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Assay Detail

CHEMBL749669

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

Binding
Binding affinity against dextromethorpin binding site associated with N-methyl-D-aspartate glutamate receptor from guinea pig mitochondrial pellet P2 determined using [3H]1 as radioligand.
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Glutamate [NMDA] receptor (CHEMBL2094124)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Synthesis and evaluation of 3-substituted 17-methylmorphinan analogs as potential anticonvulsant agents.
Newman AH, Bevan K, Bowery N, Tortella FC.
J Med Chem (1992) 35 : 4135 -4142
PubMed 1433216 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.32 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL435790 1 7.05
CHEMBL133532 1 6.82
CHEMBL133531 1 6.80
CHEMBL22207 RACEMETHORPHAN 2.0 1 6.62
CHEMBL336430 1 6.43
CHEMBL133401 1 6.36
CHEMBL337277 1 6.17
CHEMBL71 CHLORPROMAZINE 4.0 1 5.96
CHEMBL334822 1 5.77
CHEMBL130193 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL435790 IC50 = 90.0 nM 7.05
CHEMBL133532 IC50 = 150.0 nM 6.82
CHEMBL133531 IC50 = 160.0 nM 6.80
CHEMBL22207 RACEMETHORPHAN IC50 = 240.0 nM 6.62
CHEMBL336430 IC50 = 370.0 nM 6.43
CHEMBL133401 IC50 = 440.0 nM 6.36
CHEMBL337277 IC50 = 680.0 nM 6.17
CHEMBL71 CHLORPROMAZINE IC50 = 1100.0 nM 5.96
CHEMBL334822 IC50 = 1700.0 nM 5.77
CHEMBL130193 IC50 = 6400.0 nM 5.19