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Assay Detail

CHEMBL4342371

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

Binding
Antagonist activity at human glycine receptor subunit alpha-1 expressed in HEK293 cells assessed as reduction in glycine-induced whole cell currents by patch-clamp technique
3
Total Activities
3
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

11-Aminostrychnine and <i>N</i>-(Strychnine-11-yl)propionamide: Synthesis, Configuration, and Pharmacological Evaluation at Glycine Receptors.
Zlotos DP, Mohsen AMY, Mandour YM, Marzouk MA, Breitinger U, Villmann C, Breitinger HG, Sotriffer C, Jensen AA, Holzgrabe U.
J Nat Prod (2019) 82 : 2332 -2336
PubMed 31385511 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.92 7.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL227934 STRYCHNINE -1.0 1 7.29
CHEMBL4518537 1 6.76
CHEMBL4447664 1 6.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL227934 STRYCHNINE IC50 = 51.0 nM 7.29
CHEMBL4518537 IC50 = 173.0 nM 6.76
CHEMBL4447664 IC50 = 194.0 nM 6.71