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Assay Detail

CHEMBL5320170

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

Functional
Agonist activity at human MC5R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Flp-In-293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Melanocortin receptor 5 (CHEMBL4608)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Targeting Melanocortin Receptors Using S<sub><i>N</i></sub>Ar-Type Macrocyclization: A Doubly Orthogonal Route to Cyclic Peptide Conjugates.
Yue WK, Zhang T, Shandre Mugan R, Barlow N, Chalmers DK, Pouton CW, Thompson PE.
J Med Chem (2023) 66 : 3273 -3283
PubMed 36808973 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.05 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL430239 MELATONAN 1 8.20
CHEMBL5414451 1 6.53
CHEMBL5399539 1 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL430239 MELATONAN EC50 = 6.31 nM 8.20
CHEMBL5414451 EC50 = 295.12 nM 6.53
CHEMBL5399539 EC50 = 371.54 nM 6.43