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Assay Detail

CHEMBL803754

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](+)-3-PPP 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 6.30 7.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL116711 — — 1 7.12
CHEMBL116207 — — 1 7.07
CHEMBL119867 — — 1 7.01
CHEMBL117898 — — 4 6.98
CHEMBL38152 — — 1 6.97
CHEMBL325168 — — 1 6.94
CHEMBL38130 — — 1 6.94
CHEMBL115582 — — 1 6.87
CHEMBL119811 — — 1 6.83
CHEMBL35711 — — 1 6.75
CHEMBL119047 — — 1 6.69
CHEMBL119048 — — 1 6.58
CHEMBL36645 — — 1 6.55
CHEMBL442395 — — 1 6.55
CHEMBL119075 — — 1 6.55
CHEMBL332035 — — 1 6.46
CHEMBL333840 — — 1 6.43
CHEMBL331500 — — 1 6.40
CHEMBL116710 — — 1 6.32
CHEMBL118665 — — 1 6.31
CHEMBL119485 — — 1 6.29
CHEMBL332593 — — 1 6.27
CHEMBL119889 — — 1 6.15
CHEMBL118289 — — 1 6.11
CHEMBL117567 — — 1 6.04
CHEMBL285203 — — 1 6.00
CHEMBL331006 — — 1 5.92
CHEMBL433022 — — 1 5.92
CHEMBL119804 — — 1 5.89
CHEMBL119495 — — 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL116711 — IC50 = 76.0 nM 7.12
CHEMBL116207 — IC50 = 85.0 nM 7.07
CHEMBL119867 — IC50 = 98.0 nM 7.01
CHEMBL117898 — IC50 = 105.0 nM 6.98
CHEMBL117898 — IC50 = 105.0 nM 6.98
CHEMBL38152 — IC50 = 107.0 nM 6.97
CHEMBL117898 — IC50 = 108.0 nM 6.97
CHEMBL38130 — IC50 = 114.0 nM 6.94
CHEMBL325168 — IC50 = 114.0 nM 6.94
CHEMBL115582 — IC50 = 136.0 nM 6.87
CHEMBL119811 — IC50 = 148.0 nM 6.83
CHEMBL35711 — IC50 = 178.0 nM 6.75
CHEMBL119047 — IC50 = 205.0 nM 6.69
CHEMBL119048 — IC50 = 262.0 nM 6.58
CHEMBL119075 — IC50 = 281.0 nM 6.55
CHEMBL442395 — IC50 = 282.0 nM 6.55
CHEMBL36645 — IC50 = 283.0 nM 6.55
CHEMBL332035 — IC50 = 348.0 nM 6.46
CHEMBL333840 — IC50 = 368.0 nM 6.43
CHEMBL331500 — IC50 = 396.0 nM 6.40
CHEMBL116710 — IC50 = 474.0 nM 6.32
CHEMBL117898 — IC50 = 482.0 nM 6.32
CHEMBL118665 — IC50 = 487.0 nM 6.31
CHEMBL119485 — IC50 = 517.0 nM 6.29
CHEMBL332593 — IC50 = 534.0 nM 6.27
CHEMBL119889 — IC50 = 705.0 nM 6.15
CHEMBL118289 — IC50 = 782.0 nM 6.11
CHEMBL117567 — IC50 = 908.0 nM 6.04
CHEMBL285203 — IC50 = 988.0 nM 6.00
CHEMBL331006 — IC50 = 1212.0 nM 5.92
CHEMBL433022 — IC50 = 1210.0 nM 5.92
CHEMBL119495 — IC50 = 1276.0 nM 5.89
CHEMBL119804 — IC50 = 1280.0 nM 5.89
CHEMBL119409 — IC50 = 1382.0 nM 5.86
CHEMBL325845 — IC50 = 1763.0 nM 5.75
CHEMBL118276 — IC50 = 2005.0 nM 5.70
CHEMBL118288 — IC50 = 2750.0 nM 5.56
CHEMBL119725 — IC50 = 3332.0 nM 5.48
CHEMBL117695 — IC50 = 3840.0 nM 5.42
CHEMBL331611 — IC50 = 4007.0 nM 5.40
CHEMBL324092 — IC50 = 4876.0 nM 5.31
CHEMBL118445 — IC50 = 6605.0 nM 5.18
CHEMBL117748 — IC50 > 10000.0 nM -
CHEMBL323910 — IC50 > 10000.0 nM -
CHEMBL325619 — IC50 > 10000.0 nM -
CHEMBL119698 — IC50 > 10000.0 nM -