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Compound Detail

CHEMBL3359090

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COc1cccc(CNC(=O)c2nc3ccc(F)c(OCCc4ccc(N)cc4)c3c(=O)[nH]2)c1

Basic Information

ChEMBL ID CHEMBL3359090
Phase Preclinical
Structure Type MOL
InChI Key SUSHWPWUZSOLNV-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

462.5
MW (Da)
3.20
ALogP
6
HBA
3
HBD
119.3
PSA (Ų)
0.35
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H23FN4O4
MW 462.48
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.01

Activity Summary

IC50 1 meas. best 10.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Collagenase 3
CHEMBL280
IC50 10.52 10.52 0.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 233.33 mL.min-1.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Collagenase 3 IC50 = 0.03 nM 10.52 Inhibition of human recombinant MMP13 using Cy3-PLGLK(Cy5Q)AR-NH2 as substrate a... 25264600

Literature References

PubMed DOI Target Context # Activities
25264600 10.1021/jm500981k Liver microsome 1
25264600 10.1021/jm500981k Rattus norvegicus 1
25264600 10.1021/jm500981k Collagenase 3 1
34437804 10.1021/acs.jmedchem.1c00441 HEK293 1
34437804 10.1021/acs.jmedchem.1c00441 Plasmodium falciparum 1

Data from ChEMBL 36 via Core Engine