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Compound Detail

CHEMBL142697

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CN1C2CCC1CC(Nc1cc3c(ccc(=O)n3-c3c(Cl)cccc3Cl)c(-c3ccccc3Cl)n1)C2

Basic Information

ChEMBL ID CHEMBL142697
Phase Preclinical
Structure Type MOL
InChI Key KIJQUBGKXJVPER-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
4
PK Parameters
2
Publications
0
Known Names

Molecular Properties

539.9
MW (Da)
7.05
ALogP
5
HBA
1
HBD
50.2
PSA (Ų)
0.30
QED
2
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H25Cl3N4O
MW 539.89
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -0.52

Activity Summary

IC50 2 meas. best 9.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MAP kinase p38
CHEMBL2094115
IC50 9.4 8.51 0.4 2

Pharmacokinetic Data

Parameter Value Units Species
AUC 442.71 ng.hr.mL-1 Rattus norvegicus
CL 38.0 mL.min-1.kg-1 Rattus norvegicus
F 8.5 % Rattus norvegicus
T1/2 2.6 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
MAP kinase p38 IC50 = 0.4 nM 9.4 Inhibition of p38 MAP kinase 12565952
MAP kinase p38 IC50 = 24.0 nM 7.62 Inhibition of p38 kinase related TNF-alpha release 12565952

Literature References

PubMed DOI Target Context # Activities
12565952 10.1016/s0960-894x(02)00990-3 Rattus norvegicus 4
12565952 10.1016/s0960-894x(02)00990-3 MAP kinase p38 2

Data from ChEMBL 36 via Core Engine