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Compound Detail

CHEMBL96480

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COc1ccc(CC2NCCc3c2[nH]c2cc(C)c(C)cc32)cc1OC

Basic Information

ChEMBL ID CHEMBL96480
Phase Preclinical
Structure Type MOL
InChI Key ODXWUVNDEWRVGP-UHFFFAOYSA-N
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

350.5
MW (Da)
4.23
ALogP
3
HBA
2
HBD
46.3
PSA (Ų)
0.74
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H26N2O2
MW 350.46
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness 0.50

Activity Summary

Ki 5 meas. best 9.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2B
CHEMBL323
Ki 9.7 9.7 0.2 1
5-hydroxytryptamine receptor 2C
CHEMBL324
Ki 8.52 8.515 3.0 2
5-hydroxytryptamine receptor 2A
CHEMBL322
Ki 8.33 8.315 4.7 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33528252 10.1021/acs.jmedchem.0c01887 5-hydroxytryptamine receptor 2B 3
8709108 10.1021/jm960062t 5-hydroxytryptamine receptor 2B 1
8709108 10.1021/jm960062t 5-hydroxytryptamine receptor 2A 1
8709108 10.1021/jm960062t 5-hydroxytryptamine receptor 2C 1
8709108 10.1021/jm960062t Serotonin receptor 2a and 2b (5HT2A and 5HT2B) 1
8709108 10.1021/jm960062t Unchecked 1
33528252 10.1021/acs.jmedchem.0c01887 5-hydroxytryptamine receptor 2A 1
33528252 10.1021/acs.jmedchem.0c01887 5-hydroxytryptamine receptor 2C 1

Data from ChEMBL 36 via Core Engine