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Compound Detail

CHEMBL609990

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O=C([O-])C1O[C@@H](O[C@H]2C(O)C(NS(=O)(=O)[O-])[C@@H](O)O[C@H]2COS(=O)(=O)[O-])C(NS(=O)(=O)[O-])[C@@H](O)[C@@H]1O[C@@H]1OC(COS(=O)(=O)[O-])[C@@H](O[C@@H]2O[C@@H](C(=O)[O-])[C@@H](O[C@H]3O[C@@H](COS(=O)(=O)[O-])[C@@H](O)C(O)C3NS(=O)(=O)[O-])C(O)C2O)[C@H](OS(=O)(=O)[O-])C1OS(=O)(=O)[O-].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+]

Basic Information

ChEMBL ID CHEMBL609990
Phase Preclinical
Structure Type MOL
InChI Key HAAHXNKPCLVQID-AOILHKNMSA-D
Parent Compound CHEMBL2069149
Active Moiety CHEMBL2069149
2
Targets
2
Activities
2
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

1494.2
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H41N3Na10O49S8
MW 1714.07

Activity Summary

IC50 1 meas. best 6.89
Kd 1 meas. best 7.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Antithrombin-III
CHEMBL1950
Kd 7.24 7.24 58.0 1
Prothrombin
CHEMBL204
IC50 6.89 6.89 130.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.7 hr -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Antithrombin-III Kd = 58.0 nM 7.24 Dissociation constant for Antithrombin-III 9171870
Prothrombin IC50 = 130.0 nM 6.89 Inhibition of Thrombin generation was determined 9171870

Literature References

PubMed DOI Target Context # Activities
10560738 10.1016/s0960-894x(99)00550-8 Homo sapiens 4
9171870 10.1021/jm960726z Antithrombin-III 1
9171870 10.1021/jm960726z Coagulation factor X 1
9171870 10.1021/jm960726z Prothrombin 1
9171870 10.1021/jm960726z Rattus norvegicus 1
9171870 10.1021/jm960726z ADMET 1

Data from ChEMBL 36 via Core Engine