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Assay Detail

CHEMBL679567

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

Binding
In vitro inhibition of [35S]TBPS binding to GABA-A receptor of rat whole brain membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel alpha-amino-acid phenolic ester derivatives with intravenous anaesthetic activity.
Cooke A, Anderson A, Bennett J, Buchanan K, Gemmell D, Hamilton N, Maidment M, McPhail P, Stevenson D, Sundaram H.
Bioorg Med Chem Lett (2003) 13 : 1107 -1110
PubMed 12643922 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.11 5.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL268249 1 5.57
CHEMBL13253 1 5.40
CHEMBL12944 1 5.38
CHEMBL12861 1 5.21
CHEMBL13667 1 5.16
CHEMBL276208 1 5.01
CHEMBL13080 1 4.93
CHEMBL13025 1 4.83
CHEMBL13254 ORG-24447 1 4.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL268249 IC50 = 2700.0 nM 5.57
CHEMBL13253 IC50 = 4000.0 nM 5.40
CHEMBL12944 IC50 = 4200.0 nM 5.38
CHEMBL12861 IC50 = 6200.0 nM 5.21
CHEMBL13667 IC50 = 6900.0 nM 5.16
CHEMBL276208 IC50 = 9700.0 nM 5.01
CHEMBL13080 IC50 = 11700.0 nM 4.93
CHEMBL13025 IC50 = 14700.0 nM 4.83
CHEMBL13254 ORG-24447 IC50 = 29300.0 nM 4.53