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Compound Detail

CHEMBL383076

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O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2nn(CCN3CC[C@H](O)C3)cc2c1

Basic Information

ChEMBL ID CHEMBL383076
Phase Preclinical
Structure Type MOL
InChI Key FKEHSKGAWARCKO-QFIPXVFZSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

457.5
MW (Da)
4.54
ALogP
6
HBA
3
HBD
91.7
PSA (Ų)
0.38
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H27N5O3
MW 457.53
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.28

Activity Summary

IC50 2 meas. best 7.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanin-concentrating hormone receptor 1
CHEMBL344
IC50 7.24 7.24 57.0 1
IMR-32
CHEMBL614585
IC50 6.67 6.67 214.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1020.0 ng.hr.mL-1 Mus musculus
AUC - ug.hr/g Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16570930 10.1021/jm0512286 Rattus norvegicus 2
16570930 10.1021/jm0512286 Mus musculus 2
16570930 10.1021/jm0512286 IMR-32 1
16570930 10.1021/jm0512286 Melanin-concentrating hormone receptor 1 1

Data from ChEMBL 36 via Core Engine