Target Validation Information
Target ID T75440
Target Name Peripheral-type benzodiazepine receptor
Target Type
Successful
Drug Potency against Target 5-Phenyl-6-thia-10b-aza-benzo[e]azulene Drug Info Ki = 3150 nM [533589]
5-Phenyl-6-thia-10b-aza-benzo[e]azulen-4-one Drug Info IC50 = 1220 nM [533922]
ALPIDEM Drug Info Ki = 0.5 nM [529656]
6-Thia-10b-aza-benzo[e]azulen-4-one Drug Info IC50 = 14000 nM [533922]
N,N-Dimethyl-2-(2-phenyl-1H-indol-3-yl)-acetamide Drug Info Ki = 170 nM [534032]
2-(2-Phenyl-1H-indol-3-yl)-N,N-dipropyl-acetamide Drug Info Ki = 100 nM [534032]
N-Hexyl-2-(2-phenyl-1H-indol-3-yl)-acetamide Drug Info Ki = 96 nM [534032]
4-Methoxy-5-phenyl-6-thia-10b-aza-benzo[e]azulene Drug Info Ki = 7000 nM [533589]
(R)PK-11195 Drug Info IC50 = 8.26 nM [526488]
Dextofisopam Drug Info IC50 < 100 nM [553160]
N,N-Dihexyl-2-(2-phenyl-1H-indol-3-yl)-acetamide Drug Info Ki = 9.7 nM [534032]
N,N-Diethyl-2-(2-phenyl-1H-indol-3-yl)-acetamide Drug Info Ki = 156 nM [534032]
References
Ref 533589J Med Chem. 1995 Nov 10;38(23):4730-8.A concerted study using binding measurements, X-ray structural data, and molecular modeling on the stereochemical features responsible for the affinity of 6-arylpyrrolo[2,1-d][1,5]benzothiazepines toward mitochondrial benzodiazepine receptors.
Ref 533922J Med Chem. 1994 May 13;37(10):1427-38.Novel ligands specific for mitochondrial benzodiazepine receptors: 6-arylpyrrolo[2,1-d][1,5]benzothiazepine derivatives. Synthesis, structure-activity relationships, and molecular modeling studies.
Ref 529656J Med Chem. 2008 Sep 25;51(18):5798-806. Epub 2008 Aug 26.Anxiolytic-like effects of N,N-dialkyl-2-phenylindol-3-ylglyoxylamides by modulation of translocator protein promoting neurosteroid biosynthesis.
Ref 533922J Med Chem. 1994 May 13;37(10):1427-38.Novel ligands specific for mitochondrial benzodiazepine receptors: 6-arylpyrrolo[2,1-d][1,5]benzothiazepine derivatives. Synthesis, structure-activity relationships, and molecular modeling studies.
Ref 534032J Med Chem. 1993 Oct 1;36(20):2908-20.Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands.
Ref 534032J Med Chem. 1993 Oct 1;36(20):2908-20.Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands.
Ref 534032J Med Chem. 1993 Oct 1;36(20):2908-20.Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands.
Ref 533589J Med Chem. 1995 Nov 10;38(23):4730-8.A concerted study using binding measurements, X-ray structural data, and molecular modeling on the stereochemical features responsible for the affinity of 6-arylpyrrolo[2,1-d][1,5]benzothiazepines toward mitochondrial benzodiazepine receptors.
Ref 526488Bioorg Med Chem Lett. 2003 Jan 20;13(2):201-4.[18F]FMDAA1106 and [18F]FEDAA1106: two positron-emitter labeled ligands for peripheral benzodiazepine receptor (PBR).
Ref 553160Tofizopam affects binding of [3H]muscimol to gamma-amino-butyric acid receptors in rat and mouse brains. Pharmacol Res Commun. 1982 Sep;14(8):745-57.
Ref 534032J Med Chem. 1993 Oct 1;36(20):2908-20.Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands.
Ref 534032J Med Chem. 1993 Oct 1;36(20):2908-20.Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.