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Assay Detail

CHEMBL749991

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

Binding
Inhibitory concentration of compound required to displace [3H]TCP 1-[ 1-(2-thienyl)cyclohexyl]piperidine in whole rat brain homogenate
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Glutamate NMDA receptor (CHEMBL1907608)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Synthesis and biological activity of conformationally constrained 4a-phenanthreneamine derivatives as noncompetitive NMDA antagonists
Malone TC, Ortwine DF, Johnson G, Probert AW
Bioorg Med Chem Lett (1993) 3 : 49 -54
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.48 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL284237 DIZOCILPINE 2.0 1 8.52
CHEMBL151150 1 7.83
CHEMBL151238 1 7.78
CHEMBL151589 1 7.07
CHEMBL149975 1 6.86
CHEMBL434324 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL284237 DIZOCILPINE IC50 = 3.0 nM 8.52
CHEMBL151150 IC50 = 14.7 nM 7.83
CHEMBL151238 IC50 = 16.8 nM 7.78
CHEMBL151589 IC50 = 86.0 nM 7.07
CHEMBL149975 IC50 = 137.0 nM 6.86
CHEMBL434324 IC50 = 151.0 nM 6.82