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Compound Detail

CHEMBL4859971

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COc1cc(Nc2ncnc3ccc(-c4ccc(C(=O)N5CCNCC5)cc4)nc23)ccc1F

Basic Information

ChEMBL ID CHEMBL4859971
Phase Preclinical
Structure Type MOL
InChI Key NPZBGSCEEAHWNK-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

458.5
MW (Da)
3.63
ALogP
7
HBA
2
HBD
92.3
PSA (Ų)
0.47
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 C25H23FN6O2
MW 458.50
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.63

Activity Summary

IC50 2 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MAP kinase-interacting serine/threonine-protein kinase 1
CHEMBL4718
IC50 9.0 9.0 1.0 1
MAP kinase-interacting serine/threonine-protein kinase 2
CHEMBL4204
IC50 7.6 7.6 25.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34515481 10.1021/acs.jmedchem.1c01084 MAP kinase-interacting serine/threonine-protein kinase 1 2
34515481 10.1021/acs.jmedchem.1c01084 MAP kinase-interacting serine/threonine-protein kinase 2 1
34515481 10.1021/acs.jmedchem.1c01084 MOLM-13 1

Data from ChEMBL 36 via Core Engine