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Assay Detail

CHEMBL808906

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

Binding
Binding affinity for sigma-2 receptor measured on rat liver membranes using [3H]DTG as radioligand in the presence of (+)-pentazocine
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Synthesis and structure-activity relationships of naphthamides as dopamine D3 receptor ligands.
Huang Y, Luedtke RR, Freeman RA, Wu L, Mach RH.
J Med Chem (2001) 44 : 1815 -1826
PubMed 11356115 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 7.40 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL51856 1 8.68
CHEMBL53401 1 8.62
CHEMBL53078 1 8.59
CHEMBL423122 1 8.32
CHEMBL54092 1 8.17
CHEMBL298864 1 8.10
CHEMBL54026 1 8.01
CHEMBL53320 1 8.00
CHEMBL54027 1 7.82
CHEMBL54667 1 7.77
CHEMBL298875 1 7.68
CHEMBL51754 1 7.67
CHEMBL54865 1 7.60
CHEMBL53038 1 7.60
CHEMBL53778 1 7.57
CHEMBL416481 1 7.46
CHEMBL50465 1 7.38
CHEMBL301732 1 7.36
CHEMBL54571 1 7.29
CHEMBL50352 1 7.26
CHEMBL52300 1 7.24
CHEMBL52298 1 7.16
CHEMBL50517 1 7.02
CHEMBL416846 1 6.86
CHEMBL53218 1 6.85
CHEMBL52835 1 6.83
CHEMBL298759 1 6.82
CHEMBL53102 1 6.68
CHEMBL53650 1 6.65
CHEMBL52588 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL51856 Ki = 2.1 nM 8.68
CHEMBL53401 Ki = 2.4 nM 8.62
CHEMBL53078 Ki = 2.6 nM 8.59
CHEMBL423122 Ki = 4.8 nM 8.32
CHEMBL54092 Ki = 6.8 nM 8.17
CHEMBL298864 Ki = 7.9 nM 8.10
CHEMBL54026 Ki = 9.8 nM 8.01
CHEMBL53320 Ki = 10.0 nM 8.00
CHEMBL54027 Ki = 15.3 nM 7.82
CHEMBL54667 Ki = 17.0 nM 7.77
CHEMBL298875 Ki = 20.8 nM 7.68
CHEMBL51754 Ki = 21.4 nM 7.67
CHEMBL54865 Ki = 25.0 nM 7.60
CHEMBL53038 Ki = 25.0 nM 7.60
CHEMBL53778 Ki = 27.0 nM 7.57
CHEMBL416481 Ki = 35.0 nM 7.46
CHEMBL50465 Ki = 42.0 nM 7.38
CHEMBL301732 Ki = 44.0 nM 7.36
CHEMBL54571 Ki = 51.0 nM 7.29
CHEMBL50352 Ki = 55.0 nM 7.26
CHEMBL52300 Ki = 57.0 nM 7.24
CHEMBL52298 Ki = 70.0 nM 7.16
CHEMBL50517 Ki = 95.0 nM 7.02
CHEMBL416846 Ki = 137.0 nM 6.86
CHEMBL53218 Ki = 141.0 nM 6.85
CHEMBL52835 Ki = 147.0 nM 6.83
CHEMBL298759 Ki = 152.0 nM 6.82
CHEMBL53102 Ki = 207.0 nM 6.68
CHEMBL53650 Ki = 222.0 nM 6.65
CHEMBL52588 Ki = 250.0 nM 6.60
CHEMBL54662 Ki = 267.0 nM 6.57
CHEMBL301302 Ki = 279.0 nM 6.55
CHEMBL301929 Ki = 317.0 nM 6.50
CHEMBL54866 Ki = 419.0 nM 6.38