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Compound Detail

CHEMBL3808399

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C[C@H]1COC(=O)Nc2cccc(c2)CNC(=O)C(Nc2ccc3c(N)nccc3c2)c2ccc1cc2

Basic Information

ChEMBL ID CHEMBL3808399
Phase Preclinical
Structure Type MOL
InChI Key XQDFKGVDOCCXNS-LFUZPPSTSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

481.6
MW (Da)
4.95
ALogP
6
HBA
4
HBD
118.4
PSA (Ų)
0.32
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 C28H27N5O3
MW 481.56
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness 0.62

Activity Summary

Ki 5 meas. best 7.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Kallikrein-1
CHEMBL2319
Ki 7.6 7.6 25.0 1
Coagulation factor VII/tissue factor
CHEMBL2095194
Ki 6.85 6.85 140.0 1
Coagulation factor X
CHEMBL244
Ki 5.35 5.35 4500.0 1
Prothrombin
CHEMBL204
Ki 5.33 5.33 4700.0 1
Coagulation factor XI
CHEMBL2820
Ki 5.04 5.04 9100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27015008 10.1021/acs.jmedchem.6b00244 Coagulation factor VII/tissue factor 1
27015008 10.1021/acs.jmedchem.6b00244 Coagulation factor X 1
27015008 10.1021/acs.jmedchem.6b00244 Coagulation factor XI 1
27015008 10.1021/acs.jmedchem.6b00244 Prothrombin 1
27015008 10.1021/acs.jmedchem.6b00244 Trypsin 1
27015008 10.1021/acs.jmedchem.6b00244 Kallikrein-1 1

Data from ChEMBL 36 via Core Engine