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Compound Detail

CHEMBL2018865

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O=C(CC1c2ccccc2CCN1S(=O)(=O)c1ccc(Cl)c(Cl)c1)N1CCC(Cc2ccc(C3=NCCN3)cc2)CC1

Basic Information

ChEMBL ID CHEMBL2018865
Phase Preclinical
Structure Type MOL
InChI Key LJVFUNKIIQVDNX-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

625.6
MW (Da)
5.50
ALogP
5
HBA
1
HBD
82.1
PSA (Ų)
0.38
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H34Cl2N4O3S
MW 625.62
Aromatic Rings 3
Heavy Atoms 42
NP-Likeness -1.10

Activity Summary

Ki 1 meas. best 8.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
B1 bradykinin receptor
CHEMBL4308
Ki 8.42 8.42 3.8 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
B1 bradykinin receptor Ki = 3.8 nM 8.42 Binding affinity to human bradykinin B1 receptor 22483585

Literature References

PubMed DOI Target Context # Activities
22483585 10.1016/j.bmcl.2012.03.065 Liver microsomes 2
22483585 10.1016/j.bmcl.2012.03.065 B1 bradykinin receptor 1

Data from ChEMBL 36 via Core Engine