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Assay Detail

CHEMBL4409671

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

Functional
Antagonist activity at 5HT7R receptor (unknown origin) assessed as forskolin-mediated cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by TR-FRET analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and antidepressant effect of novel aralkyl piperazine and piperidine derivatives targeting SSRI/5-HT1A/5-HT7.
Gu ZS, Wang WT, Qian H, Zhou AN, Sun HB, Zhang QW, Li JQ.
Bioorg Med Chem Lett (2019) 29 : 126703 -126703
PubMed 31627993 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.64 9.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93240 METITEPINE 2.0 1 9.09
CHEMBL4434876 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93240 METITEPINE IC50 = 0.82 nM 9.09
CHEMBL4434876 IC50 = 650.0 nM 6.19