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Target
Translocator protein
Ligand
BDBM22032
Substrate
n/a
Meas. Tech.
ChEMBL_776493 (CHEMBL1913590)
IC50
1.3±n/a nM
Citation
Cappelli, A; Bini, G; Valenti, S; Giuliani, G; Paolino, M; Anzini, M; Vomero, S; Giorgi, G; Giordani, A; Stasi, LP; Makovec, F; Ghelardini, C; Di Cesare Mannelli, L; Concas, A; Porcu, P; Biggio, G Synthesis and structure-activity relationship studies in translocator protein ligands based on a pyrazolo[3,4-b]quinoline scaffold. J Med Chem 54:7165-75 (2011) [PubMed] Article
More Info.:
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:
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