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Compound Detail

CHEMBL5081988

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Cc1cc(Cn2ncn(-c3ccc(Br)cc3)c2=O)cc(C)c1OC(C)(C)C(=O)O

Basic Information

ChEMBL ID CHEMBL5081988
Phase Preclinical
Structure Type MOL
InChI Key JEFBCKUSPLSOEI-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

460.3
MW (Da)
3.70
ALogP
6
HBA
1
HBD
86.3
PSA (Ų)
0.61
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H22BrN3O4
MW 460.33
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.86

Activity Summary

EC50 3 meas. best 7.67

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Peroxisome proliferator-activated receptor delta
CHEMBL3979
EC50 7.67 7.67 21.6 1
Peroxisome proliferator-activated receptor alpha
CHEMBL239
EC50 7.21 7.21 62.2 1
Peroxisome proliferator-activated receptor gamma
CHEMBL235
EC50 5.75 5.75 1778.8 1

Pharmacokinetic Data

Parameter Value Units Species
CL 1.45 mL.min-1.kg-1 Homo sapiens
T1/2 2.0 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35060744 10.1021/acs.jmedchem.1c02002 Peroxisome proliferator-activated receptor alpha 2
35060744 10.1021/acs.jmedchem.1c02002 Peroxisome proliferator-activated receptor delta 2
35060744 10.1021/acs.jmedchem.1c02002 Peroxisome proliferator-activated receptor gamma 2
35060744 10.1021/acs.jmedchem.1c02002 ADMET 2

Data from ChEMBL 36 via Core Engine