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Compound Detail

CHEMBL2441285

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COc1ccc2nc(Nc3cc(C(F)(F)c4ccc(F)cc4)nc(N[C@H]4CC[C@H](O)CC4)n3)sc2n1

Basic Information

ChEMBL ID CHEMBL2441285
Phase Preclinical
Structure Type MOL
InChI Key PFDUFECOJKSDAT-WKILWMFISA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

516.5
MW (Da)
5.23
ALogP
9
HBA
3
HBD
105.1
PSA (Ų)
0.31
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H23F3N6O2S
MW 516.55
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.35

Activity Summary

Ki 2 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase ITK/TSK
CHEMBL2959
Ki 7.8 7.8 15.8 1
Tyrosine-protein kinase Lck
CHEMBL258
Ki 6.7 6.7 199.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24900590 10.1021/ml400206q Tyrosine-protein kinase Lck 1
24900590 10.1021/ml400206q Tyrosine-protein kinase ITK/TSK 1
24900590 10.1021/ml400206q Aurora kinase B 1

Data from ChEMBL 36 via Core Engine