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Compound Detail

CHEMBL5094234

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CCNCCc1ccc(Cl)c(-c2ccccc2OC)c1.Cl

Basic Information

ChEMBL ID CHEMBL5094234
Phase Preclinical
Structure Type MOL
InChI Key SXOXLJQRLIFVCQ-UHFFFAOYSA-N
Parent Compound CHEMBL5096019
Active Moiety CHEMBL5096019
8
Targets
11
Activities
2
Assay Types
10
PK Parameters
19
Publications
0
Known Names

Molecular Properties

289.8
MW (Da)
4.17
ALogP
2
HBA
1
HBD
21.3
PSA (Ų)
0.81
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H21Cl2NO
MW 326.27
Aromatic Rings 2
Heavy Atoms 20
NP-Likeness -0.45

Activity Summary

Ki 9 meas. best 8.8
EC50 2 meas. best 6.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 7
CHEMBL3155
Ki 8.8 8.675 1.6 2
5-hydroxytryptamine receptor 1D
CHEMBL1983
Ki 8.28 8.28 5.3 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 7.28 7.28 52.0 1
5-hydroxytryptamine receptor 2B
CHEMBL1833
Ki 6.89 6.89 130.0 1
5-hydroxytryptamine receptor 7
CHEMBL3155
EC50 6.75 6.745 180.0 2
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 6.28 6.28 520.0 1
5-hydroxytryptamine receptor 1B
CHEMBL1898
Ki 6.24 6.24 580.0 1
5-hydroxytryptamine receptor 5A
CHEMBL3426
Ki 6.16 6.16 700.0 1
5-hydroxytryptamine receptor 1E
CHEMBL2182
Ki 5.58 5.58 2600.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 32.9 ng.hr.mL-1 Mus musculus
AUC 442.3 ng.hr.mL-1 Mus musculus
CL 477.7 mL.min-1.kg-1 Mus musculus
Cmax 1199.75 nM Mus musculus
F 134.4 % Mus musculus
MRT 0.7 hr Mus musculus
MRT 1.3 hr Mus musculus
T1/2 0.5 hr Mus musculus
T1/2 1.0 hr Mus musculus
Tmax 0.4 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34032427 10.1021/acs.jmedchem.1c00110 ADMET 12
34032427 10.1021/acs.jmedchem.1c00110 Unchecked 9
34032427 10.1021/acs.jmedchem.1c00110 5-hydroxytryptamine receptor 7 8
34032427 10.1021/acs.jmedchem.1c00110 Mus musculus 4
34032427 10.1021/acs.jmedchem.1c00110 5-hydroxytryptamine receptor 5A 1
34032427 10.1021/acs.jmedchem.1c00110 Cytochrome P450 3A4 1
34032427 10.1021/acs.jmedchem.1c00110 Cytochrome P450 2D6 1
34032427 10.1021/acs.jmedchem.1c00110 Cytochrome P450 2C19 1
34032427 10.1021/acs.jmedchem.1c00110 Cytochrome P450 2C9 1
34032427 10.1021/acs.jmedchem.1c00110 Cytochrome P450 1A2 1
34032427 10.1021/acs.jmedchem.1c00110 5-hydroxytryptamine receptor 6 1
34032427 10.1021/acs.jmedchem.1c00110 5-hydroxytryptamine receptor 3A 1
34032427 10.1021/acs.jmedchem.1c00110 5-hydroxytryptamine receptor 2C 1
34032427 10.1021/acs.jmedchem.1c00110 5-hydroxytryptamine receptor 2B 1
34032427 10.1021/acs.jmedchem.1c00110 5-hydroxytryptamine receptor 2A 1
34032427 10.1021/acs.jmedchem.1c00110 5-hydroxytryptamine receptor 1E 1
34032427 10.1021/acs.jmedchem.1c00110 5-hydroxytryptamine receptor 1D 1
34032427 10.1021/acs.jmedchem.1c00110 5-hydroxytryptamine receptor 1B 1
34032427 10.1021/acs.jmedchem.1c00110 5-hydroxytryptamine receptor 1A 1

Data from ChEMBL 36 via Core Engine