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Compound Detail

CHEMBL299506

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COc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cnc(Oc3cccnc3C)cc1C)CC2

Basic Information

ChEMBL ID CHEMBL299506
Phase Preclinical
Structure Type MOL
InChI Key LGELKLOINROYEG-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

458.4
MW (Da)
5.51
ALogP
5
HBA
1
HBD
76.6
PSA (Ų)
0.56
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H21F3N4O3
MW 458.44
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.45

Activity Summary

Ki 3 meas. best 6.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2C
CHEMBL225
Ki 6.7 6.7 199.5 1
5-hydroxytryptamine receptor 2B
CHEMBL1833
Ki 6.6 6.6 251.2 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 6.2 6.2 631.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10969986 10.1016/s0960-894x(00)00364-4 5-hydroxytryptamine receptor 2C 1
10969986 10.1016/s0960-894x(00)00364-4 5-hydroxytryptamine receptor 2A 1
10969986 10.1016/s0960-894x(00)00364-4 5-hydroxytryptamine receptor 2B 1
10969986 10.1016/s0960-894x(00)00364-4 Serotonin 2 receptors; 5-HT2a & 5-HT2c 1
10969986 10.1016/s0960-894x(00)00364-4 Serotonin receptor (2b and 2c) 1

Data from ChEMBL 36 via Core Engine