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Compound Detail

CHEMBL396432

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CCN(CC)CCN[C@@H](CC(C)C)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1

Basic Information

ChEMBL ID CHEMBL396432
Phase Preclinical
Structure Type MOL
InChI Key QIYPSKLPQCIXMB-XDFJSJKPSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

648.7
MW (Da)
6.03
ALogP
5
HBA
1
HBD
59.1
PSA (Ų)
0.27
QED
2
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H48Cl2FN5O2
MW 648.70
Aromatic Rings 2
Heavy Atoms 44
NP-Likeness -1.35

Activity Summary

IC50 1 meas. best 4.43
Ki 1 meas. best 7.25

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanocortin receptor 4
CHEMBL259
Ki 7.25 7.25 56.0 1
Cytochrome P450 3A4
CHEMBL340
IC50 4.43 4.43 37000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Melanocortin receptor 4 Ki = 56.0 nM 7.25 Binding affinity at human MC4R 17822895
Cytochrome P450 3A4 IC50 = 37000.0 nM 4.43 Inhibition of microsomal CYP3A4 17822895

Literature References

PubMed DOI Target Context # Activities
17822895 10.1016/j.bmcl.2007.07.097 Melanocortin receptor 4 1
17822895 10.1016/j.bmcl.2007.07.097 Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine