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Compound Detail

CHEMBL4469308

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COc1ccc(NC(=O)c2nc3c(s2)CN(C)CC3)c(C(=O)Nc2ccc(C)cn2)c1

Basic Information

ChEMBL ID CHEMBL4469308
Phase Preclinical
Structure Type MOL
InChI Key OOSFXPQKGFCWRC-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

437.5
MW (Da)
3.35
ALogP
7
HBA
2
HBD
96.5
PSA (Ų)
0.64
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23N5O3S
MW 437.53
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.82

Activity Summary

IC50 5 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 8.0 8.0 10.0 1
Coagulation factor VII
CHEMBL3991
IC50 7.96 7.96 11.0 1
Prothrombin
CHEMBL204
IC50 7.5 7.5 32.0 1
Coagulation factor IX
CHEMBL2016
IC50 7.38 7.38 42.0 1
Trypsin
CHEMBL2095204
IC50 7.27 7.27 54.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30446438 10.1016/j.bmc.2018.09.012 Unchecked 4
30446438 10.1016/j.bmc.2018.09.012 Plasma 2
30446438 10.1016/j.bmc.2018.09.012 Coagulation factor VII 1
30446438 10.1016/j.bmc.2018.09.012 Coagulation factor IX 1
30446438 10.1016/j.bmc.2018.09.012 Trypsin 1
30446438 10.1016/j.bmc.2018.09.012 Coagulation factor X 1
30446438 10.1016/j.bmc.2018.09.012 Prothrombin 1

Data from ChEMBL 36 via Core Engine