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Compound Detail

CHEMBL447391

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N=C(N)c1ccc(C(=O)Nc2ccccc2C(=O)Nc2ccc(Cl)cn2)cc1

Basic Information

ChEMBL ID CHEMBL447391
Phase Preclinical
Structure Type MOL
InChI Key UYGNDEAYDITYQP-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

393.8
MW (Da)
3.52
ALogP
4
HBA
4
HBD
121.0
PSA (Ų)
0.39
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H16ClN5O2
MW 393.83
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.50

Activity Summary

IC50 2 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 8.4 8.4 4.0 1
Unchecked
CHEMBL612545
IC50 5.31 5.31 4900.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 5.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 4.0 nM 8.4 Inhibition of Factor 10a 19297158
Unchecked IC50 = 4900.0 nM 5.31 Inhibition of kallikrein 19297158

Literature References

PubMed DOI Target Context # Activities
19297158 10.1016/j.bmcl.2009.02.114 Unchecked 3
19297158 10.1016/j.bmcl.2009.02.114 Coagulation factor X 1
19297158 10.1016/j.bmcl.2009.02.114 Rattus norvegicus 1
19297158 10.1016/j.bmcl.2009.02.114 Prothrombin 1
19297158 10.1016/j.bmcl.2009.02.114 Tissue-type plasminogen activator 1
19297158 10.1016/j.bmcl.2009.02.114 Plasminogen 1

Data from ChEMBL 36 via Core Engine