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Compound Detail

CHEMBL4741959

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CNC(=O)c1nc(C)n2ccc(Nc3nccc(-n4cc(N[C@@H]5CCOC[C@@H]5N)c(C)n4)n3)cc12

Basic Information

ChEMBL ID CHEMBL4741959
Phase Preclinical
Structure Type MOL
InChI Key NPSUYJDNOFYGMK-DLBZAZTESA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

476.6
MW (Da)
1.56
ALogP
11
HBA
4
HBD
149.3
PSA (Ų)
0.33
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H28N10O2
MW 476.55
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.20

Activity Summary

IC50 1 meas. best 8.49

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase SYK
CHEMBL2599
IC50 8.49 8.49 3.2 1

Pharmacokinetic Data

Parameter Value Units Species
CL 32.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase SYK IC50 = 3.2 nM 8.49 Inhibition of SYK (unknown origin) 32877741

Literature References

PubMed DOI Target Context # Activities
32877741 10.1016/j.bmcl.2020.127523 ADMET 3
32877741 10.1016/j.bmcl.2020.127523 Tyrosine-protein kinase SYK 1
32877741 10.1016/j.bmcl.2020.127523 No relevant target 1
32877741 10.1016/j.bmcl.2020.127523 Unchecked 1
32877741 10.1016/j.bmcl.2020.127523 Voltage-gated inwardly rectifying potassium channel KCNH2 1
32877741 10.1016/j.bmcl.2020.127523 SUD4 1

Data from ChEMBL 36 via Core Engine