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Assay Detail

CHEMBL647211

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

Binding
Binding affinity for Diazepam-Sensitive fraction of GABA-A benzodiazepine receptors
7
Total Activities
7
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

Synthesis and evaluation of imidazo[1,5-a][1,4]benzodiazepine esters with high affinities and selectivities at "diazepam-insensitive" benzodiazepine receptors.
Gu ZQ, Wong G, Dominguez C, de Costa BR, Rice KC, Skolnick P.
J Med Chem (1993) 36 : 1001 -1006
PubMed 8386769 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.42 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6597 Ro-154513 1 8.28
CHEMBL415290 Ro-151310 1 8.27
CHEMBL6440 1 8.01
CHEMBL7290 1 7.85
CHEMBL6655 1 7.80
CHEMBL6793 1 6.30
CHEMBL6407 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6597 Ro-154513 Ki = 5.3 nM 8.28
CHEMBL415290 Ro-151310 Ki = 5.4 nM 8.27
CHEMBL6440 Ki = 9.7 nM 8.01
CHEMBL7290 Ki = 14.0 nM 7.85
CHEMBL6655 Ki = 16.0 nM 7.80
CHEMBL6793 Ki = 499.3 nM 6.30
CHEMBL6407 Ki = 3489.0 nM 5.46