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Compound Detail

CHEMBL2059527

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CCc1c(CCCC(=O)O)cccc1-c1ccc(-c2ccc(OC(C)C)c(C#N)c2)cc1

Basic Information

ChEMBL ID CHEMBL2059527
Phase Preclinical
Structure Type MOL
InChI Key ZKCIQVSIYOCDQA-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
1
PK Parameters
7
Publications
0
Known Names

Molecular Properties

427.5
MW (Da)
6.65
ALogP
3
HBA
1
HBD
70.3
PSA (Ų)
0.41
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H29NO3
MW 427.54
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.39

Activity Summary

EC50 1 meas. best 8.8
IC50 1 meas. best 5.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sphingosine 1-phosphate receptor 1
CHEMBL4333
EC50 8.8 8.8 1.6 1
Cytochrome P450 2C9
CHEMBL3397
IC50 5.4 5.4 3981.1 1

Pharmacokinetic Data

Parameter Value Units Species
Fu 0.0001 - Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22500954 10.1021/jm2016107 Nucleic Acid 2
22500954 10.1021/jm2016107 Sphingosine 1-phosphate receptor 1 1
22500954 10.1021/jm2016107 Sphingosine 1-phosphate receptor 3 1
22500954 10.1021/jm2016107 ADMET 1
22500954 10.1021/jm2016107 No relevant target 1
22500954 10.1021/jm2016107 Cytochrome P450 2C9 1
22500954 10.1021/jm2016107 Plasma 1

Data from ChEMBL 36 via Core Engine