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Assay Detail

CHEMBL4731047

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Functional
Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Melanocortin receptor 4 (CHEMBL3719)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Peptoid NPhe in AGRP-Based c[Pro-Arg-Phe-Phe-Xxx-Ala-Phe-DPro] Scaffolds Maintain Mouse MC4R Antagonist Potency.
Ericson MD,Freeman KT,Haskell-Luevano C
ACS Med Chem Lett (2020) 11 : 1942 -1948
PubMed 33062177 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 13 7.85 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4747952 1 9.00
CHEMBL4102048 1 8.60
CHEMBL4747778 1 8.40
CHEMBL4740561 1 8.40
CHEMBL3577981 1 8.20
CHEMBL4764556 1 7.50
CHEMBL4753150 1 6.60
CHEMBL4743564 1 6.10
CHEMBL4785711 1 -
CHEMBL4797774 1 -
CHEMBL4754305 1 -
CHEMBL4785157 1 -
CHEMBL4762178 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4747952 Kd = 1.0 nM 9.00
CHEMBL4102048 Kd = 2.512 nM 8.60
CHEMBL4747778 Kd = 3.981 nM 8.40
CHEMBL4740561 Kd = 3.981 nM 8.40
CHEMBL3577981 Kd = 6.31 nM 8.20
CHEMBL4764556 Kd = 31.62 nM 7.50
CHEMBL4753150 Kd = 251.19 nM 6.60
CHEMBL4743564 Kd = 794.33 nM 6.10
CHEMBL4785711 Kd > 3162.28 nM -
CHEMBL4797774 Kd > 3162.28 nM -
CHEMBL4754305 Kd > 3162.28 nM -
CHEMBL4785157 Kd > 3162.28 nM -
CHEMBL4762178 Kd > 3162.28 nM -