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Assay Detail

CHEMBL1670260

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

Binding
Displacement of [3H]melatonin from rat MT1 receptor expressed in CHO-Galpha16 cells
ChEMBL ↗
43
Total Activities
34
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type CHO-Galpha16
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Design and synthesis of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives as novel melatonin receptor ligands.
Li G, Zhou H, Jiang Y, Keim H, Topiol SW, Poda SB, Ren Y, Chandrasena G, Doller D.
Bioorg Med Chem Lett (2011) 21 : 1236 -1242
PubMed 21237644 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 6.94 9.00
IC50 9 6.11 6.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45 MELATONIN 4.0 1 9.00
CHEMBL10878 AGOMELATINE 4.0 1 8.92
CHEMBL1669703 — — 2 8.92
CHEMBL1218 RAMELTEON 4.0 1 8.70
CHEMBL1669701 — — 2 8.00
CHEMBL1669700 — — 2 7.82
CHEMBL1669710 — — 1 7.68
CHEMBL1669685 — — 1 7.40
CHEMBL1669709 — — 1 7.12
CHEMBL1669704 — — 2 6.89
CHEMBL1669688 — — 1 6.85
CHEMBL1669686 — — 1 6.82
CHEMBL1669682 — — 1 6.80
CHEMBL1669706 — — 2 6.72
CHEMBL1669708 — — 2 6.42
CHEMBL1669705 — — 2 6.39
CHEMBL1669707 — — 2 6.21
CHEMBL1669691 — — 1 6.19
CHEMBL1669681 — — 1 6.09
CHEMBL1669702 — — 2 6.00
CHEMBL1669697 — — 1 5.96
CHEMBL1669699 — — 1 5.70
CHEMBL1669698 — — 1 5.33
CHEMBL1669692 — — 1 5.24
CHEMBL1669683 — — 1 -
CHEMBL1669693 — — 1 -
CHEMBL1669694 — — 1 -
CHEMBL1669695 — — 1 -
CHEMBL1669696 — — 1 -
CHEMBL1669690 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45 MELATONIN Ki = 0.99 nM 9.00
CHEMBL1669703 — Ki = 1.2 nM 8.92
CHEMBL10878 AGOMELATINE Ki = 1.2 nM 8.92
CHEMBL1218 RAMELTEON Ki = 2.0 nM 8.70
CHEMBL1669701 — Ki = 9.9 nM 8.00
CHEMBL1669700 — Ki = 15.0 nM 7.82
CHEMBL1669710 — Ki = 21.0 nM 7.68
CHEMBL1669685 — Ki = 40.0 nM 7.40
CHEMBL1669709 — Ki = 75.0 nM 7.12
CHEMBL1669704 — Ki = 130.0 nM 6.89
CHEMBL1669688 — Ki = 140.0 nM 6.85
CHEMBL1669686 — Ki = 150.0 nM 6.82
CHEMBL1669682 — Ki = 160.0 nM 6.80
CHEMBL1669706 — Ki = 190.0 nM 6.72
CHEMBL1669708 — IC50 = 380.0 nM 6.42
CHEMBL1669705 — Ki = 410.0 nM 6.39
CHEMBL1669704 — IC50 = 440.0 nM 6.36
CHEMBL1669707 — Ki = 610.0 nM 6.21
CHEMBL1669691 — Ki = 650.0 nM 6.19
CHEMBL1669681 — Ki = 810.0 nM 6.09
CHEMBL1669705 — IC50 = 870.0 nM 6.06
CHEMBL1669707 — IC50 = 930.0 nM 6.03
CHEMBL1669702 — Ki = 1000.0 nM 6.00
CHEMBL1669697 — Ki = 1100.0 nM 5.96
CHEMBL1669708 — Ki = 1500.0 nM 5.82
CHEMBL1669699 — Ki = 2000.0 nM 5.70
CHEMBL1669706 — IC50 = 2100.0 nM 5.68
CHEMBL1669698 — Ki = 4700.0 nM 5.33
CHEMBL1669692 — Ki = 5700.0 nM 5.24
CHEMBL1669703 — IC50 - — -
CHEMBL1669680 — Ki - — -
CHEMBL1669683 — Ki - — -
CHEMBL1669684 — Ki - — -
CHEMBL1669687 — Ki - — -
CHEMBL1669689 — Ki - — -
CHEMBL1669690 — Ki - — -
CHEMBL1669693 — Ki - — -
CHEMBL1669702 — IC50 - — -
CHEMBL1669695 — Ki - — -
CHEMBL1669696 — Ki - — -
CHEMBL1669694 — Ki - — -
CHEMBL1669701 — IC50 - — -
CHEMBL1669700 — IC50 > 10000.0 nM -