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Compound Detail

CHEMBL19453

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COc1cccc(S(=O)(=O)Nc2cccn(CC(=O)NCc3ccc(C(=N)N)cc3)c2=O)c1

Basic Information

ChEMBL ID CHEMBL19453
Phase Preclinical
Structure Type MOL
InChI Key IPTHFGHOMKEWQH-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
3
PK Parameters
5
Publications
0
Known Names

Molecular Properties

469.5
MW (Da)
1.26
ALogP
7
HBA
4
HBD
156.4
PSA (Ų)
0.27
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23N5O5S
MW 469.52
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.63

Activity Summary

Ki 3 meas. best 8.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 8.28 8.28 5.3 1
Serine protease 1
CHEMBL209
Ki 7.73 7.73 18.7 1
Coagulation factor X
CHEMBL244
Ki 6.82 6.82 152.7 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 165.0 ng.hr.mL-1 Canis lupus familiaris
Cmax 298.18 nM Canis lupus familiaris
T1/2 0.8833 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11934589 10.1016/s0960-894x(02)00129-4 Canis familiaris 3
11934589 10.1016/s0960-894x(02)00129-4 Prothrombin 1
11934589 10.1016/s0960-894x(02)00129-4 Coagulation factor X 1
11934589 10.1016/s0960-894x(02)00129-4 Serine protease 1 1
11934589 10.1016/s0960-894x(02)00129-4 No relevant target 1

Data from ChEMBL 36 via Core Engine