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Compound Detail

CHEMBL63167

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FC1(Cc2ccccc2C(F)(F)F)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1

Basic Information

ChEMBL ID CHEMBL63167
Phase Preclinical
Structure Type MOL
InChI Key QCGOFEMUVCYZKT-UHFFFAOYSA-N
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

485.5
MW (Da)
5.75
ALogP
4
HBA
1
HBD
49.7
PSA (Ų)
0.34
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 C26H27F4N5
MW 485.53
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.13

Activity Summary

EC50 2 meas. best 9.7
IC50 2 meas. best 9.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1D
CHEMBL1983
EC50 9.7 9.7 0.2 1
5-hydroxytryptamine receptor 1D
CHEMBL1983
IC50 9.52 9.52 0.3 1
5-hydroxytryptamine receptor 1B
CHEMBL1898
IC50 7.85 7.85 14.0 1
5-hydroxytryptamine receptor 1B
CHEMBL1898
EC50 6.54 6.54 290.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10377215 10.1021/jm981133m 5-hydroxytryptamine receptor 1D 3
10377215 10.1021/jm981133m 5-hydroxytryptamine receptor 1B 3
10377215 10.1021/jm981133m Serotonin 1 receptors; 5-HT1B & 5-HT1D 1

Data from ChEMBL 36 via Core Engine