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Compound Detail

CHEMBL3393605

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Cc1ccc(NC(=O)c2ccc(NC(=O)/C=C/CN(C)C)cc2)cc1Nc1nccc(-c2cccnc2)n1

Basic Information

ChEMBL ID CHEMBL3393605
Phase Preclinical
Structure Type MOL
InChI Key YFRXAAWSVLQGDR-FNORWQNLSA-N
3
Targets
6
Activities
1
Assay Types
0
PK Parameters
15
Publications
0
Known Names

Molecular Properties

507.6
MW (Da)
4.90
ALogP
7
HBA
3
HBD
112.1
PSA (Ų)
0.28
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H29N7O2
MW 507.60
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.46

Activity Summary

IC50 6 meas. best 5.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 9
CHEMBL4179
IC50 5.37 5.37 4230.0 2
Mitogen-activated protein kinase 8
CHEMBL2276
IC50 5.11 5.11 7780.0 2
Mitogen-activated protein kinase 10
CHEMBL2637
IC50 5.11 5.11 7750.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25415535 10.1021/jm501212r Mitogen-activated protein kinase 10 1
25415535 10.1021/jm501212r Mitogen-activated protein kinase 8 1
25415535 10.1021/jm501212r Mitogen-activated protein kinase 9 1
35200035 10.1021/acs.jmedchem.1c01947 Mitogen-activated protein kinase 8 1
35200035 10.1021/acs.jmedchem.1c01947 Mitogen-activated protein kinase 10 1
35200035 10.1021/acs.jmedchem.1c01947 Mitogen-activated protein kinase 9 1
30108900 10.1039/C7MD00510E Serine/threonine-protein kinase Nek1 1
30108900 10.1039/C7MD00510E Serine/threonine-protein kinase Nek2 1
30108900 10.1039/C7MD00510E Serine/threonine-protein kinase Nek3 1
30108900 10.1039/C7MD00510E Serine/threonine-protein kinase Nek4 1
30108900 10.1039/C7MD00510E Serine/threonine-protein kinase Nek5 1
30108900 10.1039/C7MD00510E Serine/threonine-protein kinase Nek6 1
30108900 10.1039/C7MD00510E Serine/threonine-protein kinase Nek7 1
30108900 10.1039/C7MD00510E Serine/threonine-protein kinase Nek9 1
30108900 10.1039/C7MD00510E Serine/threonine-protein kinase Nek11 1

Data from ChEMBL 36 via Core Engine