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Compound Detail

CHEMBL247191

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COc1ccc(-n2nc(C(N)=O)c3c2C(=O)N(C2CCN(c4ccccc4CN(C)C)CC2)CC3)cc1

Basic Information

ChEMBL ID CHEMBL247191
Phase Preclinical
Structure Type MOL
InChI Key QLIJAYGAJCPYAJ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

502.6
MW (Da)
2.71
ALogP
7
HBA
1
HBD
96.9
PSA (Ų)
0.53
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H34N6O3
MW 502.62
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -1.18

Activity Summary

Ki 1 meas. best 9.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.39 9.39 0.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.41 nM 9.39 Inhibition of human factor 10a 17174550

Literature References

PubMed DOI Target Context # Activities
17174550 10.1016/j.bmcl.2006.11.071 Coagulation factor X 1
17174550 10.1016/j.bmcl.2006.11.071 Plasma 1

Data from ChEMBL 36 via Core Engine