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Assay Detail

CHEMBL811340

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Binding
Binding affinity for sigma-1 receptor measured on guinea pig brain membranes using [3H](+)-pentazocine as radioligand.
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL287)
Type SINGLE PROTEIN
Organism Homo sapiens

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 7.89 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54027 1 9.15
CHEMBL53078 1 8.96
CHEMBL51856 1 8.96
CHEMBL54026 1 8.92
CHEMBL54092 1 8.92
CHEMBL53320 1 8.77
CHEMBL53401 1 8.72
CHEMBL54571 1 8.60
CHEMBL50465 1 8.49
CHEMBL53778 1 8.44
CHEMBL298759 1 8.40
CHEMBL54667 1 8.32
CHEMBL54865 1 8.24
CHEMBL298875 1 8.23
CHEMBL301302 1 8.21
CHEMBL51754 1 8.21
CHEMBL301732 1 7.90
CHEMBL54662 1 7.78
CHEMBL53038 1 7.68
CHEMBL53218 1 7.63
CHEMBL52298 1 7.55
CHEMBL416481 1 7.51
CHEMBL50517 1 7.32
CHEMBL53650 1 7.25
CHEMBL52835 1 7.24
CHEMBL52300 1 7.23
CHEMBL423122 1 7.16
CHEMBL52588 1 7.13
CHEMBL298864 1 7.02
CHEMBL50352 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54027 Ki = 0.7 nM 9.15
CHEMBL53078 Ki = 1.1 nM 8.96
CHEMBL51856 Ki = 1.1 nM 8.96
CHEMBL54026 Ki = 1.2 nM 8.92
CHEMBL54092 Ki = 1.2 nM 8.92
CHEMBL53320 Ki = 1.7 nM 8.77
CHEMBL53401 Ki = 1.9 nM 8.72
CHEMBL54571 Ki = 2.5 nM 8.60
CHEMBL50465 Ki = 3.2 nM 8.49
CHEMBL53778 Ki = 3.6 nM 8.44
CHEMBL298759 Ki = 4.0 nM 8.40
CHEMBL54667 Ki = 4.8 nM 8.32
CHEMBL54865 Ki = 5.8 nM 8.24
CHEMBL298875 Ki = 5.9 nM 8.23
CHEMBL51754 Ki = 6.2 nM 8.21
CHEMBL301302 Ki = 6.2 nM 8.21
CHEMBL301732 Ki = 12.7 nM 7.90
CHEMBL54662 Ki = 16.7 nM 7.78
CHEMBL53038 Ki = 20.7 nM 7.68
CHEMBL53218 Ki = 23.4 nM 7.63
CHEMBL52298 Ki = 28.0 nM 7.55
CHEMBL416481 Ki = 31.0 nM 7.51
CHEMBL50517 Ki = 48.0 nM 7.32
CHEMBL53650 Ki = 56.0 nM 7.25
CHEMBL52835 Ki = 57.0 nM 7.24
CHEMBL52300 Ki = 59.0 nM 7.23
CHEMBL423122 Ki = 69.0 nM 7.16
CHEMBL52588 Ki = 74.0 nM 7.13
CHEMBL298864 Ki = 96.0 nM 7.02
CHEMBL50352 Ki = 121.0 nM 6.92
CHEMBL53102 Ki = 230.0 nM 6.64
CHEMBL301929 Ki = 375.0 nM 6.43
CHEMBL416846 Ki = 400.0 nM 6.40
CHEMBL54866 Ki > 1000.0 nM -