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Assay Detail

CHEMBL1107110

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

Functional
Antagonist activity at human recombinant alpha 3 GlyR expressed in HEK293 cells assessed as inhibition of glycine current influx by whole cell patch clamp assay
11
Total Activities
11
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-3 (CHEMBL1075092)
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
IC50 11 4.65 5.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL464651 1 5.16
CHEMBL1093848 IRCINIALACTAM C 1 4.52
CHEMBL1092618 1 4.52
CHEMBL1092619 IRCINIALACTAM D 1 4.52
CHEMBL1093582 IRCINIALACTAM A 1 4.52
CHEMBL464276 1 -
CHEMBL1093581 1 -
CHEMBL1093847 8-HYDROXYIRCINIALACTAM B 1 -
CHEMBL1093838 8-HYDROXYIRCINIALACTAM A 1 -
CHEMBL1093564 1 -
CHEMBL1089325 COMETIN A 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL464651 IC50 = 7000.0 nM 5.16
CHEMBL1093848 IRCINIALACTAM C IC50 = 30000.0 nM 4.52
CHEMBL1092618 IC50 = 30000.0 nM 4.52
CHEMBL1092619 IRCINIALACTAM D IC50 = 30000.0 nM 4.52
CHEMBL1093582 IRCINIALACTAM A IC50 = 30000.0 nM 4.52
CHEMBL464276 IC50 - -
CHEMBL1093581 IC50 - -
CHEMBL1093847 8-HYDROXYIRCINIALACTAM B IC50 - -
CHEMBL1093838 8-HYDROXYIRCINIALACTAM A IC50 - -
CHEMBL1093564 IC50 - -
CHEMBL1089325 COMETIN A IC50 - -