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Compound Detail

CHEMBL164046

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CC(C)(NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1

Basic Information

ChEMBL ID CHEMBL164046
Phase Preclinical
Structure Type MOL
InChI Key RKAKHLWCVBGMID-FQEVSTJZSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

428.6
MW (Da)
4.14
ALogP
5
HBA
2
HBD
61.8
PSA (Ų)
0.44
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H32N6
MW 428.58
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.34

Activity Summary

IC50 2 meas. best 9.0
EC50 1 meas. best 9.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1D
CHEMBL1983
EC50 9.52 9.52 0.3 1
5-hydroxytryptamine receptor 1D
CHEMBL1983
IC50 9.0 9.0 1.0 1
5-hydroxytryptamine receptor 1B
CHEMBL1898
IC50 7.41 7.41 39.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10052975 10.1021/jm9805687 5-hydroxytryptamine receptor 1D 2
10052975 10.1021/jm9805687 Serotonin 1 receptors; 5-HT1B & 5-HT1D 2
10052975 10.1021/jm9805687 5-hydroxytryptamine receptor 1B 1
29500940 10.1016/j.ejmech.2018.02.043 C-X-C chemokine receptor type 4 1

Data from ChEMBL 36 via Core Engine