Target
Apoptosis regulator Bcl-2
Ligand
BDBM50339777
Substrate
n/a
Meas. Tech.
ChEMBL_735550 (CHEMBL1693055)
IC50
8.7±n/a nM
Citation
 Sleebs, BECzabotar, PEFairbrother, WJFairlie, WDFlygare, JAHuang, DCKersten, WJKoehler, MFLessene, GLowes, KParisot, JPSmith, BJSmith, MLSouers, AJStreet, IPYang, HBaell, JB Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity. J Med Chem 54:1914-26 (2011) [PubMed]  Article 
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:
BDBM50339777
Synonyms:
(R)-N-(7-(4-((4'-chlorobiphenyl-2-yl)methyl)piperazin-1-yl)quinazolin-4-yl)-4-(4-(dimethylamino)-1-(phenylthio)butan-2-ylamino)-3-nitrobenzenesulfonamide | CHEMBL1689139 | N-{7-[4-(4'-Chloro-biphenyl-2-ylmethyl)piperazin-1-yl]quinazolin-4-yl}-4-((R)-3-dimethylamino-1-phenylsulfanylmethyl-propylamino)-3-nitro-benzenesulfonamide
Type:
Small organic molecule
Emp. Form.:
C43H45ClN8O4S2
Mol. Mass.:
837.452
SMILES:
CN(C)CC[C@H](CSc1ccccc1)Nc1ccc(cc1[N+]([O-])=O)S(=O)(=O)Nc1ncnc2cc(ccc12)N1CCN(Cc2ccccc2-c2ccc(Cl)cc2)CC1 |r|
Structure:
Search PDB for entries with ligand similarity: