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Assay Detail

CHEMBL715947

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

Binding
Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

The development of a charged melatonin receptor ligand
Li P, Chu G, Gillen ML, Parekh T, Witt-Enderby PA
Bioorg Med Chem Lett (1997) 7 : 2409 -2414
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 8.25 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL289233 IODOMELATONIN 1 10.10
CHEMBL291857 1 10.00
CHEMBL45 MELATONIN 4.0 1 9.70
CHEMBL80736 1 9.41
CHEMBL440692 1 8.66
CHEMBL78751 1 8.37
CHEMBL82135 1 8.11
CHEMBL311106 1 8.09
CHEMBL80792 1 7.38
CHEMBL78338 1 7.03
CHEMBL79224 1 7.00
CHEMBL59 DOPAMINE 4.0 1 5.15
CHEMBL39 SEROTONIN 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL289233 IODOMELATONIN Ki = 0.08 nM 10.10
CHEMBL291857 Ki = 0.099 nM 10.00
CHEMBL45 MELATONIN Ki = 0.2 nM 9.70
CHEMBL80736 Ki = 0.39 nM 9.41
CHEMBL440692 Ki = 2.2 nM 8.66
CHEMBL78751 Ki = 4.3 nM 8.37
CHEMBL82135 Ki = 7.7 nM 8.11
CHEMBL311106 Ki = 8.1 nM 8.09
CHEMBL80792 Ki = 42.0 nM 7.38
CHEMBL78338 Ki = 93.0 nM 7.03
CHEMBL79224 Ki = 100.0 nM 7.00
CHEMBL59 DOPAMINE Ki = 7100.0 nM 5.15
CHEMBL39 SEROTONIN Ki > 100000.0 nM -