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Compound Detail

CHEMBL3394105

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CC(=O)Nc1cc(-c2c(-c3ccc(F)cc3)nc(S/C=C\C(=O)O)n2C2CCCCC2)ccn1

Basic Information

ChEMBL ID CHEMBL3394105
Phase Preclinical
Structure Type MOL
InChI Key GTIQIAGCTCXGCN-OWBHPGMISA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

480.6
MW (Da)
5.91
ALogP
6
HBA
2
HBD
97.1
PSA (Ų)
0.32
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H25FN4O3S
MW 480.57
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.94

Activity Summary

IC50 2 meas. best 6.88

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 10
CHEMBL2637
IC50 6.88 6.88 133.0 1
Mitogen-activated protein kinase 14
CHEMBL260
IC50 6.78 6.78 165.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25475894 10.1021/jm501557a Unchecked 3
25475894 10.1021/jm501557a Fibroblast growth factor receptor 3 2
25475894 10.1021/jm501557a Mitogen-activated protein kinase 10 2
25475894 10.1021/jm501557a Mitogen-activated protein kinase 14 2
25475894 10.1021/jm501557a Calcium/calmodulin-dependent protein kinase type II subunit beta 1
25475894 10.1021/jm501557a Tyrosine-protein kinase ZAP-70 1
25475894 10.1021/jm501557a Fibroblast growth factor receptor 1 1
25475894 10.1021/jm501557a Receptor tyrosine-protein kinase erbB-4 1
25475894 10.1021/jm501557a Ephrin type-B receptor 4 1
25475894 10.1021/jm501557a Epidermal growth factor receptor 1
25475894 10.1021/jm501557a Proto-oncogene tyrosine-protein kinase Src 1
25475894 10.1021/jm501557a Casein kinase I isoform gamma-3 1
25475894 10.1021/jm501557a Tyrosine-protein kinase CSK 1
25475894 10.1021/jm501557a Cyclin-dependent kinase 4/cyclin D1 1
25475894 10.1021/jm501557a RAC-alpha serine/threonine-protein kinase 1
25475894 10.1021/jm501557a Aurora kinase A 1
25475894 10.1021/jm501557a Tyrosine-protein kinase ABL1 1
25475894 10.1021/jm501557a ALK tyrosine kinase receptor 1
25475894 10.1021/jm501557a Tyrosine-protein kinase BTK 1
25475894 10.1021/jm501557a Cyclin-dependent kinase 2 1

Data from ChEMBL 36 via Core Engine