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Compound Detail

CHEMBL3770689

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COc1cc(F)c(Cl)cc1C1CC1CN.Cl

Basic Information

ChEMBL ID CHEMBL3770689
Phase Preclinical
Structure Type MOL
InChI Key MJLDXOHMJFYWSZ-UHFFFAOYSA-N
Parent Compound CHEMBL3771380
Active Moiety CHEMBL3771380
3
Targets
12
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

229.7
MW (Da)
2.55
ALogP
2
HBA
1
HBD
35.2
PSA (Ų)
0.86
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C11H14Cl2FNO
MW 266.14
Aromatic Rings 1
Heavy Atoms 15
NP-Likeness -0.16

Activity Summary

EC50 12 meas. best 8.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2C
CHEMBL225
EC50 8.12 7.955 7.6 4
5-hydroxytryptamine receptor 2B
CHEMBL1833
EC50 7.6 7.04 25.0 4
5-hydroxytryptamine receptor 2A
CHEMBL224
EC50 7.09 6.86 81.0 4

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
5-hydroxytryptamine receptor 2C EC50 = 7.6 nM 8.12 Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293... 26704965
5-hydroxytryptamine receptor 2C EC50 = 7.762 nM 8.11 Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293... 26704965
5-hydroxytryptamine receptor 2C EC50 = 16.0 nM 7.8 Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293... 26704965
5-hydroxytryptamine receptor 2C EC50 = 16.22 nM 7.79 Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293... 26704965
5-hydroxytryptamine receptor 2B EC50 = 25.0 nM 7.6 Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cel... 26704965
5-hydroxytryptamine receptor 2B EC50 = 25.12 nM 7.6 Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cel... 26704965
5-hydroxytryptamine receptor 2A EC50 = 81.0 nM 7.09 Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cel... 26704965
5-hydroxytryptamine receptor 2A EC50 = 81.28 nM 7.09 Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cel... 26704965
5-hydroxytryptamine receptor 2A EC50 = 235.0 nM 6.63 Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cel... 26704965
5-hydroxytryptamine receptor 2A EC50 = 234.42 nM 6.63 Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cel... 26704965
5-hydroxytryptamine receptor 2B EC50 = 329.0 nM 6.48 Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cel... 26704965
5-hydroxytryptamine receptor 2B EC50 = 331.13 nM 6.48 Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cel... 26704965

Literature References

PubMed DOI Target Context # Activities
26704965 10.1021/acs.jmedchem.5b01153 5-hydroxytryptamine receptor 2C 6
26704965 10.1021/acs.jmedchem.5b01153 5-hydroxytryptamine receptor 2B 6
26704965 10.1021/acs.jmedchem.5b01153 5-hydroxytryptamine receptor 2A 6

Data from ChEMBL 36 via Core Engine