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Compound Detail

CHEMBL481750

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CSc1nc(-c2ccc(F)cc2)c(-c2ccnc(N[C@H]3CC[C@@H](C)CC3)c2)[nH]1

Basic Information

ChEMBL ID CHEMBL481750
Phase Preclinical
Structure Type MOL
InChI Key DDHYZAOORBKEHA-UJKQEGAGSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

396.5
MW (Da)
5.99
ALogP
4
HBA
2
HBD
53.6
PSA (Ų)
0.52
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H25FN4S
MW 396.54
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.32

Activity Summary

IC50 2 meas. best 7.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 14
CHEMBL260
IC50 7.51 7.51 31.0 1
Blood
CHEMBL613416
IC50 5.43 5.43 3680.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mitogen-activated protein kinase 14 IC50 = 31.0 nM 7.51 Inhibition of p38alpha 18578517
Blood IC50 = 3680.0 nM 5.43 Inhibition of TNFalpha release in human whole blood 18578517

Literature References

PubMed DOI Target Context # Activities
18578517 10.1021/jm701529q Blood 2
18578517 10.1021/jm701529q Mitogen-activated protein kinase 14 1

Data from ChEMBL 36 via Core Engine