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Assay Detail

CHEMBL1108343

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Agonist activity at human MT2 receptor expressed in CHO cells by [35S]GTPgamma binding assay
19
Total Activities
19
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

Design, synthesis and pharmacological evaluation of novel naphthalenic derivatives as selective MT(1) melatoninergic ligands.
Mésangeau C, Pérès B, Descamps-François C, Chavatte P, Audinot V, Coumailleau S, Boutin JA, Delagrange P, Bennejean C, Renard P, Caignard DH, Berthelot P, Yous S.
Bioorg Med Chem (2010) 18 : 3426 -3436
PubMed 20444610 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 7.68 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10878 AGOMELATINE 4.0 1 10.00
CHEMBL45 MELATONIN 4.0 1 9.31
CHEMBL1097497 1 7.69
CHEMBL1094212 1 7.58
CHEMBL1097315 1 7.40
CHEMBL1095197 1 7.06
CHEMBL1097314 1 6.87
CHEMBL1095505 1 6.79
CHEMBL14453 1 6.39
CHEMBL1097496 1 -
CHEMBL1095522 1 -
CHEMBL1095831 1 -
CHEMBL1095832 1 -
CHEMBL1096991 1 -
CHEMBL1095195 1 -
CHEMBL1095196 1 -
CHEMBL1095504 1 -
CHEMBL1094546 1 -
CHEMBL1094545 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10878 AGOMELATINE EC50 = 0.1 nM 10.00
CHEMBL45 MELATONIN EC50 = 0.49 nM 9.31
CHEMBL1097497 EC50 = 20.6 nM 7.69
CHEMBL1094212 EC50 = 26.0 nM 7.58
CHEMBL1097315 EC50 = 40.2 nM 7.40
CHEMBL1095197 EC50 = 88.0 nM 7.06
CHEMBL1097314 EC50 = 134.0 nM 6.87
CHEMBL1095505 EC50 = 161.0 nM 6.79
CHEMBL14453 EC50 = 405.0 nM 6.39
CHEMBL1097496 EC50 > 1e-05 nM -
CHEMBL1095522 EC50 > 1e-05 nM -
CHEMBL1095831 EC50 > 1e-05 nM -
CHEMBL1095832 EC50 > 1e-05 nM -
CHEMBL1096991 EC50 > 1e-05 nM -
CHEMBL1095195 EC50 > 1e-05 nM -
CHEMBL1095196 EC50 > 1e-05 nM -
CHEMBL1095504 EC50 > 1e-05 nM -
CHEMBL1094546 EC50 - -
CHEMBL1094545 EC50 > 1e-05 nM -