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Compound Detail

CHEMBL4098651

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C[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O

Basic Information

ChEMBL ID CHEMBL4098651
Phase Preclinical
Structure Type MOL
InChI Key NMIKIOBZRLWTII-ASFXGQTKSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

992.1
MW (Da)
-0.23
ALogP
10
HBA
10
HBD
314.4
PSA (Ų)
0.06
QED
2
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C51H65N11O10
MW 992.15
Aromatic Rings 3
Heavy Atoms 72
NP-Likeness 0.54

Activity Summary

EC50 1 meas. best 4.69
Kd 1 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanocortin receptor 4
CHEMBL3719
Kd 7.0 7.0 100.0 1
Melanocyte-stimulating hormone receptor
CHEMBL4077
EC50 4.69 4.69 20500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28813605 10.1021/acs.jmedchem.7b00856 Melanocortin receptor 3 2
28813605 10.1021/acs.jmedchem.7b00856 Melanocortin receptor 4 2
28813605 10.1021/acs.jmedchem.7b00856 Melanocortin receptor 5 1
28813605 10.1021/acs.jmedchem.7b00856 Melanocyte-stimulating hormone receptor 1

Data from ChEMBL 36 via Core Engine