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Compound Detail

CHEMBL436851

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CC(C)(C)CC(=O)N[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)c1nc2ccccc2o1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL436851
Phase Preclinical
Structure Type MOL
InChI Key QTDLBZHQZGPXIS-XFDHIDHYSA-N
Parent Compound CHEMBL1185856
Active Moiety CHEMBL1185856
6
Targets
7
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

617.8
MW (Da)
2.91
ALogP
7
HBA
5
HBD
183.5
PSA (Ų)
0.08
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H44F3N7O7
MW 731.77
Aromatic Rings 3
Heavy Atoms 45
NP-Likeness -0.49

Activity Summary

IC50 7 meas. best 8.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine protease 1
CHEMBL209
IC50 8.64 8.64 2.3 1
Trypsin
CHEMBL2095204
IC50 8.64 8.64 2.3 1
Prothrombin
CHEMBL204
IC50 7.17 7.17 68.0 2
Coagulation factor X
CHEMBL244
IC50 6.96 6.96 110.0 1
Unchecked
CHEMBL612545
IC50 6.96 6.96 110.0 1
Plasminogen
CHEMBL3204
IC50 5.88 5.88 1320.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(97)00227-8 Prothrombin 1
- 10.1016/S0960-894X(97)00227-8 Unchecked 1
- 10.1016/S0960-894X(97)00227-8 Serine protease 1 1
- 10.1016/S0960-894X(97)00227-8 Plasminogen 1
18053726 10.1016/j.bmc.2007.11.015 Prothrombin 1
18053726 10.1016/j.bmc.2007.11.015 Coagulation factor X 1
18053726 10.1016/j.bmc.2007.11.015 Trypsin 1

Data from ChEMBL 36 via Core Engine