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Compound Detail

CHEMBL4286792

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N=C1N[C@H]2[C@H](CN3C(=O)CCC3=O)NC(=N)N3C[C@H](NC(=O)c4cccc(C(F)(F)F)c4)C(O)(O)[C@]23N1

Basic Information

ChEMBL ID CHEMBL4286792
Phase Preclinical
Structure Type MOL
InChI Key KNGVCVURGYFVEP-UPDUFCCMSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

524.5
MW (Da)
-1.95
ALogP
7
HBA
8
HBD
194.0
PSA (Ų)
0.16
QED
2
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H23F3N8O5
MW 524.46
Aromatic Rings 1
Heavy Atoms 37
NP-Likeness 0.08

Activity Summary

IC50 3 meas. best 6.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium channel protein type 9 subunit alpha
CHEMBL4296
IC50 6.16 6.16 700.0 1
Unchecked
CHEMBL612545
IC50 4.26 4.26 55000.0 1
Sodium channel protein type 5 subunit alpha
CHEMBL1980
IC50 4.02 4.02 95000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30139550 10.1016/j.bmcl.2018.08.007 Unchecked 1
30139550 10.1016/j.bmcl.2018.08.007 Sodium channel protein type 9 subunit alpha 1
36385936 10.1021/acsmedchemlett.2c00378 Sodium channel protein type 9 subunit alpha 1
36385936 10.1021/acsmedchemlett.2c00378 Sodium channel protein type 4 subunit alpha 1
36385936 10.1021/acsmedchemlett.2c00378 Sodium channel protein type 5 subunit alpha 1
36385936 10.1021/acsmedchemlett.2c00378 Unchecked 1

Data from ChEMBL 36 via Core Engine