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Assay Detail

CHEMBL3399841

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

Binding
Displacement of [3H]DTG from rat liver sigma2 receptor by scintillation analyzer
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Improving selectivity preserving affinity: new piperidine-4-carboxamide derivatives as effective sigma-1-ligands.
Zampieri D, Laurini E, Vio L, Fermeglia M, Pricl S, Wünsch B, Schepmann D, Mamolo MG.
Eur J Med Chem (2015) 90 : 797 -808
PubMed 25528334 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.33 7.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1229211 DOLUTEGRAVIR 4.0 1 7.27
CHEMBL54 HALOPERIDOL 4.0 1 7.11
CHEMBL559979 1 6.84
CHEMBL3397616 1 6.21
CHEMBL3397625 1 6.20
CHEMBL3397626 1 6.18
CHEMBL3397617 1 5.92
CHEMBL3397624 1 5.92
CHEMBL3397622 1 5.89
CHEMBL3397613 1 5.75
CHEMBL284237 DIZOCILPINE 2.0 1 -
CHEMBL3397614 1 -
CHEMBL3397623 1 -
CHEMBL3397621 1 -
CHEMBL3397620 1 -
CHEMBL3397619 1 -
CHEMBL3397618 1 -
CHEMBL3397612 1 -
CHEMBL3397615 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1229211 DOLUTEGRAVIR Ki = 54.0 nM 7.27
CHEMBL54 HALOPERIDOL Ki = 78.0 nM 7.11
CHEMBL559979 Ki = 146.0 nM 6.84
CHEMBL3397616 Ki = 622.0 nM 6.21
CHEMBL3397625 Ki = 627.0 nM 6.20
CHEMBL3397626 Ki = 662.0 nM 6.18
CHEMBL3397617 Ki = 1200.0 nM 5.92
CHEMBL3397624 Ki = 1200.0 nM 5.92
CHEMBL3397622 Ki = 1300.0 nM 5.89
CHEMBL3397613 Ki = 1800.0 nM 5.75
CHEMBL284237 DIZOCILPINE Ki - -
CHEMBL3397614 Ki > 2000.0 nM -
CHEMBL3397623 Ki > 2000.0 nM -
CHEMBL3397621 Ki > 2000.0 nM -
CHEMBL3397620 Ki > 2000.0 nM -
CHEMBL3397619 Ki > 2000.0 nM -
CHEMBL3397618 Ki > 2000.0 nM -
CHEMBL3397612 Ki > 2000.0 nM -
CHEMBL3397615 Ki > 2000.0 nM -