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Compound Detail

CHEMBL2179670

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CC(=O)Nc1ccc(CCN2CCC(COc3nc4ccccc4c4cn(C)cc34)CC2)cc1

Basic Information

ChEMBL ID CHEMBL2179670
Phase Preclinical
Structure Type MOL
InChI Key YJAIZWWQRYKSON-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

456.6
MW (Da)
5.02
ALogP
5
HBA
1
HBD
59.4
PSA (Ų)
0.42
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H32N4O2
MW 456.59
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.11

Activity Summary

Ki 2 meas. best 8.7
IC50 1 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 4
CHEMBL1875
Ki 8.7 8.7 2.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 7.7 7.7 20.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 5.5 5.5 3162.3 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23043420 10.1021/jm300573d Voltage-gated inwardly rectifying potassium channel KCNH2 1
23043420 10.1021/jm300573d 5-hydroxytryptamine receptor 2A 1
23043420 10.1021/jm300573d 5-hydroxytryptamine receptor 4 1

Data from ChEMBL 36 via Core Engine