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Assay Detail

CHEMBL4032180

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

ADMET
Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins
15
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Melanocortin receptor 3 (CHEMBL4644)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of MC1R Selective γ-MSH Analogues with Canonical Amino Acids Leads to Potency and Pigmentation.
Zhou Y, Mowlazadeh Haghighi S, Zoi I, Sawyer JR, Hruby VJ, Cai M.
J Med Chem (2017) 60 : 9320 -9329
PubMed 29094944 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 7.44 9.10
Activity 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4093140 1 9.10
CHEMBL503229 1 8.70
CHEMBL4079302 1 8.30
CHEMBL4072387 1 8.17
CHEMBL2370964 1 6.52
CHEMBL4068654 1 6.28
CHEMBL4104092 1 6.28
CHEMBL437050 1 6.16
CHEMBL4103570 1 -
CHEMBL4068475 1 -
CHEMBL4088516 1 -
CHEMBL4060000 1 -
CHEMBL4081900 1 -
CHEMBL4089770 1 -
CHEMBL4090684 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4093140 EC50 = 0.8 nM 9.10
CHEMBL503229 EC50 = 2.0 nM 8.70
CHEMBL4079302 EC50 = 5.0 nM 8.30
CHEMBL4072387 EC50 = 6.7 nM 8.17
CHEMBL2370964 EC50 = 300.0 nM 6.52
CHEMBL4068654 EC50 = 521.0 nM 6.28
CHEMBL4104092 EC50 = 520.0 nM 6.28
CHEMBL437050 EC50 = 700.0 nM 6.16
CHEMBL4103570 Activity = - % -
CHEMBL4068475 Activity = - % -
CHEMBL4088516 EC50 > 1000.0 nM -
CHEMBL4060000 Activity = - % -
CHEMBL4081900 EC50 > 1000.0 nM -
CHEMBL4089770 EC50 > 1000.0 nM -
CHEMBL4090684 EC50 > 1000.0 nM -