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Assay Detail

CHEMBL616718

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Functional
In vitro effective concentration for stimulation of [35S]GTP-gamma-S, binding in mouse LM(tk-)cells expressing the human 5-hydroxytryptamine 1F receptor
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Novel potent 5-HT(1F) receptor agonists: structure-activity studies of a series of substituted N-[3-(1-methyl-4-piperidinyl)-1H-pyrrolo[3,2-b]pyridin-5-yl]amides.
Filla SA, Mathes BM, Johnson KW, Phebus LA, Cohen ML, Nelson DL, Zgombick JM, Erickson JA, Schenck KW, Wainscott DB, Branchek TA, Schaus JM.
J Med Chem (2003) 46 : 3060 -3071
PubMed 12825944 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 7.79 8.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL104753 1 8.03
CHEMBL105958 1 7.96
CHEMBL105091 1 7.96
CHEMBL102250 1 7.96
CHEMBL105955 1 7.89
CHEMBL321080 1 7.82
CHEMBL420475 1 7.68
CHEMBL105722 1 7.60
CHEMBL105261 1 7.50
CHEMBL104720 1 7.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL104753 EC50 = 9.4 nM 8.03
CHEMBL105958 EC50 = 11.0 nM 7.96
CHEMBL105091 EC50 = 11.0 nM 7.96
CHEMBL102250 EC50 = 11.0 nM 7.96
CHEMBL105955 EC50 = 13.0 nM 7.89
CHEMBL321080 EC50 = 15.0 nM 7.82
CHEMBL420475 EC50 = 21.0 nM 7.68
CHEMBL105722 EC50 = 25.0 nM 7.60
CHEMBL105261 EC50 = 32.0 nM 7.50
CHEMBL104720 EC50 = 34.0 nM 7.47