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Compound Detail

CHEMBL4204506

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

Basic Information

ChEMBL ID CHEMBL4204506
Phase Preclinical
Structure Type MOL
InChI Key TWYKNRDHNFNBDF-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

440.5
MW (Da)
2.55
ALogP
6
HBA
1
HBD
96.8
PSA (Ų)
0.53
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 C25H24N6O2
MW 440.51
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.29

Activity Summary

IC50 4 meas. best 6.73

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MAP kinase-interacting serine/threonine-protein kinase 2
CHEMBL4204
IC50 6.73 6.725 187.0 2
MAP kinase-interacting serine/threonine-protein kinase 1
CHEMBL4718
IC50 6.54 6.535 290.0 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