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Assay Detail

CHEMBL3636229

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

Binding
Displacement of [3H]DTG from sigma2 receptor in rat liver membranes incubated for 120 mins by scintillation counting method in presence of pentazocine
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Subcellular Membrane
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Novel Potent N-Methyl-d-aspartate (NMDA) Receptor Antagonists or σ1 Receptor Ligands Based on Properly Substituted 1,4-Dioxane Ring.
Bonifazi A, Del Bello F, Mammoli V, Piergentili A, Petrelli R, Cimarelli C, Pellei M, Schepmann D, Wünsch B, Barocelli E, Bertoni S, Flammini L, Amantini C, Nabissi M, Santoni G, Vistoli G, Quaglia W.
J Med Chem (2015) 58 : 8601 -8615
PubMed 26430967 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 6.04 7.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282433 DITOLYLGUANIDINE 1 7.19
CHEMBL3633572 1 6.96
CHEMBL3633571 1 6.76
CHEMBL3633401 1 6.16
CHEMBL3633404 1 6.08
CHEMBL3633403 1 6.00
CHEMBL3633399 1 5.80
CHEMBL3633211 1 5.60
CHEMBL3633394 1 5.37
CHEMBL3633397 1 5.31
CHEMBL3633387 1 5.24
CHEMBL3633391 1 -
CHEMBL3633392 1 -
CHEMBL3633393 1 -
CHEMBL3633206 1 -
CHEMBL3633395 1 -
CHEMBL3633396 1 -
CHEMBL3633398 1 -
CHEMBL3633390 1 -
CHEMBL3633400 1 -
CHEMBL3633388 1 -
CHEMBL3633402 1 -
CHEMBL3633210 1 -
CHEMBL3633209 1 -
CHEMBL3633208 1 -
CHEMBL3633207 1 -
CHEMBL3633389 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282433 DITOLYLGUANIDINE Ki = 64.0 nM 7.19
CHEMBL3633572 Ki = 111.0 nM 6.96
CHEMBL3633571 Ki = 174.0 nM 6.76
CHEMBL3633401 Ki = 698.0 nM 6.16
CHEMBL3633404 Ki = 841.0 nM 6.08
CHEMBL3633403 Ki = 1000.0 nM 6.00
CHEMBL3633399 Ki = 1600.0 nM 5.80
CHEMBL3633211 Ki = 2500.0 nM 5.60
CHEMBL3633394 Ki = 4300.0 nM 5.37
CHEMBL3633397 Ki = 4900.0 nM 5.31
CHEMBL3633387 Ki = 5800.0 nM 5.24
CHEMBL3633391 Ki > 10000.0 nM -
CHEMBL3633392 Ki > 10000.0 nM -
CHEMBL3633393 Ki > 10000.0 nM -
CHEMBL3633206 Ki > 10000.0 nM -
CHEMBL3633395 Ki > 10000.0 nM -
CHEMBL3633396 Ki > 10000.0 nM -
CHEMBL3633398 Ki > 10000.0 nM -
CHEMBL3633390 Ki > 10000.0 nM -
CHEMBL3633400 Ki > 10000.0 nM -
CHEMBL3633388 Ki > 10000.0 nM -
CHEMBL3633402 Ki > 10000.0 nM -
CHEMBL3633210 Ki > 10000.0 nM -
CHEMBL3633209 Ki > 10000.0 nM -
CHEMBL3633208 Ki > 10000.0 nM -
CHEMBL3633207 Ki > 10000.0 nM -
CHEMBL3633389 Ki > 10000.0 nM -