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Assay Detail

CHEMBL617005

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Functional
Agonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formation
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 1B (CHEMBL1898)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine.
Jorand-Lebrun C, Pauwels PJ, Palmier C, Moret C, Chopin P, Perez M, Marien M, Halazy S.
J Med Chem (1997) 40 : 3974 -3978
PubMed 9397179 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 7.57 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129813 1 7.60
CHEMBL128699 1 7.60
CHEMBL2112660 1 7.55
CHEMBL338015 1 7.52
CHEMBL277120 1 -
CHEMBL129661 1 -
CHEMBL340786 1 -
CHEMBL2112662 1 -
CHEMBL339308 1 -
CHEMBL2112661 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129813 EC50 = 25.0 nM 7.60
CHEMBL128699 EC50 = 25.0 nM 7.60
CHEMBL2112660 EC50 = 28.0 nM 7.55
CHEMBL338015 EC50 = 30.0 nM 7.52
CHEMBL277120 EC50 > 1000.0 nM -
CHEMBL129661 EC50 > 1000.0 nM -
CHEMBL340786 EC50 > 1000.0 nM -
CHEMBL2112662 EC50 > 1000.0 nM -
CHEMBL339308 EC50 > 1000.0 nM -
CHEMBL2112661 EC50 > 1000.0 nM -