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Assay Detail

CHEMBL4709869

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

Functional
Antagonist activity at human 5HT7 receptor expressed in CHO-K1 cells assessed as inhibition of 5CT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5CT addition by calcium 4 dye based FLIPR assay
2
Total Activities
2
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

Isoquinolinone derivatives as potent CNS multi-receptor D/5-HT/5-HT/5-HT/5-HT agents: Synthesis and pharmacological evaluation.
Jin J,Zhang K,Dou F,Hao C,Zhang Y,Cao X,Gao L,Xiong J,Liu X,Liu BF,Zhang G,Chen Y
Eur J Med Chem (2020) 207 : 112709 -112709
PubMed 32877805 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.93 7.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93240 METITEPINE 2.0 1 7.95
CHEMBL4764679 1 7.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93240 METITEPINE IC50 = 11.3 nM 7.95
CHEMBL4764679 IC50 = 12.5 nM 7.90