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Assay Detail

CHEMBL4733430

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

Binding
Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membranes after 120 mins by microbeta scintillation counting method
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL4153)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Synthesis, binding, and functional properties of tetrahydroisoquinolino-2-alkyl phenones as selective σR/TMEM97 ligands.
Xie XY,Li YY,Ma WH,Chen AF,Sun YT,Lee JY,Riad A,Xu DH,Mach RH,Huang YS
Eur J Med Chem (2021) 209 : 112906 -112906
PubMed 33049607 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.92 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.48
CHEMBL4739972 1 6.79
CHEMBL4778965 1 5.50
CHEMBL4759158 1 -
CHEMBL4749663 1 -
CHEMBL4778377 1 -
CHEMBL4763056 1 -
CHEMBL4740343 1 -
CHEMBL4796195 1 -
CHEMBL4747537 1 -
CHEMBL4744466 1 -
CHEMBL4760742 1 -
CHEMBL4744206 1 -
CHEMBL4746910 1 -
CHEMBL4761905 1 -
CHEMBL4765186 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 3.27 nM 8.48
CHEMBL4739972 Ki = 160.2 nM 6.79
CHEMBL4778965 Ki = 3192.0 nM 5.50
CHEMBL4759158 Ki > 1000.0 nM -
CHEMBL4749663 Ki > 1000.0 nM -
CHEMBL4778377 Ki > 1000.0 nM -
CHEMBL4763056 Ki > 1000.0 nM -
CHEMBL4740343 Ki > 1000.0 nM -
CHEMBL4796195 Ki > 1000.0 nM -
CHEMBL4747537 Ki > 1000.0 nM -
CHEMBL4744466 Ki > 1000.0 nM -
CHEMBL4760742 Ki > 1000.0 nM -
CHEMBL4744206 Ki > 1000.0 nM -
CHEMBL4746910 Ki > 1000.0 nM -
CHEMBL4761905 Ki > 1000.0 nM -
CHEMBL4765186 Ki > 1000.0 nM -