|Description||PF-AKT400 is an APT competitor inhibitor of AKR kinase. This compound was first described as compound 42 in J. Med. Chem. 2010, 53, 4615–4622 by a group of Pfizer scientists. The paper describes the design and synthesis of novel, ATP-competitive Akt inhibitors from an elaborated 3-aminopyrrolidine scaffold. Key findings include the discovery of an initial lead that was modestly selective and medicinal chemistry optimization of that lead to provide more selective analogues. Analysis of the data suggested that highly lipophilic analogues would likely suffer from poor overall properties. Central to the discussion is the concept of optimization of lipophilic efficiency and the ability to balance overall druglike propeties with the careful control of lipophilicity in the lead series. Discovery of the nonracemic amide series and subsequent modification produced an advanced analogue that performed well in advanced preclinical assays, including xenograft tumor growth inhibition studies, and this analogue was nominated for clinical development. The compound has no official name, has molecule weight 400.43. We temporally call this compound as PF-AKT400.|
|Synonyms||PF-AKT400; PFAKT400; Lig1; Lig-1; Lig 1; PF AKT400; AKT-0286; AKT 0286; AKT0286|
PHT-427 is an AKT inhibitor that inhibits AKT and PDPK1 at low micromolar concentrations in numerous cancer cell lines and exhibits good oral anti-tumor activit...
COTI-2 is an p53 gene activator and the PI3K/AKT/mTOR pathway inhibitor. COTI-2 induces apoptosis and suppresses proliferation of a wide variety of human cancer...
CCT128930 is a novel ATP-competitive AKT inhibitor discovered using fragment- and structure-based approaches. It is a potent, advanced lead pyrrolopyrimidine co...
SC66 is a novel and potent AKT inhibitor, which reduced cell viability in a dose- and time-dependent manner, inhibited colony formation and induced apoptosis in...
3CAI is an orally active, potent and specific allosteric inhibitor of Akt1 and Akt2 that directly binds to Ak1 and Akt2 in an ATP noncompetitive manner.
Afuresertib, also known as GSK2110183, is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineo...
Akt1 and Akt2-IN-1
Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 and Akt2 with the IC50 of 3.5 nM and 42 nM respectively. It has potent and balanced activity. It is depend...
MK-2206 hydrochloride is the hydrochloride form of MK-2206, which is an allosteric inhibitor of Akt and an orally bioavailable allosteric inhibitor of the serin...