Therapeutic Targets Database
BIDD Pharmainformatics Databases


Target Validation Information
Target NameInduced myeloid leukemia cell differentiation protein Mcl-1    
Type of TargetClinical trial target    
Drug Potency against TargetAT-101IC50 = 180 nM[1]
TW-37IC50 = 1030 nM[2]
SULFURETINIC50 = 1534.63 nM[3]
AMENTOFLAVONEIC50 = 1634.07 nM[3]
BITHIONOLIC50 = 1898.89 nM[3]
GNF-PF-1591IC50 = 19733.2 nM[3]
ROSMARINIC ACIDIC50 = 2025.72 nM[3]
MORINIC50 = 2988.26 nM[3]
GNF-PF-3955IC50 = 3567.91 nM[3]
NSC-180246IC50 = 3944.08 nM[3]
ALTENUSINIC50 = 4147.65 nM[3]
NSC-66209IC50 = 5376.77 nM[3]
GNF-PF-5134IC50 = 9187.06 nM[3]
Action against Disease ModelAT-101When administered alone, AT-101 resulted in increased apoptosis in concentration-dependent manner against both radiotherapy responsive (HCC2429) and non-responsive (A549) cell-lines, with enhanced activity in HCC2429 even at lower concentration. Furthermore, AT-101 promoted radiosensitivity of A549 and HCC2429 cells (p < 0.005). Consistent with 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazoli uM bromide assay findings, A549 cells required increased AT-101 dose to achieve a similar cytoxicity to HCC2429 cells[4]
The Effect of Target Knockout, Knockdown or Genetic VariationsAdministration of ABT-737 to Mcl-1 knockout mice induced severe liver apoptosis, suggesting that t uMor-specific inhibition of Mcl-1 is required for therapeutic purposes[5]
Ref 1Nat Rev Drug Discov. 2008 Dec;7(12):989-1000.BCL-2 family antagonists for cancer therapy. To Reference
Ref 2J Med Chem. 2006 Oct 19;49(21):6139-42.Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins. To Reference
Ref 3Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). To Reference
Ref 4J Thorac Oncol. 2010 May;5(5):680-7.AT-101, a pan-Bcl-2 inhibitor, leads to radiosensitization of non-small cell lung cancer. To Reference
Ref 5Hepatology. 2010 Oct;52(4):1310-21.The Bcl-xL inhibitor, ABT-737, efficiently induces apoptosis and suppresses growth of hepatoma cells in combination with sorafenib. To Reference


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