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Compound Detail

CHEMBL3740844

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CC(C)c1nc(C(=O)NC[C@@H]2[C@H]3CN(C(C)C)C[C@@H]23)c2ccccn12

Basic Information

ChEMBL ID CHEMBL3740844
Phase Preclinical
Structure Type MOL
InChI Key SZYHHXMEWRCMLP-PHZGNYQRSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
5
Publications
0
Known Names

Molecular Properties

340.5
MW (Da)
2.77
ALogP
4
HBA
1
HBD
49.6
PSA (Ų)
0.91
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H28N4O
MW 340.47
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -1.13

Activity Summary

EC50 1 meas. best 7.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 4
CHEMBL1875
EC50 7.74 7.74 18.3 1

Pharmacokinetic Data

Parameter Value Units Species
CL 76.2 mL.min-1.kg-1 Rattus norvegicus
CL 4.9 mL.min-1.kg-1 Homo sapiens
CL 119.0 mL.min-1.kg-1 Rattus norvegicus
Cmax 234.97 nM Rattus norvegicus
F 5.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26363507 10.1016/j.ejmech.2015.08.051 Rattus norvegicus 5
26363507 10.1016/j.ejmech.2015.08.051 5-hydroxytryptamine receptor 4 2
26363507 10.1016/j.ejmech.2015.08.051 Liver microsome 2
26363507 10.1016/j.ejmech.2015.08.051 Cytochrome P450 2D6 1
26363507 10.1016/j.ejmech.2015.08.051 Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine