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Assay Detail

CHEMBL1947484

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

Binding
Displacement of [125I]iodomelatonin form human MT2 receptor expressed in HEK cells after 120 mins
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design, synthesis and pharmacological evaluation of new series of naphthalenic analogues as melatoninergic (MT1/MT2) and serotoninergic 5-HT2C dual ligands (I).
Ettaoussi M, Sabaouni A, Rami M, Boutin JA, Delagrange P, Renard P, Spedding M, Caignard DH, Berthelot P, Yous S.
Eur J Med Chem (2012) 49 : 310 -323
PubMed 22301214 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 9.01 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1946226 1 11.00
CHEMBL1946224 1 10.40
CHEMBL342432 1 10.22
CHEMBL1946220 1 10.15
CHEMBL1946232 1 10.15
CHEMBL10878 AGOMELATINE 4.0 1 9.92
CHEMBL1946233 1 9.89
CHEMBL1946234 1 9.74
CHEMBL139410 1 9.55
CHEMBL1946229 1 9.49
CHEMBL1946235 1 9.41
CHEMBL1946227 1 9.32
CHEMBL1946704 1 9.25
CHEMBL1946222 1 9.23
CHEMBL1946705 1 9.01
CHEMBL1946707 1 8.98
CHEMBL1946231 1 8.96
CHEMBL1946708 1 8.92
CHEMBL1946225 1 8.87
CHEMBL1946236 1 8.46
CHEMBL1946709 1 8.42
CHEMBL1946228 1 8.38
CHEMBL1946221 1 8.37
CHEMBL1946223 1 8.06
CHEMBL1946706 1 8.06
CHEMBL138201 1 8.00
CHEMBL1946702 1 7.19
CHEMBL1946230 1 7.05
CHEMBL1946703 1 6.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1946226 Ki = 0.01 nM 11.00
CHEMBL1946224 Ki = 0.04 nM 10.40
CHEMBL342432 Ki = 0.06 nM 10.22
CHEMBL1946220 Ki = 0.07 nM 10.15
CHEMBL1946232 Ki = 0.07 nM 10.15
CHEMBL10878 AGOMELATINE Ki = 0.12 nM 9.92
CHEMBL1946233 Ki = 0.13 nM 9.89
CHEMBL1946234 Ki = 0.18 nM 9.74
CHEMBL139410 Ki = 0.28 nM 9.55
CHEMBL1946229 Ki = 0.32 nM 9.49
CHEMBL1946235 Ki = 0.39 nM 9.41
CHEMBL1946227 Ki = 0.48 nM 9.32
CHEMBL1946704 Ki = 0.56 nM 9.25
CHEMBL1946222 Ki = 0.59 nM 9.23
CHEMBL1946705 Ki = 0.98 nM 9.01
CHEMBL1946707 Ki = 1.05 nM 8.98
CHEMBL1946231 Ki = 1.1 nM 8.96
CHEMBL1946708 Ki = 1.19 nM 8.92
CHEMBL1946225 Ki = 1.34 nM 8.87
CHEMBL1946236 Ki = 3.5 nM 8.46
CHEMBL1946709 Ki = 3.8 nM 8.42
CHEMBL1946228 Ki = 4.2 nM 8.38
CHEMBL1946221 Ki = 4.3 nM 8.37
CHEMBL1946223 Ki = 8.7 nM 8.06
CHEMBL1946706 Ki = 8.7 nM 8.06
CHEMBL138201 Ki = 9.9 nM 8.00
CHEMBL1946702 Ki = 64.0 nM 7.19
CHEMBL1946230 Ki = 88.3 nM 7.05
CHEMBL1946703 Ki = 124.0 nM 6.91