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Assay Detail

CHEMBL712574

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

Binding
Binding affinity for melatonin receptor type 1B, 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 1B (CHEMBL1946) ↗
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 9.29 10.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL130214 — — 3 10.47
CHEMBL131424 — — 3 10.17
CHEMBL131252 — — 1 10.16
CHEMBL130542 — — 1 10.07
CHEMBL337882 — — 1 10.03
CHEMBL132802 — — 1 10.03
CHEMBL340832 — — 1 10.00
CHEMBL130490 — — 1 9.92
CHEMBL129889 — — 1 9.89
CHEMBL336509 — — 1 9.84
CHEMBL336054 — — 1 9.81
CHEMBL338425 — — 1 9.74
CHEMBL129890 — — 1 9.72
CHEMBL133001 — — 1 9.66
CHEMBL130319 — — 1 9.66
CHEMBL336858 — — 1 9.62
CHEMBL133416 — — 1 9.59
CHEMBL334962 — — 1 9.51
CHEMBL434226 — — 1 9.47
CHEMBL132340 — — 1 9.41
CHEMBL336647 — — 1 9.39
CHEMBL10878 AGOMELATINE 4.0 1 9.35
CHEMBL131602 — — 1 9.29
CHEMBL45 MELATONIN 4.0 1 9.28
CHEMBL337024 — — 1 9.26
CHEMBL130898 — — 1 9.26
CHEMBL341439 — — 1 9.24
CHEMBL130203 — — 1 9.23
CHEMBL130876 — — 1 9.10
CHEMBL131575 — — 1 8.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL130214 — Ki = 0.034 nM 10.47
CHEMBL131424 — Ki = 0.068 nM 10.17
CHEMBL131252 — Ki = 0.069 nM 10.16
CHEMBL130542 — Ki = 0.085 nM 10.07
CHEMBL132802 — Ki = 0.094 nM 10.03
CHEMBL337882 — Ki = 0.093 nM 10.03
CHEMBL340832 — Ki = 0.1 nM 10.00
CHEMBL131424 — Ki = 0.11 nM 9.96
CHEMBL130490 — Ki = 0.12 nM 9.92
CHEMBL129889 — Ki = 0.13 nM 9.89
CHEMBL336509 — Ki = 0.145 nM 9.84
CHEMBL336054 — Ki = 0.153 nM 9.81
CHEMBL338425 — Ki = 0.18 nM 9.74
CHEMBL129890 — Ki = 0.19 nM 9.72
CHEMBL130319 — Ki = 0.22 nM 9.66
CHEMBL133001 — Ki = 0.22 nM 9.66
CHEMBL336858 — Ki = 0.24 nM 9.62
CHEMBL133416 — Ki = 0.26 nM 9.59
CHEMBL334962 — Ki = 0.31 nM 9.51
CHEMBL434226 — Ki = 0.34 nM 9.47
CHEMBL130214 — Ki = 0.35 nM 9.46
CHEMBL132340 — Ki = 0.39 nM 9.41
CHEMBL336647 — Ki = 0.41 nM 9.39
CHEMBL10878 AGOMELATINE Ki = 0.45 nM 9.35
CHEMBL131602 — Ki = 0.51 nM 9.29
CHEMBL45 MELATONIN Ki = 0.53 nM 9.28
CHEMBL337024 — Ki = 0.55 nM 9.26
CHEMBL130898 — Ki = 0.55 nM 9.26
CHEMBL341439 — Ki = 0.57 nM 9.24
CHEMBL130203 — Ki = 0.59 nM 9.23
CHEMBL130876 — Ki = 0.79 nM 9.10
CHEMBL131575 — Ki = 1.59 nM 8.80
CHEMBL336333 — Ki = 1.86 nM 8.73
CHEMBL133426 — Ki = 1.86 nM 8.73
CHEMBL337295 — Ki = 3.83 nM 8.42
CHEMBL340745 — Ki = 4.03 nM 8.39
CHEMBL131424 — Ki = 4.07 nM 8.39
CHEMBL130214 — Ki = 7.4 nM 8.13
CHEMBL130286 — Ki = 11.8 nM 7.93
CHEMBL336633 — Ki = 13.2 nM 7.88
CHEMBL131431 — Ki = 16.2 nM 7.79
CHEMBL130813 — Ki = 41.8 nM 7.38