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Assay Detail

CHEMBL650869

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

Binding
Displacement of [3H]diazepam from rat brain GABA-A benzodiazepine receptor
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Design of nonpeptidal ligands for a peptide receptor: cholecystokinin antagonists.
Evans BE, Rittle KE, Bock MG, DiPardo RM, Freidinger RM, Whitter WL, Gould NP, Lundell GF, Homnick CF, Veber DF.
J Med Chem (1987) 30 : 1229 -1239
PubMed 2885419 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.05 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL452 CLONAZEPAM 4.0 1 8.77
CHEMBL13280 FLUNITRAZEPAM 4.0 1 8.77
CHEMBL12 DIAZEPAM 4.0 1 8.15
CHEMBL1907931 1 5.25
CHEMBL283117 ASPERLICIN 1 4.30
CHEMBL1907740 1 -
CHEMBL1907714 1 -
CHEMBL1907741 1 -
CHEMBL1907739 1 -
CHEMBL1907728 1 -
CHEMBL70728 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL452 CLONAZEPAM IC50 = 1.7 nM 8.77
CHEMBL13280 FLUNITRAZEPAM IC50 = 1.7 nM 8.77
CHEMBL12 DIAZEPAM IC50 = 7.0 nM 8.15
CHEMBL1907931 IC50 = 5600.0 nM 5.25
CHEMBL283117 ASPERLICIN IC50 = 50000.0 nM 4.30
CHEMBL1907740 IC50 > 100000.0 nM -
CHEMBL1907714 IC50 > 100000.0 nM -
CHEMBL1907741 IC50 > 180000.0 nM -
CHEMBL1907739 IC50 > 100000.0 nM -
CHEMBL1907728 IC50 > 100000.0 nM -
CHEMBL70728 IC50 > 100000.0 nM -