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Compound Detail

CHEMBL4204137

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Cc1[nH]c2cccnc2c1CC(=O)NCC(=O)Nc1onc(-c2ccccc2)c1C

Basic Information

ChEMBL ID CHEMBL4204137
Phase Preclinical
Structure Type MOL
InChI Key VHGMORCMXIFAJG-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

403.4
MW (Da)
3.13
ALogP
5
HBA
3
HBD
112.9
PSA (Ų)
0.46
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H21N5O3
MW 403.44
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.45

Activity Summary

IC50 2 meas. best 5.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Kallikrein-6
CHEMBL4448
IC50 5.92 5.92 1200.0 1
Trypsin
CHEMBL2095204
IC50 4.3 4.3 50000.0 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

Data from ChEMBL 36 via Core Engine