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Assay Detail

CHEMBL4711048

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Functional
Inverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NG108-15
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 6 (CHEMBL3371)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A dual-acting 5-HT receptor inverse agonist/MAO-B inhibitor displays glioprotective and pro-cognitive properties.
Canale V,Grychowska K,Kurczab R,Ryng M,Keeri AR,Satała G,Olejarz-Maciej A,Koczurkiewicz P,Drop M,Blicharz K,Piska K,Pękala E,Janiszewska P,Krawczyk M,Walczak M,Chaumont-Dubel S,Bojarski AJ,Marin P,Popik P,Zajdel P
Eur J Med Chem (2020) 208 : 112765 -112765
PubMed 32949963 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.54 7.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1083390 INTEPIRDINE 3.0 1 7.01
CHEMBL4741978 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1083390 INTEPIRDINE IC50 = 97.0 nM 7.01
CHEMBL4741978 IC50 = 860.0 nM 6.07