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Compound Detail

CHEMBL238707

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N=C(N)c1ccc(C(NC(=O)OCc2ccccc2)P(=O)(Oc2ccccc2)Oc2ccccc2)cc1

Basic Information

ChEMBL ID CHEMBL238707
Phase Preclinical
Structure Type MOL
InChI Key WYCVSPRVSFUVMA-UHFFFAOYSA-N
7
Targets
8
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

515.5
MW (Da)
6.25
ALogP
6
HBA
3
HBD
123.7
PSA (Ų)
0.13
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H26N3O5P
MW 515.51
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -0.21

Activity Summary

IC50 8 meas. best 7.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Kallikrein-4
CHEMBL4446
IC50 7.39 7.39 41.0 1
Prothrombin
CHEMBL204
IC50 6.71 6.625 196.0 2
Kallikrein-8
CHEMBL4812
IC50 6.1 6.1 790.0 1
Plasminogen
CHEMBL1801
IC50 5.44 5.44 3600.0 1
Coagulation factor X
CHEMBL244
IC50 5.22 5.22 6000.0 1
Urokinase-type plasminogen activator
CHEMBL3286
IC50 4.22 4.22 60000.0 1
Tissue-type plasminogen activator
CHEMBL1873
IC50 4.18 4.18 66000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C5MD00288E Prothrombin 2
30571121 10.1021/acs.jmedchem.8b01466 ATP-dependent Clp protease proteolytic subunit 2
8295209 10.1021/jm00028a004 Prothrombin 2
- 10.1039/C5MD00288E Kallikrein-4 2
18052026 10.1021/jm700962j Urokinase-type plasminogen activator 2
- 10.1039/C5MD00288E Kallikrein-8 2
18052026 10.1021/jm700962j Unchecked 1
- 10.1039/C5MD00288E Urokinase-type plasminogen activator 1
- 10.1039/C5MD00288E Kallikrein-2 1
- 10.1039/C5MD00288E Kallikrein-1 1
18052026 10.1021/jm700962j Coagulation factor X 1
18052026 10.1021/jm700962j Prothrombin 1
18052026 10.1021/jm700962j Plasminogen 1
9632362 10.1021/jm970543s Granzyme A 1
18052026 10.1021/jm700962j Tissue-type plasminogen activator 1
8295209 10.1021/jm00028a004 Serine protease 1 1
8295209 10.1021/jm00028a004 Plasma kallikrein 1
8295209 10.1021/jm00028a004 Coagulation factor XII 1
9632362 10.1021/jm970543s Serine protease 1 1
9632362 10.1021/jm970543s Tryptase 1

Data from ChEMBL 36 via Core Engine