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Assay Detail

CHEMBL3998489

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

Binding
Antagonist activity at recombinant human glycine receptor alpha 1 expressed in HEK293 cells assessed as inhibition of glycine-induced current at -50 mV holding potential by whole cell patch-clamp method
9
Total Activities
9
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

Oxime Ethers of (E)-11-Isonitrosostrychnine as Highly Potent Glycine Receptor Antagonists.
Mohsen AM, Mandour YM, Sarukhanyan E, Breitinger U, Villmann C, Banoub MM, Breitinger HG, Dandekar T, Holzgrabe U, Sotriffer C, Jensen AA, Zlotos DP.
J Nat Prod (2016) 79 : 2997 -3005
PubMed 27966945 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.91 7.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4079657 1 7.31
CHEMBL227934 STRYCHNINE -1.0 1 7.29
CHEMBL4103909 1 7.23
CHEMBL4060962 1 7.12
CHEMBL4102677 1 7.12
CHEMBL4089150 1 7.09
CHEMBL4068867 1 6.96
CHEMBL4096857 1 6.70
CHEMBL4069635 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4079657 IC50 = 49.0 nM 7.31
CHEMBL227934 STRYCHNINE IC50 = 51.0 nM 7.29
CHEMBL4103909 IC50 = 59.0 nM 7.23
CHEMBL4060962 IC50 = 76.0 nM 7.12
CHEMBL4102677 IC50 = 75.0 nM 7.12
CHEMBL4089150 IC50 = 82.0 nM 7.09
CHEMBL4068867 IC50 = 109.0 nM 6.96
CHEMBL4096857 IC50 = 201.0 nM 6.70
CHEMBL4069635 IC50 = 4590.0 nM 5.34