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Assay Detail

CHEMBL893556

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Functional
Effect on pigment aggregation in Xenopus laevis melanophores
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Xenopus laevis
Confidence 9 — Direct single protein target
Curated By Expert

Target

Melatonin receptor type 1C (CHEMBL5495)
Type SINGLE PROTEIN
Organism Xenopus laevis

Publication

7-Substituted-melatonin and 7-substituted-1-methylmelatonin analogues: effect of substituents on potency and binding affinity.
Faust R, Garratt PJ, Trujillo Pérez MA, Piccio VJ, Madsen C, Stenstrøm A, Frølund B, Davidson K, Teh MT, Sugden D.
Bioorg Med Chem (2007) 15 : 4543 -4551
PubMed 17459711 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 7.70 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45 MELATONIN 4.0 1 10.10
CHEMBL233728 1 8.48
CHEMBL233308 1 8.46
CHEMBL392421 1 8.01
CHEMBL233729 1 7.94
CHEMBL391350 1 7.90
CHEMBL233516 1 7.80
CHEMBL392422 1 7.78
CHEMBL233309 1 7.61
CHEMBL395221 1 7.50
CHEMBL231872 1 7.34
CHEMBL394408 1 7.34
CHEMBL394406 1 7.28
CHEMBL233310 1 7.19
CHEMBL233311 1 6.92
CHEMBL233517 1 6.81
CHEMBL233740 1 6.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45 MELATONIN EC50 = 0.07943 nM 10.10
CHEMBL233728 EC50 = 3.311 nM 8.48
CHEMBL233308 EC50 = 3.467 nM 8.46
CHEMBL392421 EC50 = 9.772 nM 8.01
CHEMBL233729 EC50 = 11.48 nM 7.94
CHEMBL391350 EC50 = 12.59 nM 7.90
CHEMBL233516 EC50 = 15.85 nM 7.80
CHEMBL392422 EC50 = 16.6 nM 7.78
CHEMBL233309 EC50 = 24.55 nM 7.61
CHEMBL395221 EC50 = 31.62 nM 7.50
CHEMBL231872 EC50 = 45.71 nM 7.34
CHEMBL394408 EC50 = 45.71 nM 7.34
CHEMBL394406 EC50 = 52.48 nM 7.28
CHEMBL233310 EC50 = 64.57 nM 7.19
CHEMBL233311 EC50 = 120.23 nM 6.92
CHEMBL233517 EC50 = 154.88 nM 6.81
CHEMBL233740 EC50 = 338.84 nM 6.47