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Assay Detail

CHEMBL4344906

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Functional
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Melanocortin receptor 5 (CHEMBL4489)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy.
Winget MD, Ericson MD, Freeman KT, Haskell-Luevano C.
ACS Med Chem Lett (2020) 11 : 272 -277
PubMed 32184956 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 7.05 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL214332 INTERMEDINE 2.0 1 9.66
CHEMBL441738 AFAMELANOTIDE 4.0 1 9.52
CHEMBL264190 1 7.96
CHEMBL50056 1 6.66
CHEMBL4590532 1 6.57
CHEMBL4465466 1 6.52
CHEMBL3287060 1 6.40
CHEMBL4574756 1 5.77
CHEMBL320157 1 5.70
CHEMBL4437801 1 5.70
CHEMBL4554278 1 -
CHEMBL4558851 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL214332 INTERMEDINE EC50 = 0.22 nM 9.66
CHEMBL441738 AFAMELANOTIDE EC50 = 0.3 nM 9.52
CHEMBL264190 EC50 = 11.0 nM 7.96
CHEMBL50056 EC50 = 220.0 nM 6.66
CHEMBL4590532 EC50 = 270.0 nM 6.57
CHEMBL4465466 EC50 = 300.0 nM 6.52
CHEMBL3287060 EC50 = 400.0 nM 6.40
CHEMBL4574756 EC50 = 1700.0 nM 5.77
CHEMBL320157 EC50 = 2000.0 nM 5.70
CHEMBL4437801 EC50 = 2000.0 nM 5.70
CHEMBL4554278 EC50 > 100000.0 nM -
CHEMBL4558851 EC50 > 100000.0 nM -