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Compound Detail

CHEMBL4796370

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Cc1nn(-c2ccnc3[nH]c(-c4cccc5c4ccn5C)nc23)cc1CN(C)C

Basic Information

ChEMBL ID CHEMBL4796370
Phase Preclinical
Structure Type MOL
InChI Key WCJUHMIFNPLSSY-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
2
PK Parameters
10
Publications
0
Known Names

Molecular Properties

385.5
MW (Da)
3.67
ALogP
6
HBA
1
HBD
67.6
PSA (Ų)
0.51
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23N7
MW 385.48
Aromatic Rings 5
Heavy Atoms 29
NP-Likeness -1.45

Activity Summary

IC50 4 meas. best 9.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase SYK
CHEMBL2599
IC50 9.08 9.08 0.8 2
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.58 5.58 2600.0 2

Pharmacokinetic Data

Parameter Value Units Species
CL 0.037 mL.min-1.kg-1 Homo sapiens
CL 37.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32721854 10.1016/j.bmcl.2020.127393 ADMET 2
32721854 10.1016/j.bmcl.2020.127393 No relevant target 2
32877741 10.1016/j.bmcl.2020.127523 ADMET 2
32721854 10.1016/j.bmcl.2020.127393 Voltage-gated inwardly rectifying potassium channel KCNH2 1
32721854 10.1016/j.bmcl.2020.127393 SUD4 1
32721854 10.1016/j.bmcl.2020.127393 Tyrosine-protein kinase SYK 1
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 Voltage-gated inwardly rectifying potassium channel KCNH2 1
32877741 10.1016/j.bmcl.2020.127523 SUD4 1

Data from ChEMBL 36 via Core Engine