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Compound Detail

CHEMBL2178522

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Cc1cn(-c2ccc(Nc3cccc4c3nc(-c3ccc(F)cc3)n4C)nc2)cn1

Basic Information

ChEMBL ID CHEMBL2178522
Phase Preclinical
Structure Type MOL
InChI Key SBMTYDPNLHAVKD-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

398.4
MW (Da)
5.01
ALogP
6
HBA
1
HBD
60.6
PSA (Ų)
0.46
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H19FN6
MW 398.45
Aromatic Rings 5
Heavy Atoms 30
NP-Likeness -1.62

Activity Summary

IC50 2 meas. best 6.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gamma-secretase
CHEMBL2094135
IC50 6.74 6.74 183.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.28 5.28 5200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22650177 10.1021/jm201710f Mus musculus 2
22650177 10.1021/jm201710f Gamma-secretase 2
22650177 10.1021/jm201710f Voltage-gated inwardly rectifying potassium channel KCNH2 1
22650177 10.1021/jm201710f Plasma 1
22650177 10.1021/jm201710f Brain 1
22650177 10.1021/jm201710f Unchecked 1
22650177 10.1021/jm201710f Beta-secretase 1 1

Data from ChEMBL 36 via Core Engine