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Compound Detail

CHEMBL4218771

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Cl.O=C(NCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1)c1ccccn1

Basic Information

ChEMBL ID CHEMBL4218771
Phase Preclinical
Structure Type MOL
InChI Key NJNMLUNJOFKGRR-UHFFFAOYSA-N
Parent Compound CHEMBL4300645
Active Moiety CHEMBL4300645
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

436.5
MW (Da)
3.50
ALogP
4
HBA
1
HBD
48.5
PSA (Ų)
0.62
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H27ClF2N4O
MW 472.97
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.66

Activity Summary

Ki 2 meas. best 9.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2C
CHEMBL324
Ki 9.1 9.1 0.8 1
5-hydroxytryptamine receptor 2A
CHEMBL322
Ki 6.66 6.66 218.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28943244 10.1016/j.bmc.2017.09.018 5-hydroxytryptamine receptor 1A 1
28943244 10.1016/j.bmc.2017.09.018 5-hydroxytryptamine receptor 2A 1
28943244 10.1016/j.bmc.2017.09.018 5-hydroxytryptamine receptor 2C 1

Data from ChEMBL 36 via Core Engine