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Assay Detail

CHEMBL650682

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

Binding
Inhibition of [3H]Ro-151788 binding to GABA-A central benzodiazepine receptor of bovine brain membranes
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Subcellular Brain membranes
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

GABA-A receptor; anion channel (CHEMBL2094107)
Type PROTEIN COMPLEX GROUP
Organism Bos taurus

Publication

Synthesis and benzodiazepine receptor affinity of pyrazolo[1,5-a]pyrimidine derivatives. 3. New 6-(3-thienyl) series as alpha 1 selective ligands.
Selleri S, Bruni F, Costagli C, Costanzo A, Guerrini G, Ciciani G, Gratteri P, Bonaccini C, Malmberg Aiello P, Besnard F, Renard S, Costa B, Martini C.
J Med Chem (2003) 46 : 310 -313
PubMed 12519068 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.43 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL322697 1 7.80
CHEMBL107228 1 7.58
CHEMBL107447 1 7.38
CHEMBL320137 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL322697 Ki = 16.0 nM 7.80
CHEMBL107228 Ki = 26.0 nM 7.58
CHEMBL107447 Ki = 42.2 nM 7.38
CHEMBL320137 Ki = 111.0 nM 6.96