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Compound Detail

CHEMBL4782307

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CN(CC[C@H](c1ccccc1)c1cc(N)nc2[nH]nnc12)C12CCC(c3ccccc3)(CC1)CC2

Basic Information

ChEMBL ID CHEMBL4782307
Phase Preclinical
Structure Type MOL
InChI Key MIFXHOUDDLZGRL-XPCYEKABSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

466.6
MW (Da)
5.43
ALogP
5
HBA
2
HBD
83.7
PSA (Ų)
0.38
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H34N6
MW 466.63
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.25

Activity Summary

IC50 1 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Myeloperoxidase
CHEMBL2439
IC50 8.22 8.22 6.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Myeloperoxidase IC50 = 6.0 nM 8.22 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
33007547 10.1016/j.bmc.2020.115723 Thyroid peroxidase 1

Data from ChEMBL 36 via Core Engine