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Compound Detail

CHEMBL4208878

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NCc1ccc(NC(=O)c2c([O-])ccc[n+]2Cc2nccn2Cc2ccccc2)cc1

Basic Information

ChEMBL ID CHEMBL4208878
Phase Preclinical
Structure Type MOL
InChI Key DMRCMJXUFJLJKH-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

413.5
MW (Da)
2.05
ALogP
5
HBA
2
HBD
99.9
PSA (Ų)
0.45
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H23N5O2
MW 413.48
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -1.11

Activity Summary

IC50 2 meas. best 6.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypsin
CHEMBL2095204
IC50 6.75 6.75 180.0 1
Kallikrein-6
CHEMBL4448
IC50 6.05 6.05 890.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30212625 10.1021/acs.jmedchem.8b01106 Kallikrein-6 1
30212625 10.1021/acs.jmedchem.8b01106 Trypsin 1
30212625 10.1021/acs.jmedchem.8b01106 Prothrombin 1
30212625 10.1021/acs.jmedchem.8b01106 Coagulation factor X 1

Data from ChEMBL 36 via Core Engine