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Compound Detail

CHEMBL428749

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CS(=O)(=O)c1ccccc1N1CCC(NC(=O)c2cc(C(F)(F)F)nn2-c2ccc3onc(N)c3c2)CC1

Basic Information

ChEMBL ID CHEMBL428749
Phase Preclinical
Structure Type MOL
InChI Key HADDJWUKDPCVQU-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
5
Publications
0
Known Names

Molecular Properties

548.5
MW (Da)
3.42
ALogP
9
HBA
2
HBD
136.3
PSA (Ų)
0.39
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H23F3N6O4S
MW 548.55
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.75

Activity Summary

Ki 1 meas. best 8.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 8.77 8.77 1.7 1

Pharmacokinetic Data

Parameter Value Units Species
CL 0.051 ml/min.mg Homo sapiens
CL 18.33 mL.min-1.kg-1 Canis lupus familiaris
F 24.0 % Canis lupus familiaris
T1/2 1.3 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 1.7 nM 8.77 Inhibition of human factor 10a 17174550

Literature References

PubMed DOI Target Context # Activities
17174550 10.1016/j.bmcl.2006.11.071 Canis familiaris 4
17174550 10.1016/j.bmcl.2006.11.071 Coagulation factor X 1
17174550 10.1016/j.bmcl.2006.11.071 Plasma 1
17174550 10.1016/j.bmcl.2006.11.071 Caco-2 1
17174550 10.1016/j.bmcl.2006.11.071 Liver microsomes 1

Data from ChEMBL 36 via Core Engine