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Assay Detail

CHEMBL714910

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

Binding
Binding affinity is evaluated for chicken brain melatonin receptor using 2-[125I]iodomelatonin as radioligand
ChEMBL ↗
46
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Melatonin receptor (CHEMBL2095154) ↗
Type PROTEIN FAMILY
Organism Gallus gallus

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 46 8.63 10.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL336054 — — 1 10.96
CHEMBL131252 — — 1 10.70
CHEMBL340832 — — 3 10.47
CHEMBL132802 — — 1 10.40
CHEMBL336509 — — 1 10.27
CHEMBL133416 — — 1 9.89
CHEMBL129890 — — 1 9.85
CHEMBL130214 — — 3 9.82
CHEMBL131424 — — 3 9.44
CHEMBL131077 — — 1 9.37
CHEMBL10878 AGOMELATINE 4.0 1 9.28
CHEMBL45 MELATONIN 4.0 1 9.15
CHEMBL129889 — — 1 9.15
CHEMBL337024 — — 1 9.10
CHEMBL336647 — — 1 9.05
CHEMBL130542 — — 1 9.05
CHEMBL434226 — — 1 8.62
CHEMBL130203 — — 1 8.57
CHEMBL130490 — — 1 8.53
CHEMBL338425 — — 1 8.49
CHEMBL130898 — — 1 8.44
CHEMBL334962 — — 1 8.42
CHEMBL337882 — — 1 8.37
CHEMBL130876 — — 1 8.34
CHEMBL336858 — — 1 8.32
CHEMBL130319 — — 1 8.26
CHEMBL131575 — — 1 7.95
CHEMBL133001 — — 1 7.84
CHEMBL132340 — — 1 7.61
CHEMBL129934 — — 1 7.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL336054 — Ki = 0.011 nM 10.96
CHEMBL131252 — Ki = 0.02 nM 10.70
CHEMBL340832 — Ki = 0.034 nM 10.47
CHEMBL132802 — Ki = 0.04 nM 10.40
CHEMBL336509 — Ki = 0.054 nM 10.27
CHEMBL340832 — Ki = 0.07 nM 10.15
CHEMBL133416 — Ki = 0.13 nM 9.89
CHEMBL129890 — Ki = 0.14 nM 9.85
CHEMBL130214 — Ki = 0.15 nM 9.82
CHEMBL130214 — Ki = 0.16 nM 9.80
CHEMBL340832 — Ki = 0.31 nM 9.51
CHEMBL131424 — Ki = 0.36 nM 9.44
CHEMBL131077 — Ki = 0.43 nM 9.37
CHEMBL10878 AGOMELATINE Ki = 0.53 nM 9.28
CHEMBL129889 — Ki = 0.7 nM 9.15
CHEMBL45 MELATONIN Ki = 0.7 nM 9.15
CHEMBL337024 — Ki = 0.8 nM 9.10
CHEMBL131424 — Ki = 0.8 nM 9.10
CHEMBL130542 — Ki = 0.9 nM 9.05
CHEMBL336647 — Ki = 0.9 nM 9.05
CHEMBL434226 — Ki = 2.4 nM 8.62
CHEMBL130203 — Ki = 2.7 nM 8.57
CHEMBL130490 — Ki = 2.95 nM 8.53
CHEMBL338425 — Ki = 3.2 nM 8.49
CHEMBL130898 — Ki = 3.6 nM 8.44
CHEMBL334962 — Ki = 3.8 nM 8.42
CHEMBL130214 — Ki = 4.3 nM 8.37
CHEMBL337882 — Ki = 4.3 nM 8.37
CHEMBL130876 — Ki = 4.6 nM 8.34
CHEMBL336858 — Ki = 4.75 nM 8.32
CHEMBL130319 — Ki = 5.5 nM 8.26
CHEMBL131575 — Ki = 11.2 nM 7.95
CHEMBL133001 — Ki = 14.3 nM 7.84
CHEMBL131424 — Ki = 21.7 nM 7.66
CHEMBL132340 — Ki = 24.4 nM 7.61
CHEMBL129934 — Ki = 28.1 nM 7.55
CHEMBL340745 — Ki = 31.7 nM 7.50
CHEMBL131602 — Ki = 36.1 nM 7.44
CHEMBL341439 — Ki = 40.5 nM 7.39
CHEMBL336633 — Ki = 43.4 nM 7.36
CHEMBL133426 — Ki = 73.7 nM 7.13
CHEMBL130813 — Ki = 97.1 nM 7.01
CHEMBL336333 — Ki = 101.8 nM 6.99
CHEMBL337295 — Ki = 123.3 nM 6.91
CHEMBL130286 — Ki = 145.0 nM 6.84
CHEMBL131431 — Ki = 399.0 nM 6.40