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Compound Detail

CHEMBL1257882

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O=C1O[C@]2(CC[C@H](CNc3ccc(-c4ccccc4F)nc3)CC2)CN1c1ccccn1

Basic Information

ChEMBL ID CHEMBL1257882
Phase Preclinical
Structure Type MOL
InChI Key GMLAPGTZUBCPCU-YGFACIEFSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
7
Publications
0
Known Names

Molecular Properties

432.5
MW (Da)
5.28
ALogP
5
HBA
1
HBD
67.3
PSA (Ų)
0.59
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H25FN4O2
MW 432.50
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.06

Activity Summary

Ki 1 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuropeptide Y receptor type 5
CHEMBL4561
Ki 8.3 8.3 5.0 1

Pharmacokinetic Data

Parameter Value Units Species
Fu - - Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neuropeptide Y receptor type 5 Ki = 5.012 nM 8.3 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