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Compound Detail

CHEMBL358835

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CS(=O)(=O)c1ccccc1-c1ccc(NC(=O)c2cc(C(F)(F)F)nn2-c2cccc(C(=N)N)c2)c(F)c1

Basic Information

ChEMBL ID CHEMBL358835
Phase Preclinical
Structure Type MOL
InChI Key ZLJCFXPKCSWCGG-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
3
PK Parameters
6
Publications
0
Known Names

Molecular Properties

545.5
MW (Da)
4.64
ALogP
6
HBA
3
HBD
130.9
PSA (Ų)
0.18
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 C25H19F4N5O3S
MW 545.52
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.73

Activity Summary

Ki 2 meas. best 8.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypsin
CHEMBL2095204
Ki 8.47 8.47 3.4 1
Prothrombin
CHEMBL204
Ki 7.3 7.3 50.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 18.33 mL.min-1.kg-1 Canis lupus familiaris
F - % Canis lupus familiaris
T1/2 3.8 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypsin Ki = 3.4 nM 8.47 In vitro activity against human trypsin. 11170646
Prothrombin Ki = 50.0 nM 7.3 In vitro activity against human thrombin. 11170646

Literature References

PubMed DOI Target Context # Activities
11170646 10.1021/jm000409z Canis familiaris 3
11170646 10.1021/jm000409z Coagulation factor X 1
11170646 10.1021/jm000409z Prothrombin 1
11170646 10.1021/jm000409z Trypsin 1
11170646 10.1021/jm000409z ADMET 1
11170646 10.1021/jm000409z Homo sapiens 1

Data from ChEMBL 36 via Core Engine