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Compound Detail

CHEMBL317076

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COc1ccc2ccc(S(=O)(=O)NC(Cc3cc4c(N)nccc4s3)C(=O)N3CCC(C(C)=O)CC3)cc2c1

Basic Information

ChEMBL ID CHEMBL317076
Phase Preclinical
Structure Type MOL
InChI Key GNDOAXCVKPOVTI-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

566.7
MW (Da)
3.76
ALogP
8
HBA
2
HBD
131.7
PSA (Ų)
0.33
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H30N4O5S2
MW 566.71
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.11

Activity Summary

IC50 2 meas. best 5.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
IC50 5.85 5.85 1400.0 1
Serine protease 1
CHEMBL209
IC50 5.7 5.7 2000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin IC50 = 1400.0 nM 5.85 In vitro thrombin inhibition 10522702
Serine protease 1 IC50 = 2000.0 nM 5.7 In vitro trypsin inhibition 10522702

Literature References

PubMed DOI Target Context # Activities
10522702 10.1016/s0960-894x(99)00483-7 Prothrombin 1
10522702 10.1016/s0960-894x(99)00483-7 Serine protease 1 1
10522702 10.1016/s0960-894x(99)00483-7 Caco-2 1

Data from ChEMBL 36 via Core Engine