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Target
Translocator protein
Ligand
BDBM50052309
Substrate
n/a
Meas. Tech.
ChEMBL_37074 (CHEMBL650011)
Ki
10±n/a nM
Citation
Campiani, G; Fiorini, I; De Filippis, MP; Ciani, SM; Garofalo, A; Nacci, V; Giorgi, G; Sega, A; Botta, M; Chiarini, A; Budriesi, R; Bruni, G; Romeo, MR; Manzoni, C; Mennini, T Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blockers. J Med Chem 39:2922-38 (1996) [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:
BDBM50052309
Synonyms:
Acetic acid (4R,5R)-7-chloro-1-dimethylaminomethyl-5-(4-methoxy-phenyl)-4,5-dihydro-6-thia-10b-aza-benzo[e]azulen-4-yl ester | CHEMBL318007
Type:
Small organic molecule
Emp. Form.:
C24H25ClN2O3S
Mol. Mass.:
456.985
SMILES:
COc1ccc(cc1)[C@H]1Sc2c(Cl)cccc2-n2c(CN(C)C)ccc2[C@H]1OC(C)=O