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Assay Detail

CHEMBL960184

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

Binding
Displacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design and synthesis of 3-phenyltetrahydronaphthalenic derivatives as new selective MT2 melatoninergic ligands. Part II.
Durieux S, Chanu A, Bochu C, Audinot V, Coumailleau S, Boutin JA, Delagrange P, Caignard DH, Bennejean C, Renard P, Lesieur D, Berthelot P, Yous S.
Bioorg Med Chem (2009) 17 : 2963 -2974
PubMed 19329323 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.08 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45 MELATONIN 4.0 1 9.85
CHEMBL477447 1 7.89
CHEMBL522811 1 7.69
CHEMBL491058 1 7.48
CHEMBL491249 1 7.46
CHEMBL491053 1 7.35
CHEMBL477448 1 7.29
CHEMBL515629 1 7.21
CHEMBL285718 1 6.97
CHEMBL489223 1 6.90
CHEMBL477048 1 6.61
CHEMBL489224 1 6.51
CHEMBL491052 1 6.36
CHEMBL443934 1 6.09
CHEMBL489825 1 6.01
CHEMBL523768 1 5.61
CHEMBL489416 1 -
CHEMBL517811 1 -
CHEMBL477662 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45 MELATONIN Ki = 0.14 nM 9.85
CHEMBL477447 Ki = 13.0 nM 7.89
CHEMBL522811 Ki = 20.5 nM 7.69
CHEMBL491058 Ki = 33.0 nM 7.48
CHEMBL491249 Ki = 35.0 nM 7.46
CHEMBL491053 Ki = 45.0 nM 7.35
CHEMBL477448 Ki = 51.0 nM 7.29
CHEMBL515629 Ki = 61.0 nM 7.21
CHEMBL285718 Ki = 108.0 nM 6.97
CHEMBL489223 Ki = 127.0 nM 6.90
CHEMBL477048 Ki = 247.0 nM 6.61
CHEMBL489224 Ki = 311.0 nM 6.51
CHEMBL491052 Ki = 439.0 nM 6.36
CHEMBL443934 Ki = 809.0 nM 6.09
CHEMBL489825 Ki = 981.0 nM 6.01
CHEMBL523768 Ki = 2480.0 nM 5.61
CHEMBL489416 Ki > 1000.0 nM -
CHEMBL517811 Ki > 1000.0 nM -
CHEMBL477662 Ki > 1000.0 nM -