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Compound Detail

CHEMBL481943

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COCCn1c(SC)nc(-c2ccc(F)cc2)c1-c1ccnc(NC2CCCCC2)c1

Basic Information

ChEMBL ID CHEMBL481943
Phase Preclinical
Structure Type MOL
InChI Key OOKDYIKDKLFLOG-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

440.6
MW (Da)
5.86
ALogP
6
HBA
1
HBD
52.0
PSA (Ų)
0.44
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H29FN4OS
MW 440.59
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.49

Activity Summary

IC50 2 meas. best 7.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 14
CHEMBL260
IC50 7.38 7.38 42.0 1
Blood
CHEMBL613416
IC50 5.45 5.45 3570.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mitogen-activated protein kinase 14 IC50 = 42.0 nM 7.38 Inhibition of p38alpha 18578517
Blood IC50 = 3570.0 nM 5.45 Inhibition of TNFalpha release in human whole blood 18578517

Literature References

PubMed DOI Target Context # Activities
18578517 10.1021/jm701529q Unchecked 3
18578517 10.1021/jm701529q Mitogen-activated protein kinase 14 2
18578517 10.1021/jm701529q Cytochrome P450 3A4 1
18578517 10.1021/jm701529q Blood 1
18578517 10.1021/jm701529q Cytochrome P450 2C19 1
18578517 10.1021/jm701529q Cytochrome P450 2C9 1
18578517 10.1021/jm701529q Cytochrome P450 1A2 1
18578517 10.1021/jm701529q Tyrosine-protein kinase Lck 1
18578517 10.1021/jm701529q Rho-associated protein kinase 2 1
18578517 10.1021/jm701529q Glycogen synthase kinase-3 beta 1
18578517 10.1021/jm701529q RAC-alpha serine/threonine-protein kinase 1
18578517 10.1021/jm701529q Protein kinase C alpha type 1
18578517 10.1021/jm701529q Mitogen-activated protein kinase 13 1
18578517 10.1021/jm701529q Mitogen-activated protein kinase 12 1
18578517 10.1021/jm701529q Mitogen-activated protein kinase 11 1
18578517 10.1021/jm701529q Mitogen-activated protein kinase 10 1
18578517 10.1021/jm701529q Mitogen-activated protein kinase 9 1
18578517 10.1021/jm701529q Dual specificity mitogen-activated protein kinase kinase 1 1
18578517 10.1021/jm701529q MAP kinase-activated protein kinase 2 1
18578517 10.1021/jm701529q Mitogen-activated protein kinase 3 1

Data from ChEMBL 36 via Core Engine