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Compound Detail

CHEMBL462830

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COc1ccccc1-c1cc(C(=O)N[C@@H](CC(C)C)C(=O)O)nn1-c1ccnc2cc(Cl)ccc12

Basic Information

ChEMBL ID CHEMBL462830
Phase Preclinical
Structure Type MOL
InChI Key QWNZBGNWUGSPGW-NRFANRHFSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

493.0
MW (Da)
4.98
ALogP
6
HBA
2
HBD
106.3
PSA (Ų)
0.36
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 C26H25ClN4O4
MW 492.96
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.91

Activity Summary

EC50 2 meas. best 6.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neurotensin receptor type 1
CHEMBL4123
EC50 6.66 6.66 220.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19195889 10.1016/j.bmcl.2009.01.024 Neurotensin receptor type 1 3
24997685 10.1016/j.bmcl.2014.06.033 Neurotensin receptor type 1 2

Data from ChEMBL 36 via Core Engine