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Compound Detail

CHEMBL328184

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COc1cc2ccc(S(=O)(=O)NC(Cc3cc4c(N)nccc4s3)C(=O)N3CCC(C)CC3)cc2cc1OC

Basic Information

ChEMBL ID CHEMBL328184
Phase Preclinical
Structure Type MOL
InChI Key HTQPFCPNXGXUIQ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

568.7
MW (Da)
4.20
ALogP
8
HBA
2
HBD
123.8
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 C28H32N4O5S2
MW 568.72
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.10

Activity Summary

IC50 2 meas. best 5.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine protease 1
CHEMBL209
IC50 5.4 5.4 4000.0 1
Prothrombin
CHEMBL204
IC50 5.3 5.3 5000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine protease 1 IC50 = 4000.0 nM 5.4 In vitro trypsin inhibition 10522702
Prothrombin IC50 = 5000.0 nM 5.3 In vitro thrombin 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