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Compound Detail

CHEMBL142187

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CN1C2CCC1CC(Nc1cc(-c3ccccc3Cl)c3c(c1)N(c1c(Cl)cccc1Cl)C(=O)NC3)C2

Basic Information

ChEMBL ID CHEMBL142187
Phase Preclinical
Structure Type MOL
InChI Key CUNDIGFRTACXCX-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

541.9
MW (Da)
7.71
ALogP
3
HBA
2
HBD
47.6
PSA (Ų)
0.36
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 C28H27Cl3N4O
MW 541.91
Aromatic Rings 3
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 8.55 0.4 2

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 = 20.0 nM 7.7 Inhibition of p38 kinase related TNF-alpha release 12565952

Literature References

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

Data from ChEMBL 36 via Core Engine