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Assay Detail

CHEMBL711696

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

Functional
Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-4 receptor (rMC4R)
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Melanocortin receptor 4 (CHEMBL2700)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist.
Sebhat IK, Martin WJ, Ye Z, Barakat K, Mosley RT, Johnston DB, Bakshi R, Palucki B, Weinberg DH, MacNeil T, Kalyani RN, Tang R, Stearns RA, Miller RR, Tamvakopoulos C, Strack AM, McGowan E, Cashen DE, Drisko JE, Hom GJ, Howard AD, MacIntyre DE, van der Ploeg LH, Patchett AA, Nargund RP.
J Med Chem (2002) 45 : 4589 -4593
PubMed 12361385 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 8.54 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL339053 1 8.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL339053 EC50 = 2.9 nM 8.54