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Compound Detail

CHEMBL544622

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Cc1ccc2cccc(OCc3c(C(=O)N(C)C)ccc(N(C)C(=O)CNC(=O)/C=C/c4ccc(C(=O)N(C)C)cc4)c3C(=O)N(C)C)c2n1.Cl

Basic Information

ChEMBL ID CHEMBL544622
Phase Preclinical
Structure Type MOL
InChI Key XMXCXVKFPCCIJJ-NEMIEIFKSA-N
Parent Compound CHEMBL1193249
Active Moiety CHEMBL1193249
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

678.8
MW (Da)
4.02
ALogP
7
HBA
1
HBD
132.5
PSA (Ų)
0.24
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C38H43ClN6O6
MW 715.25
Aromatic Rings 4
Heavy Atoms 50
NP-Likeness -1.02

Activity Summary

IC50 2 meas. best 8.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
B2 bradykinin receptor
CHEMBL4111
IC50 8.89 8.89 1.3 1
B2 bradykinin receptor
CHEMBL3157
IC50 8.41 8.41 3.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9804698 10.1021/jm980330i B2 bradykinin receptor 2
9804698 10.1021/jm980330i Cavia porcellus 1

Data from ChEMBL 36 via Core Engine