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Compound Detail

CHEMBL355992

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COc1ccc(-n2nc(C(F)(F)F)cc2C(=O)Nc2ccc(-c3ccccc3S(N)(=O)=O)cn2)cc1

Basic Information

ChEMBL ID CHEMBL355992
Phase Preclinical
Structure Type MOL
InChI Key BOIBFXPIYNHDKE-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
6
Publications
0
Known Names

Molecular Properties

517.5
MW (Da)
3.86
ALogP
7
HBA
2
HBD
129.2
PSA (Ų)
0.40
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 C23H18F3N5O4S
MW 517.49
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.65

Activity Summary

Ki 1 meas. best 8.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 8.55 8.55 2.8 1

Pharmacokinetic Data

Parameter Value Units Species
CL 2.0 mL.min-1.kg-1 Canis lupus familiaris
Cmax 730.0 nM Canis lupus familiaris
F - % -
T1/2 6.0 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 2.8 nM 8.55 Tested in vitro for inhibition of human Coagulation factor X 14640539

Literature References

PubMed DOI Target Context # Activities
14640539 10.1021/jm030212h Canis familiaris 5
14640539 10.1021/jm030212h Coagulation factor X 1
14640539 10.1021/jm030212h Prothrombin 1
14640539 10.1021/jm030212h Serine protease 1 1
14640539 10.1021/jm030212h NON-PROTEIN TARGET 1
14640539 10.1021/jm030212h ADMET 1

Data from ChEMBL 36 via Core Engine