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Compound Detail

CHEMBL356994

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CC1(C)CC(Nc2cc(-c3ccccc3Cl)c3c(c2)N(c2c(Cl)cccc2Cl)C(=O)NC3)CC(C)(C)N1

Basic Information

ChEMBL ID CHEMBL356994
Phase Preclinical
Structure Type MOL
InChI Key WLSRUNCRTNITTJ-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

558.0
MW (Da)
8.40
ALogP
3
HBA
3
HBD
56.4
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 C29H31Cl3N4O
MW 557.95
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -0.69

Activity Summary

IC50 2 meas. best 8.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MAP kinase p38
CHEMBL2094115
IC50 8.43 7.565 3.7 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
MAP kinase p38 IC50 = 3.7 nM 8.43 Inhibition of p38 MAP kinase 12565952
MAP kinase p38 IC50 = 200.0 nM 6.7 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