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Assay Detail

CHEMBL5034973

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Functional
Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
Durek T, Kaas Q, White AM, Weidmann J, Fuaad AA, Cheneval O, Schroeder CI, de Veer SJ, Dellsén A, Österlund T, Larsson N, Knerr L, Bauer U, Plowright AT, Craik DJ.
J Med Chem (2021) 64 : 9906 -9915
PubMed 34197114 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 28 8.01 10.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL430239 MELATONAN 1 10.21
CHEMBL3301624 SETMELANOTIDE 4.0 1 9.82
CHEMBL2070241 BREMELANOTIDE 4.0 1 9.17
CHEMBL5090946 1 8.94
CHEMBL5087859 1 8.91
CHEMBL5083551 1 8.84
CHEMBL5087839 1 8.66
CHEMBL5094168 1 8.45
CHEMBL5080489 1 8.39
CHEMBL5090285 1 8.18
CHEMBL5080784 1 8.18
CHEMBL5077095 1 8.11
CHEMBL5091236 1 7.95
CHEMBL5076315 1 7.87
CHEMBL5087814 1 7.80
CHEMBL5077144 1 7.79
CHEMBL5075712 1 7.76
CHEMBL5092761 1 7.74
CHEMBL5090670 1 7.70
CHEMBL5081077 1 7.62
CHEMBL5094215 1 7.41
CHEMBL5085972 1 7.40
CHEMBL5078687 1 7.25
CHEMBL5075506 1 7.14
CHEMBL5091245 1 7.02
CHEMBL5093939 1 6.89
CHEMBL4099889 1 6.55
CHEMBL5077811 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL430239 MELATONAN EC50 = 0.06166 nM 10.21
CHEMBL3301624 SETMELANOTIDE EC50 = 0.1514 nM 9.82
CHEMBL2070241 BREMELANOTIDE EC50 = 0.6761 nM 9.17
CHEMBL5090946 EC50 = 1.148 nM 8.94
CHEMBL5087859 EC50 = 1.23 nM 8.91
CHEMBL5083551 EC50 = 1.445 nM 8.84
CHEMBL5087839 EC50 = 2.188 nM 8.66
CHEMBL5094168 EC50 = 3.548 nM 8.45
CHEMBL5080489 EC50 = 4.074 nM 8.39
CHEMBL5090285 EC50 = 6.607 nM 8.18
CHEMBL5080784 EC50 = 6.607 nM 8.18
CHEMBL5077095 EC50 = 7.762 nM 8.11
CHEMBL5091236 EC50 = 11.22 nM 7.95
CHEMBL5076315 EC50 = 13.49 nM 7.87
CHEMBL5087814 EC50 = 15.85 nM 7.80
CHEMBL5077144 EC50 = 16.22 nM 7.79
CHEMBL5075712 EC50 = 17.38 nM 7.76
CHEMBL5092761 EC50 = 18.2 nM 7.74
CHEMBL5090670 EC50 = 19.95 nM 7.70
CHEMBL5081077 EC50 = 23.99 nM 7.62
CHEMBL5094215 EC50 = 38.9 nM 7.41
CHEMBL5085972 EC50 = 39.81 nM 7.40
CHEMBL5078687 EC50 = 56.23 nM 7.25
CHEMBL5075506 EC50 = 72.44 nM 7.14
CHEMBL5091245 EC50 = 95.5 nM 7.02
CHEMBL5093939 EC50 = 128.82 nM 6.89
CHEMBL4099889 EC50 = 281.84 nM 6.55
CHEMBL5077811 EC50 = 398.11 nM 6.40