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Assay Detail

CHEMBL3583849

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Functional
Agonist activity at human recombinant melatonin receptor-2 expressed in CHO cells assessed as decrease of cAMP level after 10 mins by HTRF assay
2
Total Activities
2
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

Melatonin receptor type 1B (CHEMBL1946)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel N-Acetyl Bioisosteres of Melatonin: Melatonergic Receptor Pharmacology, Physicochemical Studies, and Phenotypic Assessment of Their Neurogenic Potential.
de la Fuente Revenga M, Fernández-Sáez N, Herrera-Arozamena C, Morales-García JA, Alonso-Gil S, Pérez-Castillo A, Caignard DH, Rivara S, Rodríguez-Franco MI.
J Med Chem (2015) 58 : 4998 -5014
PubMed 26023814 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.03 8.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3580919 1 8.26
CHEMBL3580916 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3580919 EC50 = 5.5 nM 8.26
CHEMBL3580916 EC50 = 1600.0 nM 5.80