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Target
Apoptosis regulator Bcl-2
Ligand
BDBM60825
Substrate
n/a
Meas. Tech.
Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) Assay
Ki
<0.010±n/a nM
Citation
 Bruncko, M; Ding, H; Doherty, GA; Elmore, SW; Hasvold, L; Hexamer, LA; Kunzer, AR; Mantei, RA; McClellan, WJ; Park, CH; Park, C; Petros, AM; Song, X; Souers, AJ; Sullivan, GM; Tao, Z; Wang, GT; Wang, L; Wang, X; Wendt, MD Bcl-2-selective apoptosis-inducing agents for the treatment of cancer and immune diseases US Patent  US9125913 Publication Date 9/8/2015 
Target
Name:
Apoptosis regulator Bcl-2
Synonyms:
Apoptosis regulator Bcl-2 Protein | B-cell lymphoma 2 protein (Bcl-2) | BCL-2 | BCL2 | BCL2_HUMAN | Bcl-2 Protein
Type:
Homodimer or heterodimer
Mol. Mass.:
26269.11
Organism:
Homo sapiens (Human)
Description:
P10415
Residue:
239
Sequence:
MAHAGRTGYDNREIVMKYIHYKLSQRGYEWDAGDVGAAPPGAAPAPGIFSSQPGHTPHPAASRDPVARTSPLQTPAAPGAAAGPALSPVPPVVHLTLRQAGDDFSRRYRRDFAEMSSQLHLTPFTARGRFATVVEELFRDGVNWGRIVAFFEFGGVMCVESVNREMSPLVDNIALWMTEYLNRHLHTWIQDNGGWDAFVELYGPSMRPLFDFSWLSLKTLLSLALVGACITLGAYLGHK
  
Inhibitor
Name:
BDBM60825
Synonyms:
US9174982, 343
Type:
n/a
Emp. Form.:
C47H53Cl2N7O6S
Mol. Mass.:
914.938
SMILES:
C[C@]1(O)C[C@@H]2C[C@@H]1CC2CONc1ncc(cc1Cl)S(=O)(=O)NC(=O)c1ccc(cc1Oc1cnc2[nH]ccc2c1)N1CCN(CC2=C(CC(C)(C)CC2)c2ccc(Cl)cc2)CC1 |r,t:52|
Structure:
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