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Assay Detail

CHEMBL675661

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

Binding
Binding affinity for sigma-1 site over dopamine (D2) receptor in rat using [3H]spiperone as radioligand
11
Total Activities
11
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

Novel (4-phenylpiperidinyl)- and (4-phenylpiperazinyl)alkyl-spaced esters of 1-phenylcyclopentanecarboxylic acids as potent sigma-selective compounds.
Hudkins RL, Mailman RB, DeHaven-Hudkins DL.
J Med Chem (1994) 37 : 1964 -1970
PubMed 8027978 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 6.40 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL554628 1 7.26
CHEMBL545678 1 6.71
CHEMBL558028 1 6.67
CHEMBL541284 1 6.46
CHEMBL542630 1 6.33
CHEMBL555580 1 6.30
CHEMBL537464 1 6.00
CHEMBL544516 1 5.96
CHEMBL540013 1 5.92
CHEMBL537989 1 -
CHEMBL282433 DITOLYLGUANIDINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL554628 Ki = 55.0 nM 7.26
CHEMBL545678 Ki = 195.0 nM 6.71
CHEMBL558028 Ki = 215.0 nM 6.67
CHEMBL541284 Ki = 350.0 nM 6.46
CHEMBL542630 Ki = 470.0 nM 6.33
CHEMBL555580 Ki = 500.0 nM 6.30
CHEMBL537464 Ki = 1000.0 nM 6.00
CHEMBL544516 Ki = 1100.0 nM 5.96
CHEMBL540013 Ki = 1200.0 nM 5.92
CHEMBL537989 Ki > 500.0 nM -
CHEMBL282433 DITOLYLGUANIDINE Ki > 5000.0 nM -