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Compound Detail

CHEMBL113502

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CCNC(=O)NCC(=O)N(C)c1ccc(OC)c(COc2cccc3ccc(C)nc23)c1C#N

Basic Information

ChEMBL ID CHEMBL113502
Phase Preclinical
Structure Type MOL
InChI Key GSMWKYQZPCPTFR-UHFFFAOYSA-N
1
Targets
3
Activities
3
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

461.5
MW (Da)
3.28
ALogP
6
HBA
2
HBD
116.6
PSA (Ų)
0.53
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 C25H27N5O4
MW 461.52
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.60

Activity Summary

EC50 1 meas. best 6.35
IC50 1 meas. best 7.27
Ki 1 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
B2 bradykinin receptor
CHEMBL4111
Ki 8.22 8.22 6.0 1
B2 bradykinin receptor
CHEMBL4111
IC50 7.27 7.27 53.8 1
B2 bradykinin receptor
CHEMBL4111
EC50 6.35 6.35 450.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10091678 10.1016/s0960-894x(98)00736-7 B2 bradykinin receptor 4

Data from ChEMBL 36 via Core Engine