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Assay Detail

CHEMBL960190

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Functional
Agonist activity at human MT2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design and synthesis of 3-phenyltetrahydronaphthalenic derivatives as new selective MT2 melatoninergic ligands. Part II.
Durieux S, Chanu A, Bochu C, Audinot V, Coumailleau S, Boutin JA, Delagrange P, Caignard DH, Bennejean C, Renard P, Lesieur D, Berthelot P, Yous S.
Bioorg Med Chem (2009) 17 : 2963 -2974
PubMed 19329323 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 9.18 9.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL491249 1 9.39
CHEMBL45 MELATONIN 4.0 1 9.31
CHEMBL491058 1 9.13
CHEMBL522811 1 8.89
CHEMBL491052 1 -
CHEMBL523768 1 -
CHEMBL477048 1 -
CHEMBL477447 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL491249 EC50 = 0.41 nM 9.39
CHEMBL45 MELATONIN EC50 = 0.49 nM 9.31
CHEMBL491058 EC50 = 0.74 nM 9.13
CHEMBL522811 EC50 = 1.28 nM 8.89
CHEMBL491052 EC50 - -
CHEMBL523768 EC50 - -
CHEMBL477048 EC50 - -
CHEMBL477447 EC50 - -