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Assay Detail

CHEMBL4830552

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Functional
Agonist activity at 5HT1F receptor (unknown origin) expressed in HEK293 cells measured after 60 mins by Fluo-4AM dye based FLIPR assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 1F (CHEMBL1805)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of pyridinylmethylenepiperidine derivatives as potent 5-HT<sub>1F</sub> receptor agonists for migraine therapy.
Jin C, Yi C, Zhong W, Xue Y, Chen K, Deng K, Wang Z, Wang T.
Eur J Med Chem (2021) 225 : 113782 -113782
PubMed 34419891 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.27 8.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4847626 1 8.33
CHEMBL4846825 1 8.20
CHEMBL4851044 1 7.71
CHEMBL4865700 1 7.63
CHEMBL4860576 1 7.61
CHEMBL4862526 1 7.53
CHEMBL3039520 LASMIDITAN 4.0 1 7.06
CHEMBL4852743 1 6.79
CHEMBL4874958 1 6.75
CHEMBL4872571 1 6.24
CHEMBL4871295 1 6.09
CHEMBL4861949 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4847626 IC50 = 4.67 nM 8.33
CHEMBL4846825 IC50 = 6.36 nM 8.20
CHEMBL4851044 IC50 = 19.55 nM 7.71
CHEMBL4865700 IC50 = 23.41 nM 7.63
CHEMBL4860576 IC50 = 24.32 nM 7.61
CHEMBL4862526 IC50 = 29.35 nM 7.53
CHEMBL3039520 LASMIDITAN IC50 = 87.84 nM 7.06
CHEMBL4852743 IC50 = 160.9 nM 6.79
CHEMBL4874958 IC50 = 178.05 nM 6.75
CHEMBL4872571 IC50 = 570.5 nM 6.24
CHEMBL4871295 IC50 = 813.4 nM 6.09
CHEMBL4861949 IC50 > 10000.0 nM -