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Assay Detail

CHEMBL654255

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
In vitro displacement of [3H]flunitrazepam from GABA-A central benzodiazepine receptor of guinea pig cerebellum
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Cerebellum
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

GABA-A receptor; anion channel (CHEMBL2093872)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

5-cyano-1-[3-(N-methylpyrrolidin-2R-ylmethyl)indol-5-yl] benzimidazole (CP-161,242): A potent, centrally active 5-HT1D receptor agonist and benzodiazepine partial agonist
Macor JE, Blank DH, Desai K, Fox CB, Kenneth Koe B, Lebel LA, Post RJ, Schmidt AW, Schulz DW, Seymour PA
Bioorg Med Chem Lett (1995) 5 : 2391 -2396
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.45 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12 DIAZEPAM 4.0 1 7.85
CHEMBL80189 1 7.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12 DIAZEPAM IC50 = 14.0 nM 7.85
CHEMBL80189 IC50 = 89.0 nM 7.05