Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
AZD-5363, a novel pyrrolopyrimidine-derived compound, inhibits all AKT isoforms with a potency of <10nM, and inhibited phosphorylation of AKT substrates in cells with a potency of ~0.3 to 0.8µM. AZD5363 monotherapy inhibited the proliferation of 4...
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Ipatasertib, an investigational Akt inhibitor, is currently in clinical development based on its potential to specifically target Akt in tumors with activated Akt signaling. Preclinical data have shown that ipatasertib selectively decreased cell viab...
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
GSK690693 is an aminofurazan derivative, a novel ATP-competitive, low-nanomolar pan-Akt kinase inhibitor. It is selective for the Akt isoforms versus the majority of kinases in other families; however, it does inhibit additional members of the AGC ki...
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
BAY-1125976 is an orally bioavailable inhibitor of the serine/threonine protein kinase AKT (protein kinase B) isoforms 1 and 2 (AKT1/2) with potential antineoplastic activity. AKT1/2 inhibitor BAY1125976 selectively binds to and inhibits the phosphor...
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Uprosertib is an oral potent Akt inhibitor which acts equally on Akt1, Akt2 and Akt3. The drug is under clinical development in combination with trametinib for the treatment of different cancers, including melanoma, myeloma, breast, endometrial, cerv...
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
MK-2206 is an oral selective allosteric inhibitor of Akt that targets all three isoforms of human Akt (Akt-1, Akt-2 and Akt-3). In a phase I study of solid tumors, MK-2206 demonstrated evidence of target modulation and anti-proliferative activity as ...
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Miransertib (ARQ 092) is a selective, pan-AKT (protein kinase B) inhibitor that potently inhibits AKT1, 2 and 3 isoforms. Miransertib binds inactive AKT, preventing membrane localization and subsequent AKT activation, and binds active AKT, resulting ...
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Afuresertib (GSK2110183 ) is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Afuresertib binds to and inhibits the activity of Akt, which may result in inhibition ...
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
AT7867 is a novel and potent inhibitor of both AKT and the downstream kinase p70 S6 kinase (p70S6K) and also of protein kinase A. This ATP-competitive small molecule potently inhibits both AKT and p70S6K activity at the cellular level, as measured by...