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Compound Detail

CHEMBL343682

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CC1(C)CC(Nc2cc3c(ccc(=O)n3-c3c(Cl)cccc3Cl)c(-c3ccccc3Cl)n2)CC(C)(C)N1

Basic Information

ChEMBL ID CHEMBL343682
Phase Preclinical
Structure Type MOL
InChI Key JPAXUPOTRXLXQE-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
4
PK Parameters
2
Publications
0
Known Names

Molecular Properties

555.9
MW (Da)
7.73
ALogP
5
HBA
2
HBD
59.0
PSA (Ų)
0.27
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 C29H29Cl3N4O
MW 555.94
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -0.69

Activity Summary

IC50 2 meas. best 9.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MAP kinase p38
CHEMBL2094115
IC50 9.1 8.55 0.8 2

Pharmacokinetic Data

Parameter Value Units Species
AUC 1879.08 ng.hr.mL-1 Rattus norvegicus
CL 9.4 mL.min-1.kg-1 Rattus norvegicus
F 5.9 % Rattus norvegicus
T1/2 2.7 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
MAP kinase p38 IC50 = 0.8 nM 9.1 Inhibition of p38 MAP kinase 12565952
MAP kinase p38 IC50 = 10.0 nM 8.0 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