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Compound Detail

CHEMBL2023930

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CCc1cc(NC(=O)c2ccccc2F)ccc1-c1nnc(NCCCN2CCCCC2)o1

Basic Information

ChEMBL ID CHEMBL2023930
Phase Preclinical
Structure Type MOL
InChI Key WISMAYYAAISQCZ-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

451.6
MW (Da)
4.98
ALogP
6
HBA
2
HBD
83.3
PSA (Ų)
0.45
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H30FN5O2
MW 451.55
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.91

Activity Summary

EC50 1 meas. best 6.9
IC50 1 meas. best 5.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuronal acetylcholine receptor subunit alpha-7
CHEMBL2492
EC50 6.9 6.9 125.9 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.4 5.4 3981.1 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22503248 10.1016/j.bmcl.2012.03.040 Neuronal acetylcholine receptor subunit alpha-7 1
22503248 10.1016/j.bmcl.2012.03.040 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine