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Assay Detail

CHEMBL860171

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Binding
Displacement of [3H]DTG from sigma 2 receptor in rat liver membranes
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 3 — Cell-line / Tissue
Curated By Expert

Publication

Methyl substitution on the piperidine ring of N-[omega-(6-methoxynaphthalen-1-yl)alkyl] derivatives as a probe for selective binding and activity at the sigma(1) receptor.
Berardi F, Ferorelli S, Abate C, Pedone MP, Colabufo NA, Contino M, Perrone R.
J Med Chem (2005) 48 : 8237 -8244
PubMed 16366605 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 7.28 7.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL540818 1 7.76
CHEMBL540563 1 7.75
CHEMBL545278 1 7.75
CHEMBL558980 1 7.58
CHEMBL536483 1 7.58
CHEMBL554450 1 7.54
CHEMBL539545 1 7.53
CHEMBL534695 1 7.50
CHEMBL538566 1 7.50
CHEMBL282433 DITOLYLGUANIDINE 1 7.49
CHEMBL545508 1 7.49
CHEMBL540573 1 7.44
CHEMBL559178 1 7.41
CHEMBL535363 1 7.31
CHEMBL537842 1 7.31
CHEMBL559377 1 7.27
CHEMBL554663 1 7.23
CHEMBL552542 1 7.22
CHEMBL539333 1 7.19
CHEMBL544343 1 7.17
CHEMBL542701 1 7.06
CHEMBL540361 1 7.03
CHEMBL538772 1 6.98
CHEMBL537399 1 6.94
CHEMBL535366 1 6.82
CHEMBL553091 1 6.76
CHEMBL190883 1 6.67
CHEMBL537177 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL540818 Ki = 17.5 nM 7.76
CHEMBL540563 Ki = 17.9 nM 7.75
CHEMBL545278 Ki = 17.9 nM 7.75
CHEMBL558980 Ki = 26.2 nM 7.58
CHEMBL536483 Ki = 26.3 nM 7.58
CHEMBL554450 Ki = 28.6 nM 7.54
CHEMBL539545 Ki = 29.5 nM 7.53
CHEMBL534695 Ki = 31.4 nM 7.50
CHEMBL538566 Ki = 31.4 nM 7.50
CHEMBL282433 DITOLYLGUANIDINE Ki = 32.3 nM 7.49
CHEMBL545508 Ki = 32.7 nM 7.49
CHEMBL540573 Ki = 36.3 nM 7.44
CHEMBL559178 Ki = 38.9 nM 7.41
CHEMBL535363 Ki = 49.2 nM 7.31
CHEMBL537842 Ki = 48.7 nM 7.31
CHEMBL559377 Ki = 53.8 nM 7.27
CHEMBL554663 Ki = 59.3 nM 7.23
CHEMBL552542 Ki = 60.2 nM 7.22
CHEMBL539333 Ki = 64.0 nM 7.19
CHEMBL544343 Ki = 67.4 nM 7.17
CHEMBL542701 Ki = 86.2 nM 7.06
CHEMBL540361 Ki = 94.0 nM 7.03
CHEMBL538772 Ki = 104.0 nM 6.98
CHEMBL537399 Ki = 115.0 nM 6.94
CHEMBL535366 Ki = 151.0 nM 6.82
CHEMBL553091 Ki = 175.0 nM 6.76
CHEMBL190883 Ki = 212.0 nM 6.67
CHEMBL537177 Ki = 238.0 nM 6.62