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Compound Detail

CHEMBL141889

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Cc1cnc(NCC(F)(F)c2ccccn2)c(=O)n1CC(=O)NCc1ncccc1F

Basic Information

ChEMBL ID CHEMBL141889
Phase Preclinical
Structure Type MOL
InChI Key JXHWVKOKYDAROD-UHFFFAOYSA-N
2
Targets
6
Activities
2
Assay Types
12
PK Parameters
13
Publications
0
Known Names

Molecular Properties

432.4
MW (Da)
2.00
ALogP
7
HBA
2
HBD
101.8
PSA (Ų)
0.56
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H19F3N6O2
MW 432.41
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.71

Activity Summary

Ki 4 meas. best 8.38
IC50 2 meas. best 8.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
IC50 8.38 8.38 4.2 1
Prothrombin
CHEMBL204
Ki 8.38 8.38 4.2 2
Trypsin
CHEMBL2095204
IC50 6.6 6.6 252.0 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 5640.0 nM Canis lupus familiaris
Cmax 5640.0 nM Canis lupus familiaris
Cmax 2160.0 nM Rattus norvegicus
Cmax 1100.0 nM Macaca mulatta
F 87.0 % Canis lupus familiaris
F 55.0 % Rattus norvegicus
F 12.0 % Macaca mulatta
T1/2 3.5 hr Canis lupus familiaris
T1/2 3.5 hr Canis lupus familiaris
T1/2 0.57 hr Rattus norvegicus
T1/2 0.99 hr Macaca mulatta
T1/2 3.5 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12570369 10.1021/jm020311f Canis familiaris 4
12570369 10.1021/jm020311f ADMET 3
12570369 10.1021/jm020311f Rattus norvegicus 2
12570369 10.1021/jm020311f Rhesus monkey 2
12570369 10.1021/jm020311f Prothrombin 1
12570369 10.1021/jm020311f Serine protease 1 1
12570369 10.1021/jm020311f NON-PROTEIN TARGET 1
- 10.1039/C2MD20317K Trypsin 1
- 10.1039/C2MD20317K Prothrombin 1
29407959 10.1016/j.ejmech.2018.01.067 Canis familiaris 1
29407959 10.1016/j.ejmech.2018.01.067 Plasma 1
29407959 10.1016/j.ejmech.2018.01.067 Prothrombin 1
29407959 10.1016/j.ejmech.2018.01.067 Trypsin 1

Data from ChEMBL 36 via Core Engine