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Compound Detail

CHEMBL212192

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CCC(C)[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1

Basic Information

ChEMBL ID CHEMBL212192
Phase Preclinical
Structure Type MOL
InChI Key PRWVJUJCHUHVLU-KKFPZRRJSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

573.5
MW (Da)
5.46
ALogP
4
HBA
2
HBD
78.7
PSA (Ų)
0.42
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H33Cl2F3N4O2
MW 573.49
Aromatic Rings 2
Heavy Atoms 38
NP-Likeness -1.31

Activity Summary

Ki 1 meas. best 7.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanocortin receptor 4
CHEMBL259
Ki 7.75 7.75 18.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Melanocortin receptor 4 Ki = 18.0 nM 7.75 Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells 16777413

Literature References

PubMed DOI Target Context # Activities
16777413 10.1016/j.bmcl.2006.05.088 Melanocortin receptor 4 1

Data from ChEMBL 36 via Core Engine