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Assay Detail

CHEMBL718859

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

Functional
Maximal agonist response at rat melanocortin 3 receptor (MC3R)
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Melanocortin receptor 3 (CHEMBL4023)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

De novo design, synthesis, and pharmacology of alpha-melanocyte stimulating hormone analogues derived from somatostatin by a hybrid approach.
Han G, Haskell-Luevano C, Kendall L, Bonner G, Hadley ME, Cone RD, Hruby VJ.
J Med Chem (2004) 47 : 1514 -1526
PubMed 14998337 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 8.13 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL441738 AFAMELANOTIDE 4.0 1 10.00
CHEMBL414965 1 9.64
CHEMBL405087 1 9.64
CHEMBL410404 1 8.52
CHEMBL405791 1 8.28
CHEMBL406842 1 8.14
CHEMBL411378 1 7.51
CHEMBL2372365 1 7.23
CHEMBL411400 1 7.19
CHEMBL406891 1 7.12
CHEMBL415200 1 6.18
CHEMBL427814 1 -
CHEMBL407845 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL441738 AFAMELANOTIDE EC50 = 0.1 nM 10.00
CHEMBL414965 EC50 = 0.23 nM 9.64
CHEMBL405087 EC50 = 0.23 nM 9.64
CHEMBL410404 EC50 = 3.0 nM 8.52
CHEMBL405791 EC50 = 5.2 nM 8.28
CHEMBL406842 EC50 = 7.3 nM 8.14
CHEMBL411378 EC50 = 31.0 nM 7.51
CHEMBL2372365 EC50 = 59.0 nM 7.23
CHEMBL411400 EC50 = 64.0 nM 7.19
CHEMBL406891 EC50 = 75.0 nM 7.12
CHEMBL415200 EC50 = 660.0 nM 6.18
CHEMBL427814 EC50 = - nM -
CHEMBL407845 EC50 = 3e-06 nM -