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Compound Detail

CHEMBL138787

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Cc1cc(C(=O)Nc2ccc(-c3ccccc3S(N)(=O)=O)cc2)n(-c2ccc3onc(N)c3c2)n1

Basic Information

ChEMBL ID CHEMBL138787
Phase Preclinical
Structure Type MOL
InChI Key GMAFNPQQRAPSHH-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
6
Publications
0
Known Names

Molecular Properties

488.5
MW (Da)
3.47
ALogP
8
HBA
3
HBD
159.1
PSA (Ų)
0.34
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H20N6O4S
MW 488.53
Aromatic Rings 5
Heavy Atoms 35
NP-Likeness -1.78

Activity Summary

Ki 1 meas. best 8.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 8.85 8.85 1.4 1

Pharmacokinetic Data

Parameter Value Units Species
CL 5.0 mL.min-1.kg-1 Canis lupus familiaris
F 26.0 % Canis lupus familiaris
T1/2 2.8 hr Canis lupus familiaris
T1/2 3.2 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 1.4 nM 8.85 Inhibitory activity against Coagulation factor X (FXa) 14521405

Literature References

PubMed DOI Target Context # Activities
14521405 10.1021/jm020578e Canis familiaris 4
14521405 10.1021/jm020578e No relevant target 2
14521405 10.1021/jm020578e Coagulation factor X 1
14521405 10.1021/jm020578e Prothrombin 1
14521405 10.1021/jm020578e Trypsin 1
14521405 10.1021/jm020578e ADMET 1

Data from ChEMBL 36 via Core Engine