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Compound Detail

CHEMBL1236167

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O=C1COc2ccc(Cl)cc2CNC(=O)[C@@H]2CCCN2C(=O)[C@@H](C2CCCCC2)NC(=O)CCN1

Basic Information

ChEMBL ID CHEMBL1236167
Phase Preclinical
Structure Type MOL
InChI Key CNGULIMOMYJRBP-WMZHIEFXSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

505.0
MW (Da)
1.91
ALogP
5
HBA
3
HBD
116.8
PSA (Ų)
0.54
QED
1
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H33ClN4O5
MW 505.02
Aromatic Rings 1
Heavy Atoms 35
NP-Likeness 0.05

Activity Summary

Ki 2 meas. best 9.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 9.4 9.145 0.4 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 0.4 nM 9.4 Inhibition of thrombin 21381769
Prothrombin Ki = 1.3 nM 8.89 Inhibition of factor 2a 21035339

Literature References

PubMed DOI Target Context # Activities
21035339 10.1016/j.bmcl.2010.09.141 Prothrombin 1
21381769 10.1021/jm1012374 Prothrombin 1

Data from ChEMBL 36 via Core Engine