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Assay Detail

CHEMBL3107214

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

Functional
Intrinsic activity at human melatonin MT2 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr
17
Total Activities
17
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

New melatonin (MT1/MT2) ligands: design and synthesis of (8,9-dihydro-7H-furo[3,2-f]chromen-1-yl) derivatives.
Landagaray E, Ettaoussi M, Leclerc V, Traoré B, Perez V, Nosjean O, Boutin JA, Caignard DH, Delagrange P, Berthelot P, Yous S.
Bioorg Med Chem (2014) 22 : 986 -996
PubMed 24417958 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 8.94 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3103593 1 10.15
CHEMBL3103597 1 10.10
CHEMBL3103583 1 10.00
CHEMBL138321 1 9.72
CHEMBL3103595 1 9.70
CHEMBL3103598 1 9.68
CHEMBL3103594 1 9.68
CHEMBL3103596 1 9.52
CHEMBL45 MELATONIN 4.0 1 9.40
CHEMBL323332 1 9.15
CHEMBL3103585 1 8.82
CHEMBL3103586 1 7.85
CHEMBL3103575 1 7.80
CHEMBL3103590 1 7.42
CHEMBL3103584 1 7.29
CHEMBL3103580 1 6.83
CHEMBL3103587 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3103593 EC50 = 0.07 nM 10.15
CHEMBL3103597 EC50 = 0.08 nM 10.10
CHEMBL3103583 EC50 = 0.1 nM 10.00
CHEMBL138321 EC50 = 0.19 nM 9.72
CHEMBL3103595 EC50 = 0.2 nM 9.70
CHEMBL3103598 EC50 = 0.21 nM 9.68
CHEMBL3103594 EC50 = 0.21 nM 9.68
CHEMBL3103596 EC50 = 0.3 nM 9.52
CHEMBL45 MELATONIN EC50 = 0.4 nM 9.40
CHEMBL323332 EC50 = 0.7 nM 9.15
CHEMBL3103585 EC50 = 1.5 nM 8.82
CHEMBL3103586 EC50 = 14.0 nM 7.85
CHEMBL3103575 EC50 = 16.0 nM 7.80
CHEMBL3103590 EC50 = 38.0 nM 7.42
CHEMBL3103584 EC50 = 51.0 nM 7.29
CHEMBL3103580 EC50 = 149.0 nM 6.83
CHEMBL3103587 EC50 > 10000.0 nM -