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Assay Detail

CHEMBL4713193

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

Binding
Displacement of [3H](+)-pentazocine from sigma1 receptor in guinea pig brain membranes
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Subcellular Cell 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

Ifenprodil Stereoisomers: Synthesis, Absolute Configuration, and Correlation with Biological Activity.
Bechthold E,Schreiber JA,Lehmkuhl K,Frehland B,Schepmann D,Bernal FA,Daniliuc C,Álvarez I,Garcia CV,Schmidt TJ,Seebohm G,Wünsch B
J Med Chem (2021) 64 : 1170 -1179
PubMed 33426889 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.09 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49623 (R,S)-IFENPRODIL 1 7.66
CHEMBL113830 (S,R)-IFENPRODIL 1 7.12
CHEMBL493054 1 7.02
CHEMBL319706 (S)-IFENPRODIL 1 6.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49623 (R,S)-IFENPRODIL Ki = 22.0 nM 7.66
CHEMBL113830 (S,R)-IFENPRODIL Ki = 75.0 nM 7.12
CHEMBL493054 Ki = 96.0 nM 7.02
CHEMBL319706 (S)-IFENPRODIL Ki = 278.0 nM 6.56