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Assay Detail

CHEMBL832471

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Functional
Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Discovery of a beta-MSH-derived MC-4R selective agonist.
Mayer JP, Hsiung HM, Flora DB, Edwards P, Smith DP, Zhang XY, Gadski RA, Heiman ML, Hertel JL, Emmerson PJ, Husain S, O'brien TP, Kahl SD, Smiley DL, Zhang L, Dimarchi RD, Yan LZ.
J Med Chem (2005) 48 : 3095 -3098
PubMed 15857110 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 9.39 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415661 1 10.22
CHEMBL412495 1 10.00
CHEMBL407809 1 9.92
CHEMBL266879 1 9.80
CHEMBL2373515 1 9.62
CHEMBL408257 1 9.59
CHEMBL264352 1 9.57
CHEMBL267900 1 9.55
CHEMBL385556 1 9.52
CHEMBL415165 1 9.44
CHEMBL264132 1 9.27
CHEMBL414718 1 9.25
CHEMBL412523 1 9.19
CHEMBL428326 1 9.17
CHEMBL412494 1 9.10
CHEMBL427666 1 9.04
CHEMBL412536 1 8.49
CHEMBL410672 1 8.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415661 EC50 = 0.06 nM 10.22
CHEMBL412495 EC50 = 0.1 nM 10.00
CHEMBL407809 EC50 = 0.12 nM 9.92
CHEMBL266879 EC50 = 0.16 nM 9.80
CHEMBL2373515 EC50 = 0.24 nM 9.62
CHEMBL408257 EC50 = 0.26 nM 9.59
CHEMBL264352 EC50 = 0.27 nM 9.57
CHEMBL267900 EC50 = 0.28 nM 9.55
CHEMBL385556 EC50 = 0.3 nM 9.52
CHEMBL415165 EC50 = 0.36 nM 9.44
CHEMBL264132 EC50 = 0.54 nM 9.27
CHEMBL414718 EC50 = 0.56 nM 9.25
CHEMBL412523 EC50 = 0.65 nM 9.19
CHEMBL428326 EC50 = 0.67 nM 9.17
CHEMBL412494 EC50 = 0.79 nM 9.10
CHEMBL427666 EC50 = 0.92 nM 9.04
CHEMBL412536 EC50 = 3.24 nM 8.49
CHEMBL410672 EC50 = 5.24 nM 8.28