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Compound Detail

CHEMBL2087515

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Cc1c(F)cc(C(=O)NC2CC2)cc1-c1ccn2c(-c3ccncc3Cl)nnc2c1

Basic Information

ChEMBL ID CHEMBL2087515
Phase Preclinical
Structure Type MOL
InChI Key NZCDHWXRRMMWDP-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

421.9
MW (Da)
4.45
ALogP
5
HBA
1
HBD
72.2
PSA (Ų)
0.53
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H17ClFN5O
MW 421.86
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.55

Activity Summary

IC50 2 meas. best 9.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 13
CHEMBL2939
IC50 9.08 9.08 0.8 1
Blood
CHEMBL613416
IC50 7.08 7.08 84.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mitogen-activated protein kinase 13 IC50 = 0.83 nM 9.08 Inhibition of p38alpha 22521646
Blood IC50 = 84.0 nM 7.08 Inhibition of LPS-induced TNFalpha production in human whole blood 22521646

Literature References

PubMed DOI Target Context # Activities
22521646 10.1016/j.bmcl.2012.03.099 Mitogen-activated protein kinase 13 1
22521646 10.1016/j.bmcl.2012.03.099 Blood 1

Data from ChEMBL 36 via Core Engine