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Compound Detail

CHEMBL4564389

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CC1=C(C(=O)Nc2cc(Cl)ccc2Cl)C(c2ccco2)C2=C(CCCC2=O)N1

Basic Information

ChEMBL ID CHEMBL4564389
Phase Preclinical
Structure Type MOL
InChI Key GGTYQECCGLBHGS-UHFFFAOYSA-N
3
Targets
5
Activities
1
Assay Types
8
PK Parameters
9
Publications
0
Known Names

Molecular Properties

417.3
MW (Da)
5.19
ALogP
4
HBA
2
HBD
71.3
PSA (Ų)
0.72
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H18Cl2N2O3
MW 417.29
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -1.78

Activity Summary

EC50 5 meas. best 6.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Free fatty acid receptor 3
CHEMBL5201
EC50 6.89 6.2533 128.8 3
Free fatty acid receptor 3
CHEMBL3886125
EC50 6.34 6.34 457.1 1
Free fatty acid receptor 3
CHEMBL3309101
EC50 5.88 5.88 1318.3 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 7050.0 ng.hr.mL-1 Mus musculus
CL 19.6 mL.min-1.kg-1 Mus musculus
Cmax 13755.42 nM Mus musculus
F 88.0 % Mus musculus
T1/2 0.3717 hr Mus musculus
T1/2 1.013 hr Mus musculus
Tmax 0.5 hr Mus musculus
Vd 0.629 L.kg-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32141297 10.1021/acs.jmedchem.9b02036 ADMET 9
32141297 10.1021/acs.jmedchem.9b02036 Free fatty acid receptor 3 6
38641152 10.1016/j.bmcl.2024.129758 Free fatty acid receptor 3 2
32141297 10.1021/acs.jmedchem.9b02036 Free fatty acid receptor 1 1
32141297 10.1021/acs.jmedchem.9b02036 Free fatty acid receptor 4 1
32141297 10.1021/acs.jmedchem.9b02036 Free fatty acid receptor 2 1
32141297 10.1021/acs.jmedchem.9b02036 G-protein coupled receptor 84 1
32141297 10.1021/acs.jmedchem.9b02036 Voltage-dependent L-type calcium channel subunit alpha-1C 1
38641152 10.1016/j.bmcl.2024.129758 Free fatty acid receptor 2 1

Data from ChEMBL 36 via Core Engine