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Compound Detail

CHEMBL44249

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Cc1nc(N)ccc1CNC(=O)Cn1c(C)cc(C(F)(F)F)c(N)c1=O

Basic Information

ChEMBL ID CHEMBL44249
Phase Preclinical
Structure Type MOL
InChI Key TWTMIGUXBOJVCY-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

369.4
MW (Da)
1.36
ALogP
6
HBA
3
HBD
116.0
PSA (Ų)
0.75
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H18F3N5O2
MW 369.35
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -1.34

Activity Summary

Ki 2 meas. best 6.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 6.47 6.47 340.0 1
Trypsin
CHEMBL2095204
Ki 4.7 4.7 20000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 340.0 nM 6.47 Inhibition of thrombin in human plasma 12482415
Trypsin Ki = 20000.0 nM 4.7 Inhibition of trypsin in human plasma 12482415

Literature References

PubMed DOI Target Context # Activities
12482415 10.1016/s0960-894x(02)00946-0 Prothrombin 1
12482415 10.1016/s0960-894x(02)00946-0 Trypsin 1

Data from ChEMBL 36 via Core Engine