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Compound Detail

CHEMBL46708

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COC(=O)[C@H](Cc1cccc(C(=N)N)c1)[C@@H](C)NC(=O)c1ccc(-c2cccc[n+]2[O-])cc1

Basic Information

ChEMBL ID CHEMBL46708
Phase Preclinical
Structure Type MOL
InChI Key ZFKAPCBYMXUEHN-IIBYNOLFSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

446.5
MW (Da)
2.42
ALogP
5
HBA
3
HBD
132.2
PSA (Ų)
0.16
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H26N4O4
MW 446.51
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.24

Activity Summary

Ki 2 meas. best 9.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.24 9.24 0.6 1
Serine protease 1
CHEMBL209
Ki 7.44 7.44 36.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.58 nM 9.24 Inhibition of Coagulation factor Xa 12039587
Serine protease 1 Ki = 36.0 nM 7.44 In vitro inhibitory potency against Trypsin 12039587

Literature References

PubMed DOI Target Context # Activities
12039587 10.1016/s0960-894x(02)00213-5 Coagulation factor X 1
12039587 10.1016/s0960-894x(02)00213-5 Prothrombin 1
12039587 10.1016/s0960-894x(02)00213-5 Serine protease 1 1

Data from ChEMBL 36 via Core Engine