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Compound Detail

CHEMBL3799955

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CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O

Basic Information

ChEMBL ID CHEMBL3799955
Phase Preclinical
Structure Type MOL
InChI Key KJUUQMJYKGOSKZ-VAMAGGONSA-N
5
Targets
9
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

1949.2
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C94H133N25O21
MW 1949.25

Activity Summary

EC50 6 meas. best 8.92
IC50 3 meas. best 7.27

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanocortin receptor 4
CHEMBL259
EC50 8.92 7.735 1.2 2
Melanocortin receptor 5
CHEMBL4489
EC50 8.4 8.4 4.0 1
Melanocortin receptor 4
CHEMBL3719
EC50 8.14 8.14 7.3 1
Melanocyte-stimulating hormone receptor
CHEMBL4077
EC50 7.9 7.9 12.6 1
Melanocortin receptor 3
CHEMBL4774
EC50 7.64 7.64 22.7 1
Melanocortin receptor 4
CHEMBL3719
IC50 7.27 7.27 54.0 1
Melanocyte-stimulating hormone receptor
CHEMBL4077
IC50 6.88 6.88 131.0 1
Melanocortin receptor 3
CHEMBL4774
IC50 4.99 4.99 10200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26959173 10.1021/acs.jmedchem.5b01894 Melanocyte-stimulating hormone receptor 4
26959173 10.1021/acs.jmedchem.5b01894 Melanocortin receptor 3 4
26959173 10.1021/acs.jmedchem.5b01894 Melanocortin receptor 4 4
26959173 10.1021/acs.jmedchem.5b01894 Melanocortin receptor 5 2
29669202 10.1021/acs.jmedchem.8b00238 Melanocortin receptor 4 2

Data from ChEMBL 36 via Core Engine