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Compound Detail

CHEMBL159204

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Cc1nc(C(=O)Nc2ccc(-c3ccccc3S(N)(=O)=O)cc2)c(-c2cccc(C(=N)N)c2)[nH]1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL159204
Phase Preclinical
Structure Type MOL
InChI Key YVONDUZKDQGQEK-UHFFFAOYSA-N
Parent Compound CHEMBL1181217
Active Moiety CHEMBL1181217
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

474.6
MW (Da)
3.24
ALogP
5
HBA
5
HBD
167.8
PSA (Ų)
0.21
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 C26H23F3N6O5S
MW 588.57
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.14

Activity Summary

Ki 2 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 8.22 8.22 6.0 1
Trypsin
CHEMBL2095204
Ki 5.96 5.96 1100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 6.0 nM 8.22 Binding affinity towards human Serine protease FXa 11266160
Trypsin Ki = 1100.0 nM 5.96 Binding affinity towards human trypsin 11266160

Literature References

PubMed DOI Target Context # Activities
11266160 10.1016/s0960-894x(01)00029-4 Coagulation factor X 1
11266160 10.1016/s0960-894x(01)00029-4 Prothrombin 1
11266160 10.1016/s0960-894x(01)00029-4 Trypsin 1

Data from ChEMBL 36 via Core Engine