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Compound Detail

CHEMBL182597

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CC(C)N1CCC(NC(=O)c2cc3ccccc3n2CC(=O)Nc2ccc(Cl)cn2)CC1

Basic Information

ChEMBL ID CHEMBL182597
Phase Preclinical
Structure Type MOL
InChI Key ILRJJEMRKWAJMZ-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

454.0
MW (Da)
3.93
ALogP
5
HBA
2
HBD
79.3
PSA (Ų)
0.59
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H28ClN5O2
MW 453.97
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -2.12

Activity Summary

Ki 2 meas. best 9.0
IC50 1 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.0 9.0 1.0 2
Prothrombin
CHEMBL204
IC50 7.7 7.7 20.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15261268 10.1016/j.bmcl.2004.06.020 Prothrombin 3
15261268 10.1016/j.bmcl.2004.06.020 Coagulation factor X 1
15261268 10.1016/j.bmcl.2004.06.020 Serine protease 1 1
15261268 10.1016/j.bmcl.2004.06.020 Kallikrein-1 1
15261268 10.1016/j.bmcl.2004.06.020 Tissue-type plasminogen activator 1
15261268 10.1016/j.bmcl.2004.06.020 Tissue factor 1
15261268 10.1016/j.bmcl.2004.06.020 ADMET 1
20503967 10.1021/jm100146h Coagulation factor X 1

Data from ChEMBL 36 via Core Engine