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Compound Detail

CHEMBL2018864

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O=C(CC1c2ccccc2CCN1S(=O)(=O)c1ccc(Cl)c(Cl)c1)Nc1ccc(N2CCC(N3CCCCC3)CC2)cc1

Basic Information

ChEMBL ID CHEMBL2018864
Phase Preclinical
Structure Type MOL
InChI Key UZWLXQMCFATWND-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

641.7
MW (Da)
6.77
ALogP
5
HBA
1
HBD
73.0
PSA (Ų)
0.31
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 C33H38Cl2N4O3S
MW 641.67
Aromatic Rings 3
Heavy Atoms 43
NP-Likeness -1.56

Activity Summary

Ki 1 meas. best 6.86

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
B1 bradykinin receptor
CHEMBL4308
Ki 6.86 6.86 138.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
B1 bradykinin receptor Ki = 138.0 nM 6.86 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