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Assay Detail

CHEMBL652553

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

Binding
Specific binding of [3H]Ro-151788 to GABA-A Benzodiazepine receptor in rat cortex
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-activity relationship studies at the benzodiazepine receptor (BZR): a comparison of the substitutent effects of pyrazoloquinolinone analogs.
Fryer RI, Zhang P, Rios R, Gu ZQ, Basile AS, Skolnick P.
J Med Chem (1993) 36 : 1669 -1673
PubMed 8388472 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.34 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3144615 1 9.62
CHEMBL3144841 1 9.42
CHEMBL3144609 1 9.24
CHEMBL3144617 1 8.68
CHEMBL3144744 1 8.41
CHEMBL3144608 1 8.40
CHEMBL3144743 1 8.10
CHEMBL3144738 1 7.16
CHEMBL3144611 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3144615 IC50 = 0.24 nM 9.62
CHEMBL3144841 IC50 = 0.38 nM 9.42
CHEMBL3144609 IC50 = 0.58 nM 9.24
CHEMBL3144617 IC50 = 2.1 nM 8.68
CHEMBL3144744 IC50 = 3.9 nM 8.41
CHEMBL3144608 IC50 = 4.0 nM 8.40
CHEMBL3144743 IC50 = 8.0 nM 8.10
CHEMBL3144738 IC50 = 70.0 nM 7.16
CHEMBL3144611 IC50 = 990.0 nM 6.00