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Assay Detail

CHEMBL4371156

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Functional
Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.
Meanwell NA.
J Med Chem (2018) 61 : 5822 -5880
PubMed 29400967 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.57 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL439849 VILAZODONE 4.0 1 9.70
CHEMBL188799 1 9.15
CHEMBL189709 1 9.00
CHEMBL360390 1 8.52
CHEMBL188798 1 8.40
CHEMBL186655 1 8.30
CHEMBL364610 1 8.10
CHEMBL360407 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL439849 VILAZODONE IC50 = 0.2 nM 9.70
CHEMBL188799 IC50 = 0.7 nM 9.15
CHEMBL189709 IC50 = 1.0 nM 9.00
CHEMBL360390 IC50 = 3.0 nM 8.52
CHEMBL188798 IC50 = 4.0 nM 8.40
CHEMBL186655 IC50 = 5.0 nM 8.30
CHEMBL364610 IC50 = 8.0 nM 8.10
CHEMBL360407 IC50 = 40.0 nM 7.40