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Compound Detail

CHEMBL330572

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N=C(N)c1ccc(O)c(CN2CC[C@H](NS(=O)(=O)c3cc4ncccc4s3)C2=O)c1

Basic Information

ChEMBL ID CHEMBL330572
Phase Preclinical
Structure Type MOL
InChI Key PQJGWYQPOHCEDO-ZDUSSCGKSA-N
7
Targets
8
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

445.5
MW (Da)
1.37
ALogP
7
HBA
4
HBD
149.5
PSA (Ų)
0.33
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C19H19N5O4S2
MW 445.53
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.07

Activity Summary

Ki 8 meas. best 9.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.15 9.15 0.7 2
Tissue-type plasminogen activator
CHEMBL1873
Ki 6.44 6.44 360.0 1
Serine protease 1
CHEMBL209
Ki 6.0 6.0 1000.0 1
Trypsin II
CHEMBL4472
Ki 6.0 6.0 1000.0 1
Plasminogen
CHEMBL1801
Ki 5.64 5.64 2300.0 1
Prothrombin
CHEMBL204
Ki 5.4 5.4 4000.0 1
Vitamin K-dependent protein C
CHEMBL4444
Ki 5.28 5.28 5200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10966741 10.1021/jm000940u Coagulation factor X 1
10966741 10.1021/jm000940u Trypsin II 1
10966741 10.1021/jm000940u Prothrombin 1
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

Data from ChEMBL 36 via Core Engine