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Assay Detail

CHEMBL652732

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

Binding
Inhibitory concentration against specific binding of [3H]diazepam to Benzodiazepine receptor in rat brain
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

GABA-A receptor; anion channel (CHEMBL1907607)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Benzodiazepine receptor binding activity of 9-(1-phenylethyl)purines.
Kelley JL, McLean EW, Ferris RM, Howard JL.
J Med Chem (1990) 33 : 1910 -1914
PubMed 2163452 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.08 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12 DIAZEPAM 4.0 1 8.22
CHEMBL56243 1 7.96
CHEMBL60919 1 6.96
CHEMBL56277 1 6.80
CHEMBL451 CHLORDIAZEPOXIDE 4.0 1 6.70
CHEMBL299177 1 6.42
CHEMBL7474 1 6.36
CHEMBL299242 1 6.32
CHEMBL299894 1 6.28
CHEMBL7344 1 6.05
CHEMBL7293 1 5.92
CHEMBL57804 1 5.92
CHEMBL301889 1 5.77
CHEMBL275514 1 5.68
CHEMBL291511 1 5.66
CHEMBL60971 1 5.52
CHEMBL7723 9-BENZYL-6-METHYLSULFANYL-9H-PURINE 1 5.48
CHEMBL6889 1 4.89
CHEMBL293310 1 4.72
CHEMBL274148 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12 DIAZEPAM IC50 = 6.0 nM 8.22
CHEMBL56243 IC50 = 11.0 nM 7.96
CHEMBL60919 IC50 = 110.0 nM 6.96
CHEMBL56277 IC50 = 160.0 nM 6.80
CHEMBL451 CHLORDIAZEPOXIDE IC50 = 200.0 nM 6.70
CHEMBL299177 IC50 = 380.0 nM 6.42
CHEMBL7474 IC50 = 440.0 nM 6.36
CHEMBL299242 IC50 = 480.0 nM 6.32
CHEMBL299894 IC50 = 520.0 nM 6.28
CHEMBL7344 IC50 = 900.0 nM 6.05
CHEMBL7293 IC50 = 1200.0 nM 5.92
CHEMBL57804 IC50 = 1200.0 nM 5.92
CHEMBL301889 IC50 = 1700.0 nM 5.77
CHEMBL275514 IC50 = 2100.0 nM 5.68
CHEMBL291511 IC50 = 2200.0 nM 5.66
CHEMBL60971 IC50 = 3000.0 nM 5.52
CHEMBL7723 9-BENZYL-6-METHYLSULFANYL-9H-PURINE IC50 = 3300.0 nM 5.48
CHEMBL6889 IC50 = 13000.0 nM 4.89
CHEMBL293310 IC50 = 19000.0 nM 4.72
CHEMBL274148 IC50 = 100000.0 nM 4.00