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Compound Detail

CHEMBL3589153

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COc1cc(N2Cc3cn(-c4ccc(Cl)cc4)nc3C2=O)ccc1N1C[C@H](O)[C@@H](O)C1

Basic Information

ChEMBL ID CHEMBL3589153
Phase Preclinical
Structure Type MOL
InChI Key OGJOYPFWXIZCLU-OALUTQOASA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

440.9
MW (Da)
2.24
ALogP
7
HBA
2
HBD
91.1
PSA (Ų)
0.65
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H21ClN4O4
MW 440.89
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.16

Activity Summary

Ki 1 meas. best 7.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 7.96 7.96 11.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked Ki = 11.0 nM 7.96 Displacement of [Phe13, [125I]Tyr19]-MCH from human MCHR1 E4Q/A5T double mutant ... 26022839

Literature References

PubMed DOI Target Context # Activities
26022839 10.1016/j.bmcl.2015.05.008 Voltage-gated inwardly rectifying potassium channel KCNH2 2
26022839 10.1016/j.bmcl.2015.05.008 Unchecked 1

Data from ChEMBL 36 via Core Engine