Reaction Details Report a problem with these data
Target
Translocator protein
Ligand
BDBM22040
Substrate
BDBM22032
Meas. Tech.
Radioligand Binding Assay
pH
7.4±n/a
Temperature
277.15±n/a K
Ki
23±3.1 nM
Citation
 Taliani, S; Simorini, F; Sergianni, V; La Motta, C; Da Settimo, F; Cosimelli, B; Abignente, E; Greco, G; Novellino, E; Rossi, L; Gremigni, V; Spinetti, F; Chelli, B; Martini, C New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation. J Med Chem 50:404-7 (2007) [PubMed]  Article 
Target
Name:
Translocator protein
Synonyms:
Benzodiazepine receptors; peripheral & central | Bzrp | Mbr | Mitochondrial benzodiazepine receptor | PBR | PKBS | Peripheral benzodiazepine receptor (PBR) | Peripheral-Type Benzodiazepine Receptor | TSPO_RAT | Tspo
Type:
Mitochondrion membrane protein
Mol. Mass.:
18945.84
Organism:
Rattus norvegicus (rat)
Description:
Competitive binding experiments were performed on rat kidney mitochondrial membranes.
Residue:
169
Sequence:
MSQSWVPAVGLTLVPSLGGFMGAYFVRGEGLRWYASLQKPSWHPPRWTLAPIWGTLYSAMGYGSYIIWKELGGFTEEAMVPLGLYTGQLALNWAWPPIFFGARQMGWALVDLMLVSGVATATTLAWHRVSPPAARLLYPYLAWLAFATMLNYYVWRDNSGRRGGSRLTE
  
Inhibitor
Name:
BDBM22040
Synonyms:
4 -chlorodiazepam | 4' Cl-diazepam | 7-chloro-5-(4-chlorophenyl)-1-methyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one | 7-chloro-5-(4-chlorophenyl)-1-methyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one | CHEMBL286346 | Ro 5-4864 | Ro-05-4864 | Ro-4864 | Ro5-4864
Type:
Small organic molecule
Emp. Form.:
C16H12Cl2N2O
Mol. Mass.:
319.185
SMILES:
CN1c2ccc(Cl)cc2C(=NCC1=O)c1ccc(Cl)cc1 |c:10|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM22032
Synonyms:
1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)isoquinoline-3-carboxamide | CHEMBL15313 | N-(butan-2-yl)-1-(2-chlorophenyl)-N-methylisoquinoline-3-carboxamide | PK 11195 | PK-11195 | PK11195 | RP 52028 | [3H]PK 11195
Type:
radiolabeled ligand
Emp. Form.:
C21H21ClN2O
Mol. Mass.:
352.857
SMILES:
CCC(C)N(C)C(=O)c1cc2ccccc2c(n1)-c1ccccc1Cl
Structure:
Search PDB for entries with ligand similarity: