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Assay Detail

CHEMBL1107103

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

Functional
Agonist activity at human recombinant alpha 1 GlyR expressed in HEK293 cells assessed as potentiation of glycine current by whole cell patch clamp assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glycine receptor subunit alpha-1 (CHEMBL5845)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Ircinialactams: subunit-selective glycine receptor modulators from Australian sponges of the family Irciniidae.
Balansa W, Islam R, Fontaine F, Piggott AM, Zhang H, Webb TI, Gilbert DF, Lynch JW, Capon RJ.
Bioorg Med Chem (2010) 18 : 2912 -2919
PubMed 20346682 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 6.11 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1093847 8-HYDROXYIRCINIALACTAM B 1 6.30
CHEMBL464651 1 5.92
CHEMBL464276 1 -
CHEMBL1093581 1 -
CHEMBL1093848 IRCINIALACTAM C 1 -
CHEMBL1092618 1 -
CHEMBL1092619 IRCINIALACTAM D 1 -
CHEMBL1093564 1 -
CHEMBL1089325 COMETIN A 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1093847 8-HYDROXYIRCINIALACTAM B EC50 = 500.0 nM 6.30
CHEMBL464651 EC50 = 1200.0 nM 5.92
CHEMBL464276 EC50 - -
CHEMBL1093581 EC50 - -
CHEMBL1093848 IRCINIALACTAM C EC50 - -
CHEMBL1092618 EC50 - -
CHEMBL1092619 IRCINIALACTAM D EC50 - -
CHEMBL1093564 EC50 - -
CHEMBL1089325 COMETIN A EC50 - -