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Compound Detail

CHEMBL426071

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N=C(N)c1cccc(-n2nc(Cn3ccnc3)cc2C(=O)Nc2ccc(-n3cnc4ccccc43)cc2)c1

Basic Information

ChEMBL ID CHEMBL426071
Phase Preclinical
Structure Type MOL
InChI Key DGDYVKYCUQMCEL-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

501.6
MW (Da)
3.99
ALogP
8
HBA
3
HBD
132.4
PSA (Ų)
0.22
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H23N9O
MW 501.55
Aromatic Rings 6
Heavy Atoms 38
NP-Likeness -1.76

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
Coagulation factor IX
CHEMBL2016
Ki 6.92 6.92 120.0 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 Binding affinity towards human factor Xa 15454208
Coagulation factor IX Ki = 120.0 nM 6.92 Binding affinity towards human factor IXa 15454208

Literature References

PubMed DOI Target Context # Activities
15454208 10.1016/j.bmcl.2004.08.034 Coagulation factor IX 1
15454208 10.1016/j.bmcl.2004.08.034 Coagulation factor X 1
15454208 10.1016/j.bmcl.2004.08.034 Coagulation factor IX and X 1

Data from ChEMBL 36 via Core Engine