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Assay Detail

CHEMBL976157

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Functional
Agonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

8-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors--part II.
Bromidge SM, Bertani B, Borriello M, Bozzoli A, Faedo S, Gianotti M, Gordon LJ, Hill M, Zucchelli V, Watson JM, Zonzini L.
Bioorg Med Chem Lett (2009) 19 : 2338 -2342
PubMed 19286377 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 7.70 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL472289 1 8.20
CHEMBL470849 1 7.80
CHEMBL469376 1 7.60
CHEMBL469375 1 7.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL472289 EC50 = 6.31 nM 8.20
CHEMBL470849 EC50 = 15.85 nM 7.80
CHEMBL469376 EC50 = 25.12 nM 7.60
CHEMBL469375 EC50 = 63.1 nM 7.20