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Compound Detail

CHEMBL19644

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Cc1cnc(NCCc2ccccc2)c(=O)n1CC(=O)NCc1ccc(C(=N)NO)s1

Basic Information

ChEMBL ID CHEMBL19644
Phase Preclinical
Structure Type MOL
InChI Key LWSUAVKYPPCCRD-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
5
Publications
0
Known Names

Molecular Properties

440.5
MW (Da)
1.89
ALogP
8
HBA
5
HBD
132.1
PSA (Ų)
0.20
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 C21H24N6O3S
MW 440.53
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.52

Activity Summary

Ki 1 meas. best 7.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 7.51 7.51 30.8 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 153.33 ng.hr.mL-1 Canis lupus familiaris
Cmax 658.3 nM Canis lupus familiaris
T1/2 0.6333 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 30.8 nM 7.51 In vitro inhibitory constant against human thrombin (FIIa). 11934589

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