Reaction Details Report a problem with these data
Target
Bcl-2-like protein 1
Ligand
BDBM21404
Substrate
Fluorescein-labeled BAD peptide
Meas. Tech.
Fluorescence Polarization Assay and FL5.12 Cellular Assay
pH
7.4±n/a
Temperature
298.15±n/a K
Ki
3.7±1.1 nM
EC50
>20000±n/a nM
Citation
Bruncko, M; Oost, TK; Belli, BA; Ding, H; Joseph, MK; Kunzer, A; Martineau, D; McClellan, WJ; Mitten, M; Ng, SC; Nimmer, PM; Oltersdorf, T; Park, CM; Petros, AM; Shoemaker, AR; Song, X; Wang, X; Wendt, MD; Zhang, H; Fesik, SW; Rosenberg, SH; Elmore, SW Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. J Med Chem 50:641-62 (2007) [PubMed] Article
More Info.:
Target
Name:
Bcl-2-like protein 1
Synonyms:
Anti-apoptotic Bcl-2 protein | Apoptosis Regulator Bcl-xL | Apoptosis regulator Bcl-X | B2CL1_HUMAN | BCL2-like 1 isoform 1 | BCL2L | BCL2L1 | BCLX | Bcl-2-like protein 1 (Bcl-XL) | Bcl-X | Bcl-xL/Bcl-2-binding component 3 | Bcl2-L-1 | Bcl2-antagonist of cell death (BAD)
Type:
Mitochondrion membrane; Single-pass membrane protein
Mol. Mass.:
26039.60
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
233
Sequence:
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
Inhibitor
Name:
BDBM21404
Synonyms:
4-{4-benzyl-2-methyl-3-oxo-1-oxa-4,8-diazaspiro[4.5]decan-8-yl}-N-[(4-{[(2R)-4-(dimethylamino)-1-(phenylsulfanyl)butan-2-yl]amino}-3-nitrobenzene)sulfonyl]benzamide | Spirocyclic Oxazolidin-4-one, 18
Type:
Small organic molecule
Emp. Form.:
C40H46N6O7S2
Mol. Mass.:
786.959
SMILES:
CC1OC2(CCN(CC2)c2ccc(cc2)C(=O)NS(=O)(=O)c2ccc(N[C@H](CCN(C)C)CSc3ccccc3)c(c2)[N+]([O-])=O)N(Cc2ccccc2)C1=O |r|
Substrate
Name:
Fluorescein-labeled BAD peptide
Synonyms:
n/a
Type:
fluorescein-labeled probe
Mol. Mass.:
3078.53
Organism:
n/a
Description:
n/a
Residue:
25
Sequence:
NLWAAQRYGRELRRMSDKFITCFVD