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Assay Detail

CHEMBL803916

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

Binding
Binding affinity against sigma sites in guinea pig membrane using [3H]DTG as the radioligand
ChEMBL ↗
46
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
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 in vitro evaluation of 5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indoles: high-affinity ligands for the N,N'-di-o-tolylguanidine-labeled sigma binding site.
Mewshaw RE, Sherrill RG, Mathew RM, Kaiser C, Bailey MA, Karbon EW.
J Med Chem (1993) 36 : 343 -352
PubMed 8426363 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 6.66 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL119867 — — 1 7.68
CHEMBL38130 — — 1 7.60
CHEMBL117898 — — 4 7.55
CHEMBL38152 — — 1 7.43
CHEMBL35711 — — 1 7.42
CHEMBL325168 — — 1 7.36
CHEMBL116711 — — 1 7.27
CHEMBL285203 — — 1 7.27
CHEMBL119811 — — 1 7.26
CHEMBL115582 — — 1 7.18
CHEMBL333840 — — 1 7.09
CHEMBL117567 — — 1 7.07
CHEMBL119047 — — 1 7.06
CHEMBL332035 — — 1 6.97
CHEMBL332593 — — 1 6.96
CHEMBL119075 — — 1 6.94
CHEMBL36645 — — 1 6.89
CHEMBL119048 — — 1 6.88
CHEMBL119485 — — 1 6.88
CHEMBL116207 — — 1 6.85
CHEMBL442395 — — 1 6.74
CHEMBL433022 — — 1 6.67
CHEMBL119889 — — 1 6.64
CHEMBL119804 — — 1 6.63
CHEMBL324092 — — 1 6.60
CHEMBL331500 — — 1 6.57
CHEMBL119409 — — 1 6.50
CHEMBL118288 — — 1 6.46
CHEMBL118289 — — 1 6.40
CHEMBL118665 — — 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL119867 — IC50 = 21.0 nM 7.68
CHEMBL38130 — IC50 = 25.0 nM 7.60
CHEMBL117898 — IC50 = 28.0 nM 7.55
CHEMBL117898 — IC50 = 28.0 nM 7.55
CHEMBL38152 — IC50 = 37.0 nM 7.43
CHEMBL35711 — IC50 = 38.0 nM 7.42
CHEMBL325168 — IC50 = 44.0 nM 7.36
CHEMBL117898 — IC50 = 46.0 nM 7.34
CHEMBL285203 — IC50 = 54.0 nM 7.27
CHEMBL116711 — IC50 = 54.0 nM 7.27
CHEMBL119811 — IC50 = 55.0 nM 7.26
CHEMBL115582 — IC50 = 66.0 nM 7.18
CHEMBL333840 — IC50 = 81.0 nM 7.09
CHEMBL117567 — IC50 = 86.0 nM 7.07
CHEMBL119047 — IC50 = 88.0 nM 7.06
CHEMBL332035 — IC50 = 107.0 nM 6.97
CHEMBL332593 — IC50 = 110.0 nM 6.96
CHEMBL119075 — IC50 = 116.0 nM 6.94
CHEMBL36645 — IC50 = 129.0 nM 6.89
CHEMBL119485 — IC50 = 133.0 nM 6.88
CHEMBL119048 — IC50 = 132.0 nM 6.88
CHEMBL116207 — IC50 = 141.0 nM 6.85
CHEMBL117898 — IC50 = 170.0 nM 6.77
CHEMBL442395 — IC50 = 182.0 nM 6.74
CHEMBL433022 — IC50 = 212.0 nM 6.67
CHEMBL119889 — IC50 = 231.0 nM 6.64
CHEMBL119804 — IC50 = 234.0 nM 6.63
CHEMBL324092 — IC50 = 251.0 nM 6.60
CHEMBL331500 — IC50 = 267.0 nM 6.57
CHEMBL119409 — IC50 = 317.0 nM 6.50
CHEMBL118288 — IC50 = 345.0 nM 6.46
CHEMBL118289 — IC50 = 400.0 nM 6.40
CHEMBL118665 — IC50 = 482.0 nM 6.32
CHEMBL116710 — IC50 = 509.0 nM 6.29
CHEMBL325845 — IC50 = 683.0 nM 6.17
CHEMBL325619 — IC50 = 702.0 nM 6.15
CHEMBL119725 — IC50 = 836.0 nM 6.08
CHEMBL119495 — IC50 = 1084.0 nM 5.96
CHEMBL331611 — IC50 = 1483.0 nM 5.83
CHEMBL331006 — IC50 = 1473.0 nM 5.83
CHEMBL117748 — IC50 = 1612.0 nM 5.79
CHEMBL118445 — IC50 = 1895.0 nM 5.72
CHEMBL118276 — IC50 = 2650.0 nM 5.58
CHEMBL323910 — IC50 = 3044.0 nM 5.52
CHEMBL117695 — IC50 = 3560.0 nM 5.45
CHEMBL119698 — IC50 = 8085.0 nM 5.09