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Assay Detail

CHEMBL868101

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

Binding
Displacement of [3H]strychnine from strychnine-sensitive glycine receptor in rat spinal cord
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds.
Gelmi ML, Pocar D, Pontremoli G, Pellegrino S, Bombardelli E, Fontana G, Riva A, Balduini W, Carloni S, Cimino M, Johnson F.
J Med Chem (2006) 49 : 5571 -5577
PubMed 16942030 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.40 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL227934 STRYCHNINE -1.0 1 7.85
CHEMBL213907 THIOCOLCHICOSIDE 3.0 1 5.82
CHEMBL213312 1 5.48
CHEMBL215655 1 5.39
CHEMBL214151 1 5.38
CHEMBL213034 1 5.34
CHEMBL386430 1 5.07
CHEMBL438794 1 4.97
CHEMBL214305 1 4.88
CHEMBL773 GLYCINE 4.0 1 4.80
CHEMBL213015 1 4.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL227934 STRYCHNINE IC50 = 14.0 nM 7.85
CHEMBL213907 THIOCOLCHICOSIDE IC50 = 1500.0 nM 5.82
CHEMBL213312 IC50 = 3300.0 nM 5.48
CHEMBL215655 IC50 = 4100.0 nM 5.39
CHEMBL214151 IC50 = 4200.0 nM 5.38
CHEMBL213034 IC50 = 4600.0 nM 5.34
CHEMBL386430 IC50 = 8600.0 nM 5.07
CHEMBL438794 IC50 = 10600.0 nM 4.97
CHEMBL214305 IC50 = 13100.0 nM 4.88
CHEMBL773 GLYCINE IC50 = 15800.0 nM 4.80
CHEMBL213015 IC50 = 39900.0 nM 4.40