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Compound Detail

CHEMBL296737

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CCNC(=O)COc1ccc(Cl)cc1CNC(=O)Cn1c(C)ccc(NS(=O)(=O)Cc2ccccc2)c1=O

Basic Information

ChEMBL ID CHEMBL296737
Phase Preclinical
Structure Type MOL
InChI Key VFOBRZBTHIRLJE-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

561.1
MW (Da)
2.58
ALogP
7
HBA
3
HBD
135.6
PSA (Ų)
0.31
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H29ClN4O6S
MW 561.06
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -2.01

Activity Summary

Ki 3 meas. best 10.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 10.4 10.4 0.0 2
Trypsin
CHEMBL2095204
Ki 5.7 5.7 2000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 0.04 nM 10.4 Inhibition of thrombin in human plasma 12482415
Prothrombin Ki = 0.04 nM 10.4 Inhibition of thrombin 18291642
Trypsin Ki = 2000.0 nM 5.7 Inhibition of trypsin in human plasma 12482415

Literature References

PubMed DOI Target Context # Activities
12482415 10.1016/s0960-894x(02)00946-0 Prothrombin 1
12482415 10.1016/s0960-894x(02)00946-0 Trypsin 1
12482415 10.1016/s0960-894x(02)00946-0 Homo sapiens 1
18291642 10.1016/j.bmcl.2008.01.098 Prothrombin 1

Data from ChEMBL 36 via Core Engine