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Compound Detail

CHEMBL393979

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COC(=O)NC(Cc1ccc(NC(=N)N)cc1)P(=O)(Oc1ccc(NC(C)=O)cc1)Oc1ccc(NC(C)=O)cc1

Basic Information

ChEMBL ID CHEMBL393979
Phase Preclinical
Structure Type MOL
InChI Key VYDDQNBUEWMIFT-UHFFFAOYSA-N
11
Targets
11
Activities
1
Assay Types
4
PK Parameters
11
Publications
0
Known Names

Molecular Properties

582.5
MW (Da)
4.48
ALogP
8
HBA
6
HBD
194.0
PSA (Ų)
0.11
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H31N6O7P
MW 582.55
Aromatic Rings 3
Heavy Atoms 41
NP-Likeness -0.30

Activity Summary

IC50 11 meas. best 8.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Urokinase-type plasminogen activator
CHEMBL3286
IC50 8.47 8.47 3.4 1
Urokinase-type plasminogen activator
CHEMBL1075311
IC50 8.1 8.1 8.0 1
Urokinase-type plasminogen activator
CHEMBL1075245
IC50 7.61 7.61 24.5 1
Prothrombin
CHEMBL204
IC50 5.95 5.95 1130.0 1
Plasminogen
CHEMBL3204
IC50 5.66 5.66 2200.0 1
Plasminogen
CHEMBL1801
IC50 5.55 5.55 2800.0 1
Prothrombin
CHEMBL1075308
IC50 5.35 5.35 4500.0 1
Plasminogen
CHEMBL1075299
IC50 5.32 5.32 4800.0 1
Tissue-type plasminogen activator
CHEMBL1873
IC50 5.21 5.21 6100.0 1
Coagulation factor X
CHEMBL244
IC50 4.52 4.52 30000.0 1
Prothrombin
CHEMBL3078
IC50 4.35 4.35 45000.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 35.0 hr -
T1/2 336.0 hr -
T1/2 64.0 hr -
T1/2 3.0 hr -

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18052026 10.1021/jm700962j Rattus norvegicus 14
18052026 10.1021/jm700962j NON-PROTEIN TARGET 10
18052026 10.1021/jm700962j No relevant target 5
18052026 10.1021/jm700962j Urokinase-type plasminogen activator 4
18052026 10.1021/jm700962j Unchecked 4
18052026 10.1021/jm700962j Plasminogen 3
18052026 10.1021/jm700962j Prothrombin 3
18052026 10.1021/jm700962j Tissue-type plasminogen activator 1
18052026 10.1021/jm700962j Coagulation factor X 1
18052026 10.1021/jm700962j ADMET 1
18052026 10.1021/jm700962j Plasma 1

Data from ChEMBL 36 via Core Engine