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Compound Detail

CHEMBL4206349

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CN1CCN(C(=O)c2ccc(-c3cn4c(-c5ccccc5)cnc4cn3)cc2)CC1

Basic Information

ChEMBL ID CHEMBL4206349
Phase Preclinical
Structure Type MOL
InChI Key YXKOPGVYGQVAPR-UHFFFAOYSA-N
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

397.5
MW (Da)
3.45
ALogP
5
HBA
0
HBD
53.7
PSA (Ų)
0.53
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H23N5O
MW 397.48
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.32

Activity Summary

IC50 5 meas. best 5.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MAP kinase-interacting serine/threonine-protein kinase 2
CHEMBL4204
IC50 5.85 5.845 1400.0 2
MAP kinase-interacting serine/threonine-protein kinase 1/2
CHEMBL3883293
IC50 5.72 5.72 1920.0 1
MAP kinase-interacting serine/threonine-protein kinase 1
CHEMBL4718
IC50 5.57 5.57 2680.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
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