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Compound Detail

CHEMBL4081863

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Cc1nc(-c2cccc3ccccc23)sc1C(=O)N1CCC(CO)CC1

Basic Information

ChEMBL ID CHEMBL4081863
Phase Preclinical
Structure Type MOL
InChI Key OZMVYBUWNRHUPA-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
10
Publications
0
Known Names

Molecular Properties

366.5
MW (Da)
4.12
ALogP
4
HBA
1
HBD
53.4
PSA (Ų)
0.76
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 C21H22N2O2S
MW 366.49
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -1.32

Activity Summary

EC50 1 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2C
CHEMBL225
EC50 8.22 8.22 6.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.35 hr Homo sapiens
T1/2 0.1 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28635286 10.1021/acs.jmedchem.7b00385 ADMET 7
28635286 10.1021/acs.jmedchem.7b00385 Plasma 4
28635286 10.1021/acs.jmedchem.7b00385 5-hydroxytryptamine receptor 2C 2
28635286 10.1021/acs.jmedchem.7b00385 Liver 2
28635286 10.1021/acs.jmedchem.7b00385 No relevant target 2
28635286 10.1021/acs.jmedchem.7b00385 Brain 2
28635286 10.1021/acs.jmedchem.7b00385 Unchecked 2
28635286 10.1021/acs.jmedchem.7b00385 Broad substrate specificity ATP-binding cassette transporter ABCG2 2
28635286 10.1021/acs.jmedchem.7b00385 5-hydroxytryptamine receptor 2A 1
28635286 10.1021/acs.jmedchem.7b00385 5-hydroxytryptamine receptor 2B 1

Data from ChEMBL 36 via Core Engine