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Assay Detail

CHEMBL652733

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

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

Assay Information

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

Target

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

Publication

Synthesis and evaluation of a series of aryl[e]fused pyrazolo[4,3-c]pyridines with potential anxiolytic activity.
Forbes IT, Johnson CN, Jones GE, Loudon J, Nicholass JM, Thompson M, Upton N.
J Med Chem (1990) 33 : 2640 -2645
PubMed 1975276 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 8.31 9.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3144654 1 9.54
CHEMBL327229 1 9.49
CHEMBL20042 CGS-9896 1 9.46
CHEMBL3144769 1 9.34
CHEMBL3144653 1 9.34
CHEMBL3144770 1 8.62
CHEMBL3144771 1 7.92
CHEMBL3144656 1 7.85
CHEMBL12 DIAZEPAM 4.0 1 7.85
CHEMBL3144652 1 7.00
CHEMBL3144651 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3144654 Ki = 0.29 nM 9.54
CHEMBL327229 Ki = 0.32 nM 9.49
CHEMBL20042 CGS-9896 Ki = 0.35 nM 9.46
CHEMBL3144769 Ki = 0.46 nM 9.34
CHEMBL3144653 Ki = 0.46 nM 9.34
CHEMBL3144770 Ki = 2.4 nM 8.62
CHEMBL3144771 Ki = 12.0 nM 7.92
CHEMBL3144656 Ki = 14.0 nM 7.85
CHEMBL12 DIAZEPAM Ki = 14.0 nM 7.85
CHEMBL3144652 Ki = 99.0 nM 7.00
CHEMBL3144651 Ki = 11000.0 nM 4.96