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Assay Detail

CHEMBL2175143

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

Binding
Displacement of [3H]-(+)-MK-801 from PCP binding site of NMDA receptor in pig brain cortex
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Enantiomerically pure 1,3-dioxanes as highly selective NMDA and σ₁ receptor ligands.
Köhler J, Bergander K, Fabian J, Schepmann D, Wünsch B.
J Med Chem (2012) 55 : 8953 -8957
PubMed 23013229 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 6.88 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL344151 DIZOCILPINE MALEATE -1.0 1 8.52
CHEMBL1783455 1 7.89
CHEMBL2170309 1 7.68
CHEMBL2170304 1 7.64
CHEMBL1165411 DEXOXADROL 2.0 1 7.50
CHEMBL2170306 1 7.34
CHEMBL275528 PHENCYCLIDINE 2.0 1 7.23
CHEMBL2170311 1 6.52
CHEMBL395091 ESKETAMINE 4.0 1 6.42
CHEMBL2170310 1 6.40
CHEMBL807 MEMANTINE 4.0 1 6.37
CHEMBL2170307 1 5.83
CHEMBL2170308 1 5.82
CHEMBL2170305 1 5.21
CHEMBL2170315 1 -
CHEMBL1783426 1 -
CHEMBL2170312 1 -
CHEMBL1783450 1 -
CHEMBL2170313 1 -
CHEMBL2170314 1 -
CHEMBL2170178 1 -
CHEMBL1783458 1 -
CHEMBL2170179 1 -
CHEMBL2170180 1 -
CHEMBL2170301 1 -
CHEMBL2170302 1 -
CHEMBL2170303 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL344151 DIZOCILPINE MALEATE Ki = 3.0 nM 8.52
CHEMBL1783455 Ki = 13.0 nM 7.89
CHEMBL2170309 Ki = 21.0 nM 7.68
CHEMBL2170304 Ki = 23.0 nM 7.64
CHEMBL1165411 DEXOXADROL Ki = 32.0 nM 7.50
CHEMBL2170306 Ki = 46.0 nM 7.34
CHEMBL275528 PHENCYCLIDINE Ki = 59.0 nM 7.23
CHEMBL2170311 Ki = 304.0 nM 6.52
CHEMBL395091 ESKETAMINE Ki = 383.0 nM 6.42
CHEMBL2170310 Ki = 400.0 nM 6.40
CHEMBL807 MEMANTINE Ki = 429.0 nM 6.37
CHEMBL2170307 Ki = 1490.0 nM 5.83
CHEMBL2170308 Ki = 1530.0 nM 5.82
CHEMBL2170305 Ki = 6120.0 nM 5.21
CHEMBL2170315 Ki > 10000.0 nM -
CHEMBL1783426 Ki > 10000.0 nM -
CHEMBL2170312 Ki > 10000.0 nM -
CHEMBL1783450 Ki > 10000.0 nM -
CHEMBL2170313 Ki > 10000.0 nM -
CHEMBL2170314 Ki > 10000.0 nM -
CHEMBL2170178 Ki > 10000.0 nM -
CHEMBL1783458 Ki > 10000.0 nM -
CHEMBL2170179 Ki > 10000.0 nM -
CHEMBL2170180 Ki > 10000.0 nM -
CHEMBL2170301 Ki > 10000.0 nM -
CHEMBL2170302 Ki > 10000.0 nM -
CHEMBL2170303 Ki > 10000.0 nM -