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Compound Detail

CHEMBL4436229

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CCCC1C(C(=O)Nc2cc(Cl)ccc2Cl)=C(C)NC2=C1C(=O)CCC2

Basic Information

ChEMBL ID CHEMBL4436229
Phase Preclinical
Structure Type MOL
InChI Key IIXZJMYGKNKDGN-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
8
PK Parameters
9
Publications
0
Known Names

Molecular Properties

393.3
MW (Da)
5.23
ALogP
3
HBA
2
HBD
58.2
PSA (Ų)
0.74
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H22Cl2N2O2
MW 393.31
Aromatic Rings 1
Heavy Atoms 26
NP-Likeness -1.33

Activity Summary

EC50 1 meas. best 6.84

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Free fatty acid receptor 3
CHEMBL5201
EC50 6.84 6.84 144.5 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 563.33 ng.hr.mL-1 Mus musculus
CL 70.3 mL.min-1.kg-1 Mus musculus
Cmax 1426.36 nM Mus musculus
F 36.0 % Mus musculus
T1/2 0.19 hr Mus musculus
T1/2 1.058 hr Mus musculus
Tmax 0.5 hr Mus musculus
Vd 1.15 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 No relevant target 6
32141297 10.1021/acs.jmedchem.9b02036 Free fatty acid receptor 3 3
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
32141297 10.1021/acs.jmedchem.9b02036 Unchecked 1

Data from ChEMBL 36 via Core Engine