patented-recorded Target
UniProt ID KS6A1_HUMAN
Gene Name RPS6KA1
Synonyms
p90S6K; p90RSK1; p90-RSK 1; S6K-alpha-1; Ribosomal S6 kinase 1; RSK-1; MAPKAPK1A; MAPKAPK-1a; MAPKAP kinase 1a; MAPK-activated protein kinase 1a; MAP kinase-activated protein kinase 1a; 90 kDa ribosomal protein S6 kinase 1
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Representative Drug(s) GSK2141795 Drug Info IC50 = 339 nM [3]
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) GSK2141795 Drug Info IC50 = 1 nM Click to Show More [3]
2 GSK690693 Drug Info Ki = 4 nM [9]
3 Capivasertib Drug Info IC50 = 8 nM [4]
4 MK-2206 Drug Info IC50 = 12 nM [8]
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) GSK690693 Drug Info IC50 = 33 nM [1]
Co-Target Name Death-associated protein kinase 3 (DAPK3) Literature-reported Target
UniProt ID DAPK3_HUMAN
Gene Name DAPK3
Synonyms
Zipper-interacting protein kinase; ZIPK; ZIP-kinase; MYPT1 kinase; DAP-like kinase; DAP kinase 3
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Representative Drug(s) GSK690693 Drug Info IC50 = 81 nM [1]
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) GSK690693 Drug Info IC50 = 2 nM [1]
Co-Target Name Serine/threonine-protein kinase PRKX (PRKX) Co-Target
UniProt ID PRKX_HUMAN
Gene Name PRKX
Synonyms
cAMP-dependent protein kinase catalytic subunit PRKX; PrKX; Protein kinase X; Protein kinase X-linked; Protein kinase PKX1
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Representative Drug(s) GSK690693 Drug Info IC50 = 5 nM [1]
Co-Target Name Serine/threonine-protein kinase PAK 6 (PAK6) Co-Target
UniProt ID PAK6_HUMAN
Gene Name PAK6
Synonyms
PAK-5; p21-activated kinase 6; PAK-6
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Representative Drug(s) GSK690693 Drug Info IC50 = 6 nM [1]
Co-Target Name Serine/threonine-protein kinase PAK 5 (PAK5) Co-Target
UniProt ID PAK5_HUMAN
Gene Name PAK5
Synonyms
p21-activated kinase 5; PAK-5; p21-activated kinase 7; PAK-7
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Representative Drug(s) GSK690693 Drug Info IC50 = 52 nM [1]
References  Top
REF 1 Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-o... J Med Chem. 2008 Sep 25;51(18):5663-79.
REF 2 6-N-Acyltriciribine analogues: structure-activity relationship between acyl carbon chain length and activity against HIV-1. J Med Chem. 2000 Jun 15;43(12):2457-63.
REF 3 Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design. J Med Chem. 2019 Aug 8;62(15):7264-7288.
REF 4 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 5 Discovery of pyrazole-thiophene derivatives as highly Potent, orally active Akt inhibitors. Eur J Med Chem. 2019 Oct 15;180:72-85.
REF 6 Phenylalanine-Based Inactivator of AKT Kinase: Design, Synthesis, and Biological Evaluation. ACS Med Chem Lett. 2014 Mar 7;5(5):462-7.
REF 7 Pyrazolopyrimidines as dual Akt/p70S6K inhibitors. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2693-7.
REF 8 Selectively nonselective kinase inhibition: striking the right balance. J Med Chem. 2010 Feb 25;53(4):1413-37.
REF 9 Aminofurazans as potent inhibitors of AKT kinase. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1508-11.

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