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Compound Detail

CHEMBL5398877

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Cc1cccc2c3c(ccc12)-c1oc2c(c1C(=O)C3=O)CCN(CCO)C2

Basic Information

ChEMBL ID CHEMBL5398877
Phase Preclinical
Structure Type MOL
InChI Key GCYKCXXLWUWUFQ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
5
Publications
0
Known Names

Molecular Properties

361.4
MW (Da)
3.14
ALogP
5
HBA
1
HBD
70.8
PSA (Ų)
0.71
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H19NO4
MW 361.40
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness 0.32

Activity Summary

IC50 1 meas. best 6.94

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Peritoneal macrophage
CHEMBL5314330
IC50 6.94 6.94 114.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 2.0 mL.min-1.g-1 Homo sapiens
CL 7.64 mL.min-1.g-1 Mus musculus
T1/2 11.55 hr Homo sapiens
T1/2 3.03 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Peritoneal macrophage IC50 = 114.0 nM 6.94 Antiinflammatory activity against LPS-stimulated mouse peritoneal macrophage ass... 36786612

Literature References

PubMed DOI Target Context # Activities
36786612 10.1021/acs.jmedchem.2c01967 Peritoneal macrophage 6
36786612 10.1021/acs.jmedchem.2c01967 NACHT, LRR and PYD domains-containing protein 3 6
36786612 10.1021/acs.jmedchem.2c01967 Unchecked 6
36786612 10.1021/acs.jmedchem.2c01967 ADMET 4
36786612 10.1021/acs.jmedchem.2c01967 No relevant target 1

Data from ChEMBL 36 via Core Engine