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Compound Detail

CHEMBL244640

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COc1ccc(OC)c(S(=O)(=O)N2CCC(N(Cc3ccc4ccc(C(=N)N)cc4c3)C(=O)CC(=O)O)CC2)c1

Basic Information

ChEMBL ID CHEMBL244640
Phase Preclinical
Structure Type MOL
InChI Key HSPYEJCVHDDLAJ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

568.6
MW (Da)
2.80
ALogP
7
HBA
3
HBD
163.3
PSA (Ų)
0.19
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H32N4O7S
MW 568.65
Aromatic Rings 3
Heavy Atoms 40
NP-Likeness -1.14

Activity Summary

IC50 2 meas. best 8.09

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 8.09 8.09 8.1 1
Trypsin
CHEMBL2095204
IC50 5.43 5.43 3700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 8.1 nM 8.09 Inhibition of human factor 10a 17416533
Trypsin IC50 = 3700.0 nM 5.43 Inhibition of human trypsin 17416533

Literature References

PubMed DOI Target Context # Activities
17416533 10.1016/j.bmc.2007.03.066 Unchecked 2
17416533 10.1016/j.bmc.2007.03.066 Plasma 2
17416533 10.1016/j.bmc.2007.03.066 Coagulation factor X 1
17416533 10.1016/j.bmc.2007.03.066 Prothrombin 1
17416533 10.1016/j.bmc.2007.03.066 Trypsin 1

Data from ChEMBL 36 via Core Engine