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Compound Detail

CHEMBL143879

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Cc1cnc(NCC(F)(F)c2ccccc2)c(=O)n1CC(=O)NCc1ncccc1F

Basic Information

ChEMBL ID CHEMBL143879
Phase Preclinical
Structure Type MOL
InChI Key UPYFICZRANWLAQ-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

431.4
MW (Da)
2.61
ALogP
6
HBA
2
HBD
88.9
PSA (Ų)
0.57
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 C21H20F3N5O2
MW 431.42
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.62

Activity Summary

Ki 2 meas. best 8.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 8.17 8.17 6.8 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 3730.0 nM Canis lupus familiaris
T1/2 2.0 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 6.8 nM 8.17 Inhibitory constant against thrombin (IIa) 12570369

Literature References

PubMed DOI Target Context # Activities
12570369 10.1021/jm020311f Canis familiaris 2
12570369 10.1021/jm020311f Prothrombin 1
12570369 10.1021/jm020311f Serine protease 1 1
12570369 10.1021/jm020311f NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine