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Assay Detail

CHEMBL1947486

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

Functional
Agonist activity at human MT1 receptor expressed in CHO cells after 1 hr by [35S]GTPgammaS binding assay
15
Total Activities
15
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, synthesis and pharmacological evaluation of new series of naphthalenic analogues as melatoninergic (MT1/MT2) and serotoninergic 5-HT2C dual ligands (I).
Ettaoussi M, Sabaouni A, Rami M, Boutin JA, Delagrange P, Renard P, Spedding M, Caignard DH, Berthelot P, Yous S.
Eur J Med Chem (2012) 49 : 310 -323
PubMed 22301214 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 7.70 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1946221 1 10.22
CHEMBL1946233 1 9.02
CHEMBL10878 AGOMELATINE 4.0 1 8.89
CHEMBL1946220 1 8.75
CHEMBL1946222 1 8.10
CHEMBL1946235 1 7.85
CHEMBL1946708 1 7.68
CHEMBL342432 1 7.56
CHEMBL1946709 1 7.50
CHEMBL1946228 1 7.18
CHEMBL1946227 1 6.73
CHEMBL1946225 1 6.70
CHEMBL1946236 1 6.64
CHEMBL1946226 1 6.57
CHEMBL1946223 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1946221 EC50 = 0.06 nM 10.22
CHEMBL1946233 EC50 = 0.96 nM 9.02
CHEMBL10878 AGOMELATINE EC50 = 1.29 nM 8.89
CHEMBL1946220 EC50 = 1.79 nM 8.75
CHEMBL1946222 EC50 = 8.01 nM 8.10
CHEMBL1946235 EC50 = 14.2 nM 7.85
CHEMBL1946708 EC50 = 21.1 nM 7.68
CHEMBL342432 EC50 = 27.8 nM 7.56
CHEMBL1946709 EC50 = 31.8 nM 7.50
CHEMBL1946228 EC50 = 65.6 nM 7.18
CHEMBL1946227 EC50 = 185.0 nM 6.73
CHEMBL1946225 EC50 = 200.0 nM 6.70
CHEMBL1946236 EC50 = 227.0 nM 6.64
CHEMBL1946226 EC50 = 272.0 nM 6.57
CHEMBL1946223 EC50 = 789.0 nM 6.10