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Compound Detail

CHEMBL143418

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Cc1nc(N)ccc1CNC(=O)Cn1c(C)cnc(NCC(F)(F)c2ccccn2)c1=O

Basic Information

ChEMBL ID CHEMBL143418
Phase Preclinical
Structure Type MOL
InChI Key OWCMVQFLPIOYNL-UHFFFAOYSA-N
3
Targets
7
Activities
2
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

443.5
MW (Da)
1.75
ALogP
8
HBA
3
HBD
127.8
PSA (Ų)
0.48
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 C21H23F2N7O2
MW 443.46
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.44

Activity Summary

Ki 5 meas. best 10.38
IC50 2 meas. best 10.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
IC50 10.38 10.38 0.0 1
Prothrombin
CHEMBL204
Ki 10.38 10.38 0.0 3
Serine protease 1
CHEMBL209
Ki 6.1 6.1 800.0 1
Trypsin
CHEMBL2095204
IC50 6.1 6.1 800.0 1
Trypsin
CHEMBL2095204
Ki 6.1 6.1 800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
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 Prothrombin 1
- 10.1039/C2MD20317K Trypsin 1
26200936 10.1021/acs.jmedchem.5b00258 Prothrombin 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