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Assay Detail

CHEMBL4625531

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

Functional
Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 Hunter cell preincubated for 30 mins followed by incubation with agonist for 30 to 60 mins by hit-hunter cAMP assay based chemiluminescence analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 7 (CHEMBL3155)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structural manipulation of aporphines via C10 nitrogenation leads to the identification of new 5-HT<sub>7A</sub>R ligands.
Karki A, Namballa HK, Alberts I, Harding WW.
Bioorg Med Chem (2020) 28 : 115578 -115578
PubMed 32631561 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.66 6.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4636148 1 6.90
CHEMBL4633786 1 6.58
CHEMBL1256875 SPIPERONE HYDROCHLORIDE 1 6.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4636148 IC50 = 125.0 nM 6.90
CHEMBL4633786 IC50 = 260.0 nM 6.58
CHEMBL1256875 SPIPERONE HYDROCHLORIDE IC50 = 310.0 nM 6.51