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Compound Detail

CHEMBL139063

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COC(=O)CC1(C(=O)Nc2ccc(-c3ccccc3S(N)(=O)=O)cc2)CC(c2cccc(C(=N)N)c2)=NO1

Basic Information

ChEMBL ID CHEMBL139063
Phase Preclinical
Structure Type MOL
InChI Key QMEXGOMLMAXBEB-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

535.6
MW (Da)
2.35
ALogP
8
HBA
4
HBD
187.0
PSA (Ų)
0.19
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 C26H25N5O6S
MW 535.58
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -0.70

Activity Summary

Ki 2 meas. best 8.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 8.2 8.2 6.3 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 6.3 nM 8.2 Binding affinity against human coagulation factor X 11087565
Coagulation factor X Ki = 6.3 nM 8.2 Inhibition of factor 10a 20503967

Literature References

PubMed DOI Target Context # Activities
11087565 10.1021/jm000113t Coagulation factor X 1
20503967 10.1021/jm100146h Coagulation factor X 1

Data from ChEMBL 36 via Core Engine