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Compound Detail

CHEMBL154238

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CS(=O)(=O)c1ccccc1-c1ccc(NC(=O)c2cc(C(F)(F)F)nn2-c2cccc(C(=N)N)c2)cc1

Basic Information

ChEMBL ID CHEMBL154238
Phase Preclinical
Structure Type MOL
InChI Key HTIXLULNBZFLJX-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

527.5
MW (Da)
4.50
ALogP
6
HBA
3
HBD
130.9
PSA (Ų)
0.25
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H20F3N5O3S
MW 527.53
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -1.58

Activity Summary

Ki 3 meas. best 8.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypsin
CHEMBL2095204
Ki 8.37 8.37 4.3 1
Prothrombin
CHEMBL204
Ki 7.16 7.16 70.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypsin Ki = 4.3 nM 8.37 In vitro activity against human trypsin. 11170646
Prothrombin Ki = 70.0 nM 7.16 In vitro activity against human thrombin. 11170646

Literature References

PubMed DOI Target Context # Activities
11170646 10.1021/jm000409z Coagulation factor X 1
11170646 10.1021/jm000409z Prothrombin 1
11170646 10.1021/jm000409z Trypsin 1

Data from ChEMBL 36 via Core Engine