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Compound Detail

CHEMBL4587472

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CC(C)Oc1cc(-c2cncc(-c3nn[nH]n3)c2)ccc1C(N)=O

Basic Information

ChEMBL ID CHEMBL4587472
Phase Preclinical
Structure Type MOL
InChI Key YXYNMHMVPRQKBT-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

324.3
MW (Da)
1.81
ALogP
6
HBA
2
HBD
119.7
PSA (Ų)
0.74
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H16N6O2
MW 324.34
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.32

Activity Summary

IC50 3 meas. best 7.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MAP kinase-interacting serine/threonine-protein kinase 2
CHEMBL4204
IC50 7.1 7.1 80.0 1
MAP kinase-interacting serine/threonine-protein kinase 1
CHEMBL4718
IC50 6.51 6.51 310.0 1
MAP kinase-interacting serine/threonine-protein kinase 1/2
CHEMBL3883293
IC50 6.24 6.24 570.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31910010 10.1021/acs.jmedchem.9b01582 MAP kinase-interacting serine/threonine-protein kinase 1 1
31910010 10.1021/acs.jmedchem.9b01582 MAP kinase-interacting serine/threonine-protein kinase 2 1
31910010 10.1021/acs.jmedchem.9b01582 MAP kinase-interacting serine/threonine-protein kinase 1/2 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