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Compound Detail

CHEMBL345731

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COc1ccc(-n2nc(C)cc2C(=O)Nc2ccc(-c3ccccc3S(N)(=O)=O)cc2)c(CN)c1

Basic Information

ChEMBL ID CHEMBL345731
Phase Preclinical
Structure Type MOL
InChI Key KQFAYMXIXLIVEC-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

491.6
MW (Da)
3.21
ALogP
7
HBA
3
HBD
142.3
PSA (Ų)
0.36
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H25N5O4S
MW 491.57
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.42

Activity Summary

Ki 1 meas. best 8.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 8.42 8.42 3.8 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 3.8 nM 8.42 Tested in vitro for inhibition of human Coagulation factor X 14640539

Literature References

PubMed DOI Target Context # Activities
14640539 10.1021/jm030212h Coagulation factor X 2
14640539 10.1021/jm030212h NON-PROTEIN TARGET 2
14640539 10.1021/jm030212h Prothrombin 1
14640539 10.1021/jm030212h Serine protease 1 1
14640539 10.1021/jm030212h Oryctolagus cuniculus 1

Data from ChEMBL 36 via Core Engine