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Compound Detail

CHEMBL1258340

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O=C1O[C@]2(CC[C@H](CNc3cnn(-c4ccccc4F)c3)CC2)CN1c1cccnc1F

Basic Information

ChEMBL ID CHEMBL1258340
Phase Preclinical
Structure Type MOL
InChI Key OWWQCKUPXVDRLG-QXONSOMPSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
7
Publications
0
Known Names

Molecular Properties

439.5
MW (Da)
4.54
ALogP
6
HBA
1
HBD
72.3
PSA (Ų)
0.59
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H23F2N5O2
MW 439.47
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.03

Activity Summary

Ki 1 meas. best 10.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuropeptide Y receptor type 5
CHEMBL4561
Ki 10.0 10.0 0.1 1

Pharmacokinetic Data

Parameter Value Units Species
Fu 0.019 - Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neuropeptide Y receptor type 5 Ki = 0.1 nM 10.0 Antagonist activity at human NPY Y5 receptor 20813523

Literature References

PubMed DOI Target Context # Activities
20813523 10.1016/j.bmcl.2010.08.041 Neuropeptide Y receptor type 5 1
20813523 10.1016/j.bmcl.2010.08.041 Cytochrome P450 1A2 1
20813523 10.1016/j.bmcl.2010.08.041 Cytochrome P450 2C19 1
20813523 10.1016/j.bmcl.2010.08.041 Cytochrome P450 2C9 1
20813523 10.1016/j.bmcl.2010.08.041 Cytochrome P450 2D6 1
20813523 10.1016/j.bmcl.2010.08.041 Cytochrome P450 3A4 1
20813523 10.1016/j.bmcl.2010.08.041 Brain 1

Data from ChEMBL 36 via Core Engine