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Compound Detail

CHEMBL4740830

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Nc1cc([C@H](CCN(CCF)C23CCC(c4ccccc4)(CC2)CC3)c2ccccc2)c2nn[nH]c2n1

Basic Information

ChEMBL ID CHEMBL4740830
Phase Preclinical
Structure Type MOL
InChI Key VNYMUUQLIGPEDY-URCVZGBWSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

498.6
MW (Da)
5.77
ALogP
5
HBA
2
HBD
83.7
PSA (Ų)
0.31
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H35FN6
MW 498.65
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -0.31

Activity Summary

IC50 1 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Myeloperoxidase
CHEMBL2439
IC50 8.3 8.3 5.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Myeloperoxidase IC50 = 5.0 nM 8.3 Inhibition of recombinant human MPO incubated for 10 mins in presence of 120 mM ... 33007547

Literature References

PubMed DOI Target Context # Activities
33007547 10.1016/j.bmc.2020.115723 ADMET 1
33007547 10.1016/j.bmc.2020.115723 Myeloperoxidase 1

Data from ChEMBL 36 via Core Engine