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Compound Detail

CHEMBL5078139

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COc1ccc(C(Nc2cc(-c3ccc4ccn(C)c4c3)c3nccnc3c2)c2cnnn2C)cn1

Basic Information

ChEMBL ID CHEMBL5078139
Phase Preclinical
Structure Type MOL
InChI Key MZUHOFZPDUAMNB-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
2
PK Parameters
1
Publications
0
Known Names

Molecular Properties

476.5
MW (Da)
4.52
ALogP
9
HBA
1
HBD
95.6
PSA (Ų)
0.38
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H24N8O
MW 476.54
Aromatic Rings 6
Heavy Atoms 36
NP-Likeness -1.24

Activity Summary

IC50 2 meas. best 8.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3
CHEMBL2331053
IC50 8.46 8.03 3.5 2

Pharmacokinetic Data

Parameter Value Units Species
CL 188.0 mL.min-1.g-1 Mus musculus
CL 163.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32679452 10.1016/j.ejmech.2020.112612 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 1

Data from ChEMBL 36 via Core Engine