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Assay Detail

CHEMBL4713198

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

Binding
Displacement of [3H]ketanserin from human 5-HT2A receptor expressed in CHO-K1 cells incubated for 1 hr by radioligand binding assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

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 6.39 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL493054 1 6.47
CHEMBL319706 (S)-IFENPRODIL 1 6.43
CHEMBL49623 (R,S)-IFENPRODIL 1 6.38
CHEMBL113830 (S,R)-IFENPRODIL 1 6.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL493054 Ki = 338.0 nM 6.47
CHEMBL319706 (S)-IFENPRODIL Ki = 369.0 nM 6.43
CHEMBL49623 (R,S)-IFENPRODIL Ki = 421.0 nM 6.38
CHEMBL113830 (S,R)-IFENPRODIL Ki = 510.0 nM 6.29