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Compound Detail

CHEMBL195914

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O=c1n(-c2ccc(Oc3ccccc3)cc2)ccn1-c1ccc2c(cnn2CCN2CCCC2)c1

Basic Information

ChEMBL ID CHEMBL195914
Phase Preclinical
Structure Type MOL
InChI Key KJCQYSICJWKIHX-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
4
PK Parameters
3
Publications
0
Known Names

Molecular Properties

465.6
MW (Da)
4.87
ALogP
7
HBA
0
HBD
57.2
PSA (Ų)
0.34
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 C28H27N5O2
MW 465.56
Aromatic Rings 5
Heavy Atoms 35
NP-Likeness -1.42

Activity Summary

IC50 2 meas. best 8.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanin-concentrating hormone receptor 1
CHEMBL4730
IC50 8.23 8.23 5.9 1
Melanin-concentrating hormone receptor
CHEMBL2111437
IC50 6.18 6.18 654.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1350.0 ng.hr.mL-1 Mus musculus
AUC 1.71 ug hr-1 g-1 Mus musculus
Cmax 1166.34 nM Mus musculus
Cmax 183.0 ng g-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15911251 10.1016/j.bmcl.2005.03.114 ADMET 4
15911251 10.1016/j.bmcl.2005.03.114 Melanin-concentrating hormone receptor 1 1
15911251 10.1016/j.bmcl.2005.03.114 Melanin-concentrating hormone receptor 1

Data from ChEMBL 36 via Core Engine