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Compound Detail

CHEMBL85757

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N=C(N)c1cccc(CN2CC[C@H](NS(=O)(=O)c3cc4ncccc4s3)C2=O)c1

Basic Information

ChEMBL ID CHEMBL85757
Phase Preclinical
Structure Type MOL
InChI Key OQBGESKCQRRAQW-AWEZNQCLSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

429.5
MW (Da)
1.66
ALogP
6
HBA
3
HBD
129.2
PSA (Ų)
0.41
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H19N5O3S2
MW 429.53
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.52

Activity Summary

Ki 5 meas. best 7.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 7.58 7.58 26.0 1
Coagulation factor X
CHEMBL3656
Ki 7.58 7.58 26.0 1
Serine protease 1
CHEMBL209
Ki 5.54 5.54 2900.0 1
Tissue-type plasminogen activator
CHEMBL1873
Ki 5.06 5.06 8700.0 1
Vitamin K-dependent protein C
CHEMBL4444
Ki 4.92 4.92 12000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10498204 10.1016/s0960-894x(99)00421-7 Unchecked 5
10509929 10.1016/s0960-894x(99)00466-7 Coagulation factor X 1
10509929 10.1016/s0960-894x(99)00466-7 Prothrombin 1
10509929 10.1016/s0960-894x(99)00466-7 Serine protease 1 1
10509929 10.1016/s0960-894x(99)00466-7 Vitamin K-dependent protein C 1
10509929 10.1016/s0960-894x(99)00466-7 Plasminogen 1
10509929 10.1016/s0960-894x(99)00466-7 Tissue-type plasminogen activator 1
10498204 10.1016/s0960-894x(99)00421-7 Coagulation factor X 1

Data from ChEMBL 36 via Core Engine