Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL915383

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

Binding
Activity at human alpha-1GlyR expressed in HEK293 cells assessed as inhibition of 300 uM glycine-induced current by whole-cell patch clamp experiment
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Probing the pharmacophore of ginkgolides as glycine receptor antagonists.
Jensen AA, Begum N, Vogensen SB, Knapp KM, Gundertofte K, Dzyuba SV, Ishii H, Nakanishi K, Kristiansen U, Strømgaard K.
J Med Chem (2007) 50 : 1610 -1617
PubMed 17352465 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.67 6.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2113267 GINKGOLIDE M 1 6.19
CHEMBL221821 GINKGOLIDE C 1 5.77
CHEMBL514432 GINKOLIDE B 1 5.77
CHEMBL465161 GINKGOLIDE A 1 5.42
CHEMBL374004 GINKGOLIDE J 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2113267 GINKGOLIDE M IC50 = 650.0 nM 6.19
CHEMBL221821 GINKGOLIDE C IC50 = 1700.0 nM 5.77
CHEMBL514432 GINKOLIDE B IC50 = 1700.0 nM 5.77
CHEMBL465161 GINKGOLIDE A IC50 = 3800.0 nM 5.42
CHEMBL374004 GINKGOLIDE J IC50 = 6400.0 nM 5.19