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Compound Detail

CHEMBL1771260

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CCOc1cc(Cl)c(-c2c(C)nn3c(NCCNC4CCOCC4)cc(C)nc23)c(Cl)c1

Basic Information

ChEMBL ID CHEMBL1771260
Phase Preclinical
Structure Type MOL
InChI Key KXVKWNPVAHBIOP-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
3
PK Parameters
2
Publications
0
Known Names

Molecular Properties

478.4
MW (Da)
4.90
ALogP
7
HBA
2
HBD
72.7
PSA (Ų)
0.45
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H29Cl2N5O2
MW 478.42
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.32

Activity Summary

IC50 1 meas. best 7.82
Ki 1 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuropeptide Y receptor type 1
CHEMBL4777
Ki 8.52 8.52 3.0 1
Neuropeptide Y receptor type 1
CHEMBL4777
IC50 7.82 7.82 15.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 28.0 mL.min-1.kg-1 Rattus norvegicus
CL 996.0 mL.min-1.kg-1 Rattus norvegicus
Fu 0.029 - Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21295475 10.1016/j.bmcl.2010.12.116 Rattus norvegicus 4
21295475 10.1016/j.bmcl.2010.12.116 Neuropeptide Y receptor type 1 2

Data from ChEMBL 36 via Core Engine