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Assay Detail

CHEMBL1065458

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

Binding
Displacement of [3H]strychnine from GlyR in Wistar rat spinal cord by scintillation spectrometry
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glycine receptor subunit alpha-1 (CHEMBL3246)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis of heteroaromatic tropeines and heterogeneous binding to glycine receptors.
Maksay G, Vincze Z, Nemes P.
Bioorg Med Chem (2009) 17 : 6872 -6878
PubMed 19726200 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.17 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3084712 1 7.47
CHEMBL3084718 1 7.38
CHEMBL3084707 1 7.10
CHEMBL3084711 1 7.00
CHEMBL3084716 1 6.89
CHEMBL3084714 1 6.78
CHEMBL3084706 1 6.63
CHEMBL3084708 1 5.80
CHEMBL3084713 1 5.72
CHEMBL3084717 1 5.72
CHEMBL3084710 1 5.37
CHEMBL3084705 1 5.33
CHEMBL3084704 1 5.25
CHEMBL3084709 1 5.12
CHEMBL3084715 1 4.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3084712 IC50 = 33.88 nM 7.47
CHEMBL3084718 IC50 = 41.69 nM 7.38
CHEMBL3084707 IC50 = 79.43 nM 7.10
CHEMBL3084711 IC50 = 100.0 nM 7.00
CHEMBL3084716 IC50 = 128.82 nM 6.89
CHEMBL3084714 IC50 = 165.96 nM 6.78
CHEMBL3084706 IC50 = 234.42 nM 6.63
CHEMBL3084708 IC50 = 1584.89 nM 5.80
CHEMBL3084713 IC50 = 1905.46 nM 5.72
CHEMBL3084717 IC50 = 1905.46 nM 5.72
CHEMBL3084710 IC50 = 4265.8 nM 5.37
CHEMBL3084705 IC50 = 4677.35 nM 5.33
CHEMBL3084704 IC50 = 5623.41 nM 5.25
CHEMBL3084709 IC50 = 7585.78 nM 5.12
CHEMBL3084715 IC50 = 11220.18 nM 4.95