Target family: Akt (Protein kinase B, PKB) family (type: enzyme)
Target: AKT serine/threonine kinase 1

Ligand: A-443654 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.800000190734863 pKi
Reference (Journal): Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo.
Published in: Mol Cancer Ther

Ligand: A-674563 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.119999885559082 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: A-674563 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.960000038146973 pKi
Reference (Journal): Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo.
Published in: Mol Cancer Ther

Ligand: afuresertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 10.100000381469727 pKi
Reference (Journal): Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor.
Published in: PLoS ONE

Ligand: Akt inhibitor VIII (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: yes
Median affinity: 7.239999771118164 pIC50
Reference (Journal): Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: BAY1125976 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 8.279999732971191 pIC50
Reference (Patent): Imidazopyridazines as Akt kinase inhibitors

Ligand: capivasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2023)
Primary target: no
Median affinity: 7.590000152587891 pIC50
Reference (Journal): Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design.
Published in: J Med Chem

Ligand: capivasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2023)
Primary target: yes
Median affinity: 8.520000457763672 pIC50
Reference (Journal): 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.
Published in: J Med Chem

Ligand: compound 1 [PMID: 20005102] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9 pIC50
Reference (Journal): 2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles.
Published in: Bioorg Med Chem Lett

Ligand: compound E22 [PMID: 31298542] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.859999656677246 pIC50
Reference (Journal): Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design.
Published in: J Med Chem

Ligand: GSK690693 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.65999984741211 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: GSK690693 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.699999809265137 pIC50
Reference (Journal): 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-ol (GSK690693), a novel inhibitor of AKT kinase.
Published in: J Med Chem

Ligand: Hu7691 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Discovery of <i>N</i>-((3<i>S</i>,4<i>S</i>)-4-(3,4-Difluorophenyl)piperidin-3-yl)-2-fluoro-4-(1-methyl-1<i>H</i>-pyrazol-5-yl)benzamide (Hu7691), a Potent and Selective Akt Inhibitor That Enables Decrease of Cutaneous Toxicity.
Published in: J Med Chem

Ligand: ipatasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9 pIC50
Reference (Journal): Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
Published in: J Med Chem

Ligand: miltefosine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2014)
Primary target: no
Median affinity: 5.019999980926514 pIC50
Reference (Journal): Synthesis, characterization and Akt phosphorylation inhibitory activity of cyclopentanecarboxylate-substituted alkylphosphocholines.
Published in: Bioorg Med Chem

Ligand: miransertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.890000343322754 pIC50
Reference (Journal): Novel Allosteric Inhibitor-Derived AKT Proteolysis Targeting Chimeras (PROTACs) Enable Potent and Selective AKT Degradation in KRAS/BRAF Mutant Cells.
Published in: J Med Chem

Ligand: miransertib (Synthetic organic)
Interaction type: Allosteric modulator
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Discovery of 3-(3-(4-(1-Aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine (ARQ 092): An Orally Bioavailable, Selective, and Potent Allosteric AKT Inhibitor.
Published in: J Med Chem

Ligand: MK-2206 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: yes
Median affinity: 8.300000190734863 pIC50
Reference (Webpage): Abstract #DDT01-1: MK-2206: A potent oral allosteric AKT inhibitor.

Ligand: MK-2206 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: yes
Median affinity: 8.300000190734863 pIC50
Reference (Journal): MK-2206: a potent oral allosteric AKT inhibitor.[Abstract].
Published in: AACR Annual Meeting 2009

Ligand: MS15 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.099999904632568 pIC50
Reference (Journal): Novel Allosteric Inhibitor-Derived AKT Proteolysis Targeting Chimeras (PROTACs) Enable Potent and Selective AKT Degradation in KRAS/BRAF Mutant Cells.
Published in: J Med Chem

Ligand: NTQ1062 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.399999618530273 pIC50
Reference (Journal): Discovery of Clinical Candidate NTQ1062 as a Potent and Bioavailable Akt Inhibitor for the Treatment of Human Tumors.
Published in: J Med Chem

Ligand: oridonin (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.079999923706055 pIC50
Reference (Journal): Targeting AKT with Oridonin Inhibits Growth of Esophageal Squamous Cell Carcinoma <i>In Vitro</i> and Patient-Derived Xenografts <i>In Vivo</i>.
Published in: Mol Cancer Ther

Ligand: pifusertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.319999694824219 pIC50
Reference (Journal): Selective and potent Akt inhibition triggers anti-myeloma activities and enhances fatal endoplasmic reticulum stress induced by proteasome inhibition.
Published in: Cancer Res

Ligand: rupitasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): M2698 is a potent dual-inhibitor of p70S6K and Akt that affects tumor growth in mouse models of cancer and crosses the blood-brain barrier.
Published in: Am J Cancer Res

Ligand: uprosertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 10.180000305175781 pKi
Reference (Journal): Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor.
Published in: PLoS ONE