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Compound Detail

CHEMBL279199

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COc1cccc(S(=O)(=O)Nc2cccn(CC(=O)NCc3ccc(C(=N)N)cc3F)c2=O)c1

Basic Information

ChEMBL ID CHEMBL279199
Phase Preclinical
Structure Type MOL
InChI Key QEIZOZWDTCKRDF-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

487.5
MW (Da)
1.40
ALogP
7
HBA
4
HBD
156.4
PSA (Ų)
0.26
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H22FN5O5S
MW 487.51
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.94

Activity Summary

Ki 3 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 8.22 8.22 6.0 1
Serine protease 1
CHEMBL209
Ki 7.5 7.5 31.3 1
Coagulation factor X
CHEMBL244
Ki 6.6 6.6 248.6 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax - ug.mL-1 Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11934589 10.1016/s0960-894x(02)00129-4 Prothrombin 1
11934589 10.1016/s0960-894x(02)00129-4 Coagulation factor X 1
11934589 10.1016/s0960-894x(02)00129-4 Serine protease 1 1
11934589 10.1016/s0960-894x(02)00129-4 No relevant target 1
11934589 10.1016/s0960-894x(02)00129-4 Canis familiaris 1

Data from ChEMBL 36 via Core Engine