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Compound Detail

CHEMBL27008

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CC(C)(C)CC(=O)N[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)c1nc2ccccc2[nH]1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL27008
Phase Preclinical
Structure Type MOL
InChI Key WXCATCHPXHGZTJ-IZTVGRIKSA-N
Parent Compound CHEMBL1178409
Active Moiety CHEMBL1178409
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

616.8
MW (Da)
2.44
ALogP
6
HBA
5
HBD
188.7
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 C35H45F3N8O6
MW 730.79
Aromatic Rings 3
Heavy Atoms 45
NP-Likeness -0.33

Activity Summary

IC50 2 meas. best 7.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
IC50 7.04 7.04 92.1 1
Serine protease 1
CHEMBL209
IC50 6.0 6.0 1010.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin IC50 = 92.1 nM 7.04 Inhibitory concentration against thrombin(FIIa). -
Serine protease 1 IC50 = 1010.0 nM 6.0 Inhibitory concentration against trypsin. -

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

Data from ChEMBL 36 via Core Engine