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Assay Detail

CHEMBL823355

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

Functional
Effective concentration for its agonist activity against melatonin of Xenopus melanophores
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism frog
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Mapping the melatonin receptor. 6. Melatonin agonists and antagonists derived from 6H-isoindolo[2,1-a]indoles, 5,6-dihydroindolo[2,1-a]isoquinolines, and 6,7-dihydro-5H-benzo[c]azepino[2,1-a]indoles.
Faust R, Garratt PJ, Jones R, Yeh LK, Tsotinis A, Panoussopoulou M, Calogeropoulou T, Teh MT, Sugden D.
J Med Chem (2000) 43 : 1050 -1061
PubMed 10737738 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 7.67 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45 MELATONIN 4.0 1 10.10
CHEMBL9772 1 8.64
CHEMBL10009 1 8.24
CHEMBL9997 1 8.22
CHEMBL10099 1 8.03
CHEMBL274842 1 7.90
CHEMBL274317 1 7.66
CHEMBL9630 1 6.75
CHEMBL9590 1 6.69
CHEMBL274896 1 6.50
CHEMBL273624 1 5.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45 MELATONIN EC50 = 0.08 nM 10.10
CHEMBL9772 EC50 = 2.29 nM 8.64
CHEMBL10009 EC50 = 5.75 nM 8.24
CHEMBL9997 EC50 = 6.03 nM 8.22
CHEMBL10099 EC50 = 9.33 nM 8.03
CHEMBL274842 EC50 = 12.6 nM 7.90
CHEMBL274317 EC50 = 21.9 nM 7.66
CHEMBL9630 EC50 = 178.0 nM 6.75
CHEMBL9590 EC50 = 204.0 nM 6.69
CHEMBL274896 EC50 = 316.0 nM 6.50
CHEMBL273624 EC50 = 2090.0 nM 5.68