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Compound Detail

CHEMBL360620

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Nc1ccc2cccc(O[C@H]3CCN(Cc4ccc5c(c4)OCO5)C3)c2n1

Basic Information

ChEMBL ID CHEMBL360620
Phase Preclinical
Structure Type MOL
InChI Key YGVPVRLYSXAJMW-INIZCTEOSA-N
1
Targets
2
Activities
1
Assay Types
6
PK Parameters
2
Publications
0
Known Names

Molecular Properties

363.4
MW (Da)
3.20
ALogP
6
HBA
1
HBD
69.8
PSA (Ų)
0.77
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H21N3O3
MW 363.42
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.60

Activity Summary

IC50 2 meas. best 7.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Melanin-concentrating hormone receptor 1
CHEMBL344
IC50 7.52 7.34 30.0 2

Pharmacokinetic Data

Parameter Value Units Species
AUC 1711.0 ng.hr.mL-1 Mus musculus
AUC 1350.0 ng.hr.mL-1 Mus musculus
Cmax 1494.14 nM Mus musculus
Cmax 503.55 nM Mus musculus
T1/2 6.5 hr Mus musculus
T1/2 8.3 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15341944 10.1016/j.bmcl.2004.07.035 ADMET 6
15341944 10.1016/j.bmcl.2004.07.035 Melanin-concentrating hormone receptor 1 2

Data from ChEMBL 36 via Core Engine