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BioAssay: AID 507827

Binding affinity to AKT2

Activating mutations in the receptor tyrosine kinase FLT3 are present in up to approximately 30% of acute myeloid leukemia (AML) patients, implicating FLT3 as a driver of the disease and therefore as a target for therapy. We report the characterization of AC220, a second-generation FLT3 inhibitor, and a comparison of AC220 with the first-generation FLT3 inhibitors CEP-701, MLN-518, PKC-412, more ..
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 Tested Compounds
 Tested Compounds
All(7)
 
 
Active(3)
 
 
Unspecified(4)
 
 
 Tested Substances
 Tested Substances
All(7)
 
 
Active(3)
 
 
Unspecified(4)
 
 
 Related BioAssays
 Related BioAssays
AID: 507827
Data Source: ChEMBL (655676)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2011-09-17
Modify Date: 2014-12-06

Data Table ( Complete ):           View Active Data    View All Data
BioActive Compounds: 3
Description:
Title: AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).

Abstract: Activating mutations in the receptor tyrosine kinase FLT3 are present in up to approximately 30% of acute myeloid leukemia (AML) patients, implicating FLT3 as a driver of the disease and therefore as a target for therapy. We report the characterization of AC220, a second-generation FLT3 inhibitor, and a comparison of AC220 with the first-generation FLT3 inhibitors CEP-701, MLN-518, PKC-412, sorafenib, and sunitinib. AC220 exhibits low nanomolar potency in biochemical and cellular assays and exceptional kinase selectivity, and in animal models is efficacious at doses as low as 1 mg/kg given orally once daily. The data reveal that the combination of excellent potency, selectivity, and pharmacokinetic properties is unique to AC220, which therefore is the first drug candidate with a profile that matches the characteristics desirable for a clinical FLT3 inhibitor.
(PMID: 19654408)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.
Putative Target:
ChEMBL Target ID: 10695
Target Type: SINGLE PROTEIN
Pref Name: Serine/threonine-protein kinase AKT2
Synonyms: PKB beta;Protein kinase Akt-2;Protein kinase B beta;RAC-beta serine/threonine-protein kinase;RAC-PK-beta;
Gene Name: AKT2;
Protein Accession: P31751;
Protein GI: 1170703;
Organism: Homo sapiens
Tax ID: 9606
Target Classification: enzyme kinase protein kinase agc akt
Confidence: Homologous single protein target assigned
Relationship Type: Homologous protein target assigned
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Assay Data Source: Scientific Literature
Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Kd*Kd PubChem standard valueFloatμM
3BEIBinding Efficiency Index(nM)Float
2SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6Kd activity commentKd activity commentString
7Kd standard flagKd standard flagInteger
8Kd qualifierKd qualifierString
9Kd published valueKd published valueFloatnM
10Kd standard valueKd standard valueFloatnM
11Kd activity commentKd activity commentString
12Kd standard flagKd standard flagInteger
13Kd qualifierKd qualifierString
14Kd published valueKd published valueFloatμM
15Kd standard valueKd standard valueFloatnM

* Activity Concentration.

Data Table (Concise)
Data Table ( Complete ):     View Active Data    View All Data
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