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Compound Detail

CHEMBL464011

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CC(C)C[C@H](NC(=O)c1cc(-c2ccccc2)n(-c2ccnc3cc(Cl)ccc23)n1)C(=O)O

Basic Information

ChEMBL ID CHEMBL464011
Phase Preclinical
Structure Type MOL
InChI Key PEGYBOFPNDMHLK-NRFANRHFSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

462.9
MW (Da)
4.97
ALogP
5
HBA
2
HBD
97.1
PSA (Ų)
0.40
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 C25H23ClN4O3
MW 462.94
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.01

Activity Summary

EC50 1 meas. best 5.69

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neurotensin receptor type 1
CHEMBL4123
EC50 5.69 5.69 2043.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neurotensin receptor type 1 EC50 = 2043.0 nM 5.69 Agonist activity at NTR1 expressed in CHOK1 cells by calcium mobilization assay 19195889

Literature References

PubMed DOI Target Context # Activities
19195889 10.1016/j.bmcl.2009.01.024 Neurotensin receptor type 1 3

Data from ChEMBL 36 via Core Engine