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Compound Detail

CHEMBL4217366

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CN1CCN(C(=O)c2ccc(-c3cn4c(-c5ccc(C(=O)O)cc5)cnc4cn3)cc2)CC1

Basic Information

ChEMBL ID CHEMBL4217366
Phase Preclinical
Structure Type MOL
InChI Key PZNMULIOTSQSJK-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

441.5
MW (Da)
3.15
ALogP
6
HBA
1
HBD
91.0
PSA (Ų)
0.52
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H23N5O3
MW 441.49
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.09

Activity Summary

IC50 4 meas. best 6.45

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MAP kinase-interacting serine/threonine-protein kinase 2
CHEMBL4204
IC50 6.45 6.445 355.0 2
MAP kinase-interacting serine/threonine-protein kinase 1
CHEMBL4718
IC50 6.16 6.16 700.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29683667 10.1021/acs.jmedchem.7b01714 No relevant target 3
29683667 10.1021/acs.jmedchem.7b01714 MAP kinase-interacting serine/threonine-protein kinase 1/2 1
29683667 10.1021/acs.jmedchem.7b01714 MAP kinase-interacting serine/threonine-protein kinase 2 1
29683667 10.1021/acs.jmedchem.7b01714 MAP kinase-interacting serine/threonine-protein kinase 1 1
37360400 10.1039/d3md00121k MAP kinase-interacting serine/threonine-protein kinase 1 1
37360400 10.1039/d3md00121k MAP kinase-interacting serine/threonine-protein kinase 2 1

Data from ChEMBL 36 via Core Engine