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Assay Detail

CHEMBL682645

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

Binding
GABA-modulatory action compound was evaluated on Oocytes expressing recombinant human alpha-1-beta-3-gamma-2L GABA A receptor at concentrations of >=100 micro<M
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

GABA-A receptor; alpha-1/beta-3/gamma-2 (CHEMBL2094121)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Alpha-amino acid phenolic ester derivatives: novel water-soluble general anesthetic agents which allosterically modulate GABA(A) receptors.
Anderson A, Belelli D, Bennett DJ, Buchanan KI, Casula A, Cooke A, Feilden H, Gemmell DK, Hamilton NM, Hutchinson EJ, Lambert JJ, Maidment MS, McGuire R, McPhail P, Miller S, Muntoni A, Peters JA, Sansbury FH, Stevenson D, Sundaram H.
J Med Chem (2001) 44 : 3582 -3591
PubMed 11606122 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 5.26 5.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL526 PROPOFOL 4.0 1 5.39
CHEMBL331192 1 5.39
CHEMBL116662 1 5.26
CHEMBL13254 ORG-24447 1 5.00
CHEMBL544583 1 -
CHEMBL120361 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL526 PROPOFOL EC50 = 4100.0 nM 5.39
CHEMBL331192 EC50 = 4100.0 nM 5.39
CHEMBL116662 EC50 = 5500.0 nM 5.26
CHEMBL13254 ORG-24447 EC50 = 10000.0 nM 5.00
CHEMBL544583 EC50 = 198000.0 nM -
CHEMBL120361 EC50 > 100000.0 nM -