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Assay Detail

CHEMBL653110

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

Binding
Displacement of [3H]diazepam from rat cerebral cortex benzodiazepine receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
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 structure--activity relationships of fused imidazopyridines: a new series of benzodiazepine receptor ligands.
Takada S, Sasatani T, Chomei N, Adachi M, Fujishita T, Eigyo M, Murata S, Kawasaki K, Matsushita A.
J Med Chem (1996) 39 : 2844 -2851
PubMed 8709114 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.48 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19732 CGS-8216 1 9.66
CHEMBL3144843 1 9.49
CHEMBL317036 1 9.22
CHEMBL12 DIAZEPAM 4.0 1 8.30
CHEMBL95085 1 7.66
CHEMBL316782 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19732 CGS-8216 Ki = 0.22 nM 9.66
CHEMBL3144843 Ki = 0.32 nM 9.49
CHEMBL317036 Ki = 0.6 nM 9.22
CHEMBL12 DIAZEPAM Ki = 5.0 nM 8.30
CHEMBL95085 Ki = 22.0 nM 7.66
CHEMBL316782 Ki = 270.0 nM 6.57