Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL713111

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

Binding
Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand)
ChEMBL ↗
42
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Synthesis of phenalene and acenaphthene derivatives as new conformationally restricted ligands for melatonin receptors.
Jellimann C, Mathé-Allainmat M, Andrieux J, Kloubert S, Boutin JA, Nicolas JP, Bennejean C, Delagrange P, Langlois M.
J Med Chem (2000) 43 : 4051 -4062
PubMed 11063602 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 42 9.35 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL132802 — — 1 11.00
CHEMBL336054 — — 1 10.92
CHEMBL336509 — — 1 10.82
CHEMBL340832 — — 1 10.80
CHEMBL133416 — — 1 10.59
CHEMBL130214 — — 3 10.52
CHEMBL129890 — — 1 10.24
CHEMBL337024 — — 1 10.15
CHEMBL132340 — — 1 10.00
CHEMBL130542 — — 1 10.00
CHEMBL131424 — — 3 9.96
CHEMBL130490 — — 1 9.92
CHEMBL10878 AGOMELATINE 4.0 1 9.74
CHEMBL129889 — — 1 9.72
CHEMBL45 MELATONIN 4.0 1 9.70
CHEMBL130898 — — 1 9.70
CHEMBL336858 — — 1 9.66
CHEMBL434226 — — 1 9.43
CHEMBL130203 — — 1 9.39
CHEMBL131575 — — 1 9.18
CHEMBL337882 — — 1 9.10
CHEMBL336647 — — 1 9.10
CHEMBL130876 — — 1 9.02
CHEMBL341439 — — 1 8.97
CHEMBL130319 — — 1 8.92
CHEMBL338425 — — 1 8.89
CHEMBL334962 — — 1 8.88
CHEMBL336633 — — 1 8.72
CHEMBL340745 — — 1 8.68
CHEMBL133001 — — 1 8.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL132802 — Ki = 0.01 nM 11.00
CHEMBL336054 — Ki = 0.012 nM 10.92
CHEMBL336509 — Ki = 0.015 nM 10.82
CHEMBL340832 — Ki = 0.016 nM 10.80
CHEMBL133416 — Ki = 0.026 nM 10.59
CHEMBL130214 — Ki = 0.03 nM 10.52
CHEMBL129890 — Ki = 0.057 nM 10.24
CHEMBL337024 — Ki = 0.07 nM 10.15
CHEMBL130542 — Ki = 0.1 nM 10.00
CHEMBL132340 — Ki = 0.1 nM 10.00
CHEMBL131424 — Ki = 0.11 nM 9.96
CHEMBL130490 — Ki = 0.12 nM 9.92
CHEMBL10878 AGOMELATINE Ki = 0.18 nM 9.74
CHEMBL129889 — Ki = 0.19 nM 9.72
CHEMBL45 MELATONIN Ki = 0.2 nM 9.70
CHEMBL130898 — Ki = 0.2 nM 9.70
CHEMBL336858 — Ki = 0.22 nM 9.66
CHEMBL130214 — Ki = 0.37 nM 9.43
CHEMBL434226 — Ki = 0.37 nM 9.43
CHEMBL130203 — Ki = 0.41 nM 9.39
CHEMBL131424 — Ki = 0.45 nM 9.35
CHEMBL131575 — Ki = 0.66 nM 9.18
CHEMBL337882 — Ki = 0.79 nM 9.10
CHEMBL336647 — Ki = 0.8 nM 9.10
CHEMBL130876 — Ki = 0.95 nM 9.02
CHEMBL341439 — Ki = 1.06 nM 8.97
CHEMBL130319 — Ki = 1.2 nM 8.92
CHEMBL338425 — Ki = 1.3 nM 8.89
CHEMBL334962 — Ki = 1.32 nM 8.88
CHEMBL336633 — Ki = 1.89 nM 8.72
CHEMBL340745 — Ki = 2.08 nM 8.68
CHEMBL133001 — Ki = 2.65 nM 8.58
CHEMBL131424 — Ki = 2.9 nM 8.54
CHEMBL130214 — Ki = 3.9 nM 8.41
CHEMBL131602 — Ki = 4.24 nM 8.37
CHEMBL336333 — Ki = 4.34 nM 8.36
CHEMBL131431 — Ki = 6.48 nM 8.19
CHEMBL133426 — Ki = 6.41 nM 8.19
CHEMBL337295 — Ki = 6.5 nM 8.19
CHEMBL130286 — Ki = 8.9 nM 8.05
CHEMBL130813 — Ki = 10.0 nM 8.00
CHEMBL131252 — Ki = 0.008 nM -