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Compound Detail

CHEMBL3594305

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Nc1nccc2cc(N[C@H]3C(=O)NCc4cccc(c4)NC(=O)CCCc4ccc3cc4)ccc12

Basic Information

ChEMBL ID CHEMBL3594305
Phase Preclinical
Structure Type MOL
InChI Key LXFPTSIBSQOGTO-AREMUKBSSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

465.6
MW (Da)
4.56
ALogP
5
HBA
4
HBD
109.1
PSA (Ų)
0.35
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H27N5O2
MW 465.56
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness 0.63

Activity Summary

Ki 4 meas. best 7.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Kallikrein-1
CHEMBL2319
Ki 7.75 7.75 18.0 1
Coagulation factor VII/tissue factor
CHEMBL2095194
Ki 6.4 6.4 400.0 2
Vitamin K-dependent protein C
CHEMBL4444
Ki 5.55 5.55 2800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26151189 10.1021/acs.jmedchem.5b00788 Plasma 1
26151189 10.1021/acs.jmedchem.5b00788 Kallikrein-1 1
26151189 10.1021/acs.jmedchem.5b00788 Plasma kallikrein 1
26151189 10.1021/acs.jmedchem.5b00788 Trypsin 1
26151189 10.1021/acs.jmedchem.5b00788 Vitamin K-dependent protein C 1
26151189 10.1021/acs.jmedchem.5b00788 Prothrombin 1
26151189 10.1021/acs.jmedchem.5b00788 Coagulation factor X 1
26151189 10.1021/acs.jmedchem.5b00788 Coagulation factor IX 1
26151189 10.1021/acs.jmedchem.5b00788 Coagulation factor VII/tissue factor 1
27015008 10.1021/acs.jmedchem.6b00244 Coagulation factor VII/tissue factor 1

Data from ChEMBL 36 via Core Engine