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Compound Detail

CHEMBL1771097

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O=C(NC1CC1)c1ccc(OCC2CC2C2CCN(c3ncc(Cl)cn3)CC2)cc1F

Basic Information

ChEMBL ID CHEMBL1771097
Phase Preclinical
Structure Type MOL
InChI Key RWBWCXVARSSZKV-UHFFFAOYSA-N
3
Targets
6
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

444.9
MW (Da)
4.09
ALogP
5
HBA
1
HBD
67.3
PSA (Ų)
0.70
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H26ClFN4O2
MW 444.94
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -1.25

Activity Summary

EC50 4 meas. best 8.05
IC50 2 meas. best 5.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glucose-dependent insulinotropic receptor
CHEMBL5263
EC50 8.05 7.845 9.0 2
Glucose-dependent insulinotropic receptor
CHEMBL5652
EC50 7.7 7.56 20.0 2
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.82 5.77 1500.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21273063 10.1016/j.bmcl.2010.12.086 Glucose-dependent insulinotropic receptor 4
21273063 10.1016/j.bmcl.2010.12.086 Voltage-gated inwardly rectifying potassium channel KCNH2 2

Data from ChEMBL 36 via Core Engine