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Assay Detail

CHEMBL809876

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

Binding
Binding affinity for sigma receptor of guinea pig whole brain using [3H]-SKF- 100047 radioligand
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Piperidinyltetralin sigma ligands.
Gilligan PJ, Kergaye AA, Lewis BM, McElroy JF.
J Med Chem (1994) 37 : 364 -370
PubMed 7905926 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 7.91 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL554874 1 9.00
CHEMBL544123 1 8.72
CHEMBL122165 1 8.70
CHEMBL554437 1 8.70
CHEMBL303336 1 8.62
CHEMBL542709 1 8.52
CHEMBL331470 1 8.40
CHEMBL544594 1 8.40
CHEMBL545285 1 8.40
CHEMBL542942 1 8.36
CHEMBL543889 1 8.30
CHEMBL123014 1 8.15
CHEMBL124234 1 8.10
CHEMBL122538 1 8.05
CHEMBL545058 1 8.05
CHEMBL539288 1 8.00
CHEMBL543412 1 8.00
CHEMBL545287 1 7.96
CHEMBL123937 1 7.96
CHEMBL331172 1 7.89
CHEMBL330865 1 7.89
CHEMBL542462 1 7.82
CHEMBL552572 1 7.72
CHEMBL123488 1 7.62
CHEMBL124411 1 7.58
CHEMBL543176 1 7.58
CHEMBL542217 1 7.58
CHEMBL122761 1 7.46
CHEMBL553311 1 7.34
CHEMBL554873 1 7.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL554874 Ki = 1.0 nM 9.00
CHEMBL544123 Ki = 1.9 nM 8.72
CHEMBL122165 Ki = 2.0 nM 8.70
CHEMBL554437 Ki = 2.0 nM 8.70
CHEMBL303336 Ki = 2.4 nM 8.62
CHEMBL542709 Ki = 3.0 nM 8.52
CHEMBL331470 Ki = 4.0 nM 8.40
CHEMBL544594 Ki = 4.0 nM 8.40
CHEMBL545285 Ki = 4.0 nM 8.40
CHEMBL542942 Ki = 4.4 nM 8.36
CHEMBL543889 Ki = 5.0 nM 8.30
CHEMBL123014 Ki = 7.0 nM 8.15
CHEMBL124234 Ki = 8.0 nM 8.10
CHEMBL122538 Ki = 9.0 nM 8.05
CHEMBL545058 Ki = 9.0 nM 8.05
CHEMBL543412 Ki = 10.0 nM 8.00
CHEMBL539288 Ki = 10.0 nM 8.00
CHEMBL545287 Ki = 11.0 nM 7.96
CHEMBL123937 Ki = 11.0 nM 7.96
CHEMBL331172 Ki = 13.0 nM 7.89
CHEMBL330865 Ki = 13.0 nM 7.89
CHEMBL542462 Ki = 15.0 nM 7.82
CHEMBL552572 Ki = 19.0 nM 7.72
CHEMBL123488 Ki = 24.0 nM 7.62
CHEMBL124411 Ki = 26.0 nM 7.58
CHEMBL542217 Ki = 26.0 nM 7.58
CHEMBL543176 Ki = 26.0 nM 7.58
CHEMBL122761 Ki = 35.0 nM 7.46
CHEMBL553311 Ki = 46.0 nM 7.34
CHEMBL554873 Ki = 56.0 nM 7.25
CHEMBL122758 Ki = 174.0 nM 6.76
CHEMBL275707 RIMCAZOLE Ki = 820.0 nM 6.09
CHEMBL542946 Ki = 1042.0 nM 5.98