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Compound Detail

CHEMBL4287941

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CC(CC(=O)O)CC(=O)c1c(CCCCCCc2ccccc2)n(C)c2ccc(Cl)cc12

Basic Information

ChEMBL ID CHEMBL4287941
Phase Preclinical
Structure Type MOL
InChI Key LSXCAWRVGLPZEY-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
3
Publications
0
Known Names

Molecular Properties

454.0
MW (Da)
6.86
ALogP
3
HBA
1
HBD
59.3
PSA (Ų)
0.24
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H32ClNO3
MW 454.01
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.13

Activity Summary

IC50 1 meas. best 9.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxoeicosanoid receptor 1
CHEMBL1628461
IC50 9.55 9.55 0.3 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 567512.5 ng.hr.mL-1 Macaca fascicularis
Cmax 108000.0 nM Macaca fascicularis
T1/2 7.4 hr Macaca fascicularis
Tmax 2.5 hr Macaca fascicularis

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29972644 10.1021/acs.jmedchem.8b00154 Cynomolgus monkey 4
29972644 10.1021/acs.jmedchem.8b00154 Oxoeicosanoid receptor 1 1
29972644 10.1021/acs.jmedchem.8b00154 ADMET 1

Data from ChEMBL 36 via Core Engine