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Compound Detail

CHEMBL544720

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CNC(=O)c1ccc(/C=C/C(=O)NCC(=O)N(C)c2ccc(C)c(COc3cccc4c(-c5ccccc5)cc(C)nc34)c2C)cc1.Cl

Basic Information

ChEMBL ID CHEMBL544720
Phase Preclinical
Structure Type MOL
InChI Key ABPNSOGFLXSOHW-DIRYEVLESA-N
Parent Compound CHEMBL1193332
Active Moiety CHEMBL1193332
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

626.8
MW (Da)
6.56
ALogP
5
HBA
2
HBD
100.6
PSA (Ų)
0.17
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C39H39ClN4O4
MW 663.22
Aromatic Rings 5
Heavy Atoms 47
NP-Likeness -0.90

Activity Summary

IC50 2 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
B2 bradykinin receptor
CHEMBL3157
IC50 9.0 9.0 1.0 1
B2 bradykinin receptor
CHEMBL4111
IC50 8.51 8.51 3.1 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15027853 10.1021/jm030159x B2 bradykinin receptor 2

Data from ChEMBL 36 via Core Engine