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Compound Detail

CHEMBL3956307

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COc1cc(C(=O)N(CCCc2ccccc2)Cc2ccc(OCC(=O)O)cc2)cc(OC)c1C

Basic Information

ChEMBL ID CHEMBL3956307
Phase Preclinical
Structure Type MOL
InChI Key PLXXUMCDNICFNH-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
7
Publications
0
Known Names

Molecular Properties

477.6
MW (Da)
4.75
ALogP
5
HBA
1
HBD
85.3
PSA (Ų)
0.41
QED
0
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H31NO6
MW 477.56
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.83

Activity Summary

IC50 2 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Lysophosphatidic acid receptor 1
CHEMBL3819
IC50 7.0 7.0 100.0 1
Lysophosphatidic acid receptor 2
CHEMBL3724
IC50 4.64 4.64 23000.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.4 hr Rattus norvegicus
T1/2 0.3667 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27774128 10.1021/acsmedchemlett.6b00225 ADMET 2
27774128 10.1021/acsmedchemlett.6b00225 Rattus norvegicus 1
27774128 10.1021/acsmedchemlett.6b00225 NON-PROTEIN TARGET 1
27774128 10.1021/acsmedchemlett.6b00225 No relevant target 1
27774128 10.1021/acsmedchemlett.6b00225 Lysophosphatidic acid receptor 3 1
27774128 10.1021/acsmedchemlett.6b00225 Lysophosphatidic acid receptor 2 1
27774128 10.1021/acsmedchemlett.6b00225 Lysophosphatidic acid receptor 1 1

Data from ChEMBL 36 via Core Engine