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Assay Detail

CHEMBL987964

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

Binding
Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells
21
Total Activities
21
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 Autocuration

Target

Melatonin receptor type 1B (CHEMBL1946)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of 3-phenylnaphthalenic derivatives as new selective MT(2) melatoninergic ligands.
Poissonnier-Durieux S, Ettaoussi M, Pérès B, Boutin JA, Audinot V, Bennejean C, Delagrange P, Caignard DH, Renard P, Berthelot P, Lesieur D, Yous S.
Bioorg Med Chem (2008) 16 : 8339 -8348
PubMed 18778943 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 8.87 9.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL490188 1 9.57
CHEMBL10878 AGOMELATINE 4.0 1 9.57
CHEMBL476341 1 9.55
CHEMBL476131 1 9.44
CHEMBL453138 1 9.43
CHEMBL45 MELATONIN 4.0 1 9.39
CHEMBL491604 1 9.38
CHEMBL477835 1 9.29
CHEMBL518113 1 9.28
CHEMBL490595 1 9.25
CHEMBL491605 1 9.19
CHEMBL477833 1 9.15
CHEMBL478217 1 9.03
CHEMBL491403 1 9.02
CHEMBL517502 1 8.73
CHEMBL477834 1 8.47
CHEMBL489170 1 8.12
CHEMBL478218 1 8.08
CHEMBL476132 1 7.64
CHEMBL490594 1 7.36
CHEMBL478438 1 7.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL490188 Ki = 0.27 nM 9.57
CHEMBL10878 AGOMELATINE Ki = 0.27 nM 9.57
CHEMBL476341 Ki = 0.28 nM 9.55
CHEMBL476131 Ki = 0.36 nM 9.44
CHEMBL453138 Ki = 0.37 nM 9.43
CHEMBL45 MELATONIN Ki = 0.41 nM 9.39
CHEMBL491604 Ki = 0.42 nM 9.38
CHEMBL477835 Ki = 0.51 nM 9.29
CHEMBL518113 Ki = 0.52 nM 9.28
CHEMBL490595 Ki = 0.56 nM 9.25
CHEMBL491605 Ki = 0.64 nM 9.19
CHEMBL477833 Ki = 0.71 nM 9.15
CHEMBL478217 Ki = 0.94 nM 9.03
CHEMBL491403 Ki = 0.95 nM 9.02
CHEMBL517502 Ki = 1.86 nM 8.73
CHEMBL477834 Ki = 3.4 nM 8.47
CHEMBL489170 Ki = 7.54 nM 8.12
CHEMBL478218 Ki = 8.3 nM 8.08
CHEMBL476132 Ki = 23.0 nM 7.64
CHEMBL490594 Ki = 43.3 nM 7.36
CHEMBL478438 Ki = 48.3 nM 7.32