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Compound Detail

CHEMBL4218417

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CC(C)OCc1ccc2c(c1)c1c3c(c4c5ccccc5[nH]c4c1n2CCO)CNC3=O

Basic Information

ChEMBL ID CHEMBL4218417
Phase Preclinical
Structure Type MOL
InChI Key OCMCHCVNRKLMAQ-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

427.5
MW (Da)
4.59
ALogP
4
HBA
3
HBD
79.3
PSA (Ų)
0.38
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H25N3O3
MW 427.50
Aromatic Rings 5
Heavy Atoms 32
NP-Likeness 0.06

Activity Summary

IC50 4 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase kinase kinase 11
CHEMBL2708
IC50 8.15 8.15 7.0 1
Mitogen-activated protein kinase kinase kinase 9
CHEMBL2872
IC50 7.89 7.89 13.0 1
Mitogen-activated protein kinase kinase kinase 10
CHEMBL2873
IC50 7.34 7.34 46.0 1
Protein delta homolog 1
CHEMBL5671
IC50 6.92 6.92 119.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29863360 10.1021/acs.jmedchem.8b00370 Mitogen-activated protein kinase kinase kinase 11 1
29863360 10.1021/acs.jmedchem.8b00370 Mitogen-activated protein kinase kinase kinase 10 1
29863360 10.1021/acs.jmedchem.8b00370 Mitogen-activated protein kinase kinase kinase 9 1
29863360 10.1021/acs.jmedchem.8b00370 Protein delta homolog 1 1

Data from ChEMBL 36 via Core Engine