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Assay Detail

CHEMBL1775440

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 assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers
4
Total Activities
4
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 1A (CHEMBL1945)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1,6-Dihydro-2H-indeno[5,4-b]furan derivatives: design, synthesis, and pharmacological characterization of a novel class of highly potent MT₂-selective agonists.
Koike T, Hoashi Y, Takai T, Nakayama M, Yukuhiro N, Ishikawa T, Hirai K, Uchikawa O.
J Med Chem (2011) 54 : 3436 -3444
PubMed 21473625 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 9.19 10.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45 MELATONIN 4.0 1 10.59
CHEMBL1774518 1 9.29
CHEMBL1774529 1 8.52
CHEMBL1774519 1 8.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45 MELATONIN EC50 = 0.0257 nM 10.59
CHEMBL1774518 EC50 = 0.5129 nM 9.29
CHEMBL1774529 EC50 = 3.02 nM 8.52
CHEMBL1774519 EC50 = 4.467 nM 8.35