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Compound Detail

CHEMBL4066327

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O=C(NCC(O)CO)c1ccc2c(c1)C(=O)c1ccc(Nc3ccc(F)c(NC(=O)C4CC4)c3)cc1CC2

Basic Information

ChEMBL ID CHEMBL4066327
Phase Preclinical
Structure Type MOL
InChI Key RQTNBTMMWRUTFF-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

517.6
MW (Da)
3.33
ALogP
6
HBA
5
HBD
127.8
PSA (Ų)
0.31
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H28FN3O5
MW 517.56
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -1.05

Activity Summary

IC50 1 meas. best 8.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 14
CHEMBL260
IC50 8.17 8.17 6.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mitogen-activated protein kinase 14 IC50 = 6.7 nM 8.17 Inhibition of P38 alpha MAPK (unknown origin) by ELISA 28834431

Literature References

PubMed DOI Target Context # Activities
28834431 10.1021/acs.jmedchem.7b00745 Liver 2
28834431 10.1021/acs.jmedchem.7b00745 Mitogen-activated protein kinase 14 2

Data from ChEMBL 36 via Core Engine