Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4049189

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

Functional
Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method
ChEMBL ↗
33
Total Activities
18
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.
Durek T, Cromm PM, White AM, Schroeder CI, Kaas Q, Weidmann J, Ahmad Fuaad A, Cheneval O, Harvey PJ, Daly NL, Zhou Y, Dellsén A, Österlund T, Larsson N, Knerr L, Bauer U, Kessler H, Cai M, Hruby VJ, Plowright AT, Craik DJ.
J Med Chem (2018) 61 : 3674 -3684
PubMed 29605997 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 6.38 9.46
Activity 15 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL430239 MELATONAN — 1 9.46
CHEMBL4060381 — — 1 8.78
CHEMBL2070241 BREMELANOTIDE 4.0 1 8.39
CHEMBL4073016 — — 2 6.94
CHEMBL4067967 — — 2 6.61
CHEMBL4101216 — — 2 6.48
CHEMBL4084765 — — 2 5.71
CHEMBL4104465 — — 2 5.61
CHEMBL4098785 — — 2 5.61
CHEMBL4099889 — — 2 5.44
CHEMBL4074479 — — 2 5.13
CHEMBL4063111 — — 2 5.08
CHEMBL4064433 — — 2 5.04
CHEMBL4080223 — — 2 4.97
CHEMBL4074074 — — 2 -
CHEMBL4094606 — — 2 -
CHEMBL4102353 — — 2 -
CHEMBL4089162 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL430239 MELATONAN EC50 = 0.3467 nM 9.46
CHEMBL4060381 — EC50 = 1.66 nM 8.78
CHEMBL2070241 BREMELANOTIDE EC50 = 4.074 nM 8.39
CHEMBL4073016 — EC50 = 114.82 nM 6.94
CHEMBL4067967 — EC50 = 245.47 nM 6.61
CHEMBL4101216 — EC50 = 331.13 nM 6.48
CHEMBL4084765 — EC50 = 1949.84 nM 5.71
CHEMBL4104465 — EC50 = 2454.71 nM 5.61
CHEMBL4098785 — EC50 = 2454.71 nM 5.61
CHEMBL4099889 — EC50 = 3630.78 nM 5.44
CHEMBL4074479 — EC50 = 7413.1 nM 5.13
CHEMBL4063111 — EC50 = 8317.64 nM 5.08
CHEMBL4064433 — EC50 = 9120.11 nM 5.04
CHEMBL4080223 — EC50 = 10715.19 nM 4.97
CHEMBL4104465 — Activity = 100.0 % -
CHEMBL4080223 — Activity = 100.0 % -
CHEMBL4073016 — Activity = 100.0 % -
CHEMBL4099889 — Activity = 100.0 % -
CHEMBL4064433 — Activity = 100.0 % -
CHEMBL4102353 — Activity = 100.0 % -
CHEMBL4094606 — Activity = 100.0 % -
CHEMBL4074074 — Activity = 100.0 % -
CHEMBL4089162 — EC50 > 1000.0 nM -
CHEMBL4084765 — Activity = 100.0 % -
CHEMBL4101216 — Activity = 100.0 % -
CHEMBL4074479 — Activity = 100.0 % -
CHEMBL4067967 — Activity = 100.0 % -
CHEMBL4089162 — Activity = 100.0 % -
CHEMBL4098785 — Activity = 100.0 % -
CHEMBL4074074 — EC50 > 1000.0 nM -
CHEMBL4094606 — EC50 > 100000.0 nM -
CHEMBL4102353 — EC50 > 1000.0 nM -
CHEMBL4063111 — Activity = 100.0 % -