Target family: Akt (Protein kinase B, PKB) family (type: enzyme)
Target: AKT serine/threonine kinase 3

Ligand: A-443654 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
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: afuresertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.59000015258789 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: no
Median affinity: 5.670000076293945 pIC50
Reference (Journal): Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: capivasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2023)
Primary target: yes
Median affinity: 8.100000381469727 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: no
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: 8.770000457763672 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: 8.050000190734863 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: ipatasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.100000381469727 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: miransertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 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: 7.800000190734863 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: 7.190000057220459 pIC50
Reference (Journal): MK-2206: a potent oral allosteric AKT inhibitor.[Abstract].
Published in: AACR Annual Meeting 2009

Ligand: MK-2206 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: yes
Median affinity: 7.190000057220459 pIC50
Reference (Webpage): Abstract #DDT01-1: MK-2206: A potent oral allosteric AKT inhibitor.

Ligand: MS15 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.260000228881836 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: 10 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: pifusertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.360000133514404 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: 8.819999694824219 pKi
Reference (Journal): Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor.
Published in: PLoS ONE