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Assay Detail

CHEMBL718087

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

Functional
Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Melanocortin receptor 4 (CHEMBL259)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Aryl piperazine melanocortin MC4 receptor agonists.
Dyck B, Parker J, Phillips T, Carter L, Murphy B, Summers R, Hermann J, Baker T, Cismowski M, Saunders J, Goodfellow V.
Bioorg Med Chem Lett (2003) 13 : 3793 -3796
PubMed 14552781 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 24 6.33 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL339053 1 8.40
CHEMBL333283 1 7.62
CHEMBL340355 1 7.10
CHEMBL123426 1 6.96
CHEMBL435410 1 6.77
CHEMBL338768 1 6.72
CHEMBL338594 1 6.42
CHEMBL339545 1 6.42
CHEMBL338274 1 6.36
CHEMBL124688 1 6.33
CHEMBL338277 1 6.28
CHEMBL125935 1 6.22
CHEMBL127491 1 6.19
CHEMBL124633 1 6.17
CHEMBL338275 1 6.16
CHEMBL337941 1 6.00
CHEMBL340908 1 6.00
CHEMBL333368 1 5.96
CHEMBL127461 1 5.80
CHEMBL127574 1 5.72
CHEMBL333071 1 5.68
CHEMBL339708 1 5.66
CHEMBL339979 1 5.62
CHEMBL125529 1 5.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL339053 EC50 = 4.0 nM 8.40
CHEMBL333283 EC50 = 24.0 nM 7.62
CHEMBL340355 EC50 = 80.0 nM 7.10
CHEMBL123426 EC50 = 110.0 nM 6.96
CHEMBL435410 EC50 = 170.0 nM 6.77
CHEMBL338768 EC50 = 190.0 nM 6.72
CHEMBL338594 EC50 = 380.0 nM 6.42
CHEMBL339545 EC50 = 380.0 nM 6.42
CHEMBL338274 EC50 = 440.0 nM 6.36
CHEMBL124688 EC50 = 470.0 nM 6.33
CHEMBL338277 EC50 = 520.0 nM 6.28
CHEMBL125935 EC50 = 600.0 nM 6.22
CHEMBL127491 EC50 = 650.0 nM 6.19
CHEMBL124633 EC50 = 680.0 nM 6.17
CHEMBL338275 EC50 = 690.0 nM 6.16
CHEMBL337941 EC50 = 1000.0 nM 6.00
CHEMBL340908 EC50 = 1000.0 nM 6.00
CHEMBL333368 EC50 = 1100.0 nM 5.96
CHEMBL127461 EC50 = 1600.0 nM 5.80
CHEMBL127574 EC50 = 1900.0 nM 5.72
CHEMBL333071 EC50 = 2100.0 nM 5.68
CHEMBL339708 EC50 = 2200.0 nM 5.66
CHEMBL339979 EC50 = 2400.0 nM 5.62
CHEMBL125529 EC50 = 4400.0 nM 5.36