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Assay Detail

CHEMBL1785974

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

Binding
Displacement of [3H]-(+)-MK801 from NMDA receptor PCP binding site in pig cortex membrane after 90 mins by liquid scintillation counting
26
Total Activities
26
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

Synthesis of 4-(aminoalkyl) substituted 1,3-dioxanes as potent NMDA and σ receptor antagonists.
Utech T, Köhler J, Wünsch B.
Eur J Med Chem (2011) 46 : 2157 -2169
PubMed 21444132 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 6.52 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1165411 DEXOXADROL 2.0 1 7.72
CHEMBL305904 ETOXADROL 2.0 1 7.66
CHEMBL1783455 1 7.62
CHEMBL275528 PHENCYCLIDINE 2.0 1 7.55
CHEMBL1783467 1 7.16
CHEMBL1783456 1 6.81
CHEMBL1783469 1 6.59
CHEMBL1783457 1 6.15
CHEMBL1783468 1 6.14
CHEMBL1783451 1 5.63
CHEMBL1783466 1 5.49
CHEMBL1783452 1 5.16
CHEMBL1783465 1 5.12
CHEMBL1783448 1 -
CHEMBL1783449 1 -
CHEMBL1783450 1 -
CHEMBL1783453 1 -
CHEMBL1783454 1 -
CHEMBL1783458 1 -
CHEMBL1783459 1 -
CHEMBL1783460 1 -
CHEMBL1783461 1 -
CHEMBL1783426 1 -
CHEMBL1783464 1 -
CHEMBL1783463 1 -
CHEMBL1783462 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1165411 DEXOXADROL Ki = 19.0 nM 7.72
CHEMBL305904 ETOXADROL Ki = 22.0 nM 7.66
CHEMBL1783455 Ki = 24.0 nM 7.62
CHEMBL275528 PHENCYCLIDINE Ki = 28.0 nM 7.55
CHEMBL1783467 Ki = 69.0 nM 7.16
CHEMBL1783456 Ki = 154.0 nM 6.81
CHEMBL1783469 Ki = 257.0 nM 6.59
CHEMBL1783457 Ki = 713.0 nM 6.15
CHEMBL1783468 Ki = 717.0 nM 6.14
CHEMBL1783451 Ki = 2350.0 nM 5.63
CHEMBL1783466 Ki = 3260.0 nM 5.49
CHEMBL1783452 Ki = 6870.0 nM 5.16
CHEMBL1783465 Ki = 7670.0 nM 5.12
CHEMBL1783448 Ki > 10000.0 nM -
CHEMBL1783449 Ki > 10000.0 nM -
CHEMBL1783450 Ki > 10000.0 nM -
CHEMBL1783453 Ki > 10000.0 nM -
CHEMBL1783454 Ki > 10000.0 nM -
CHEMBL1783458 Ki > 10000.0 nM -
CHEMBL1783459 Ki > 10000.0 nM -
CHEMBL1783460 Ki > 10000.0 nM -
CHEMBL1783461 Ki > 10000.0 nM -
CHEMBL1783426 Ki > 10000.0 nM -
CHEMBL1783464 Ki > 10000.0 nM -
CHEMBL1783463 Ki > 10000.0 nM -
CHEMBL1783462 Ki > 10000.0 nM -