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Compound Detail

CHEMBL352099

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COCc1onc(-c2cccc(C(=N)N)c2)c1C(=O)Nc1ccc(-c2ccccc2S(N)(=O)=O)cc1

Basic Information

ChEMBL ID CHEMBL352099
Phase Preclinical
Structure Type MOL
InChI Key GLMPXCWPQNWBLX-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

505.6
MW (Da)
3.34
ALogP
7
HBA
4
HBD
174.4
PSA (Ų)
0.21
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H23N5O5S
MW 505.56
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.19

Activity Summary

Ki 3 meas. best 9.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.2 9.2 0.6 1
Serine protease 1
CHEMBL3769
Ki 7.12 7.12 76.0 1
Prothrombin
CHEMBL204
Ki 5.42 5.42 3800.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 28.33 mL.min-1.kg-1 Canis lupus familiaris
T1/2 1.2 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10782664 10.1016/s0960-894x(00)00097-4 Canis familiaris 3
10782664 10.1016/s0960-894x(00)00097-4 Coagulation factor X 1
10782664 10.1016/s0960-894x(00)00097-4 Prothrombin 1
10782664 10.1016/s0960-894x(00)00097-4 Serine protease 1 1

Data from ChEMBL 36 via Core Engine