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Assay Detail

CHEMBL4835169

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Functional
Agonist activity at human MT1 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by AlphaScreen assay
3
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Melatonin receptor type 1A (CHEMBL1945)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Potent and Orally Bioavailable Melatonin Receptor Agonist.
Hoashi Y, Takai T, Kosugi Y, Nakashima M, Nakayama M, Hirai K, Uchikawa O, Koike T.
J Med Chem (2021) 64 : 3059 -3074
PubMed 33682410 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 10.74 10.82
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3648356 1 10.82
CHEMBL45 MELATONIN 4.0 2 10.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3648356 EC50 = 0.015 nM 10.82
CHEMBL45 MELATONIN EC50 = 0.022 nM 10.66
CHEMBL45 MELATONIN Activity - -