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Compound Detail

CHEMBL185232

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N=C(N)c1cccc(-n2nc(Cn3ccnn3)cc2C(=O)Nc2ccc(-n3cnc4ccccc43)cc2)c1

Basic Information

ChEMBL ID CHEMBL185232
Phase Preclinical
Structure Type MOL
InChI Key LQFYPYCYEHAMOM-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

502.5
MW (Da)
3.39
ALogP
9
HBA
3
HBD
145.3
PSA (Ų)
0.23
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 C27H22N10O
MW 502.54
Aromatic Rings 6
Heavy Atoms 38
NP-Likeness -1.88

Activity Summary

Ki 2 meas. best 9.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.59 9.59 0.3 1
Coagulation factor IX
CHEMBL2016
Ki 7.7 7.7 20.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.26 nM 9.59 Binding affinity towards human factor Xa 15454208
Coagulation factor IX Ki = 20.0 nM 7.7 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