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Compound Detail

CHEMBL356754

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CC(C)N1CCC(c2cc3c(ccc(=O)n3-c3c(Cl)cccc3Cl)c(-c3ccccc3Cl)n2)CC1

Basic Information

ChEMBL ID CHEMBL356754
Phase Preclinical
Structure Type MOL
InChI Key WTYSITXLWIBADH-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
2
PK Parameters
2
Publications
0
Known Names

Molecular Properties

526.9
MW (Da)
7.60
ALogP
4
HBA
0
HBD
38.1
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 C28H26Cl3N3O
MW 526.90
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.93

Activity Summary

IC50 2 meas. best 8.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MAP kinase p38
CHEMBL2094115
IC50 8.89 8.6 1.3 2

Pharmacokinetic Data

Parameter Value Units Species
CL 51.0 mL.min-1.kg-1 Rattus norvegicus
F 32.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
MAP kinase p38 IC50 = 1.3 nM 8.89 Inhibition of p38 MAP kinase 12565952
MAP kinase p38 IC50 = 4.9 nM 8.31 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
12565952 10.1016/s0960-894x(02)00990-3 Rattus norvegicus 2

Data from ChEMBL 36 via Core Engine