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Compound Detail

CHEMBL102547

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CC(C)(C)c1cc(NC(=O)Nc2ccc3ccccc3c2)n(-c2ccccc2)n1

Basic Information

ChEMBL ID CHEMBL102547
Phase Preclinical
Structure Type MOL
InChI Key RTEBQURMARYTDH-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

384.5
MW (Da)
5.97
ALogP
3
HBA
2
HBD
59.0
PSA (Ų)
0.46
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H24N4O
MW 384.48
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.69

Activity Summary

EC50 1 meas. best 6.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MAP kinase p38
CHEMBL2094115
EC50 6.16 6.16 700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
MAP kinase p38 EC50 = 700.0 nM 6.16 Inhibition of LPS-induced tumor necrosis factor-alpha (TNF-alpha) production in ... 12086485

Literature References

PubMed DOI Target Context # Activities
12086485 10.1021/jm020057r MAP kinase p38 1
33035818 10.1016/j.ejmech.2020.112721 Mitogen-activated protein kinase 14 1
33035818 10.1016/j.ejmech.2020.112721 Mitogen-activated protein kinase 11 1
33035818 10.1016/j.ejmech.2020.112721 Serine/threonine-protein kinase B-raf 1
33035818 10.1016/j.ejmech.2020.112721 Aurora kinase B 1
33035818 10.1016/j.ejmech.2020.112721 STE20-like serine/threonine-protein kinase 1
33035818 10.1016/j.ejmech.2020.112721 Serine/threonine-protein kinase 10 1
33035818 10.1016/j.ejmech.2020.112721 Ephrin type-A receptor 2 1

Data from ChEMBL 36 via Core Engine