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Compound Detail

CHEMBL219682

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Cc1c(CNc2ccc3ncc(C#N)c(Nc4ccc(F)c(Cl)c4)c3c2)ncn1C

Basic Information

ChEMBL ID CHEMBL219682
Phase Preclinical
Structure Type MOL
InChI Key JYQVSVOKFMJLNQ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

420.9
MW (Da)
5.30
ALogP
6
HBA
2
HBD
78.6
PSA (Ų)
0.46
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H18ClFN6
MW 420.88
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.84

Activity Summary

IC50 1 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase kinase kinase 8
CHEMBL4899
IC50 8.52 8.52 3.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mitogen-activated protein kinase kinase kinase 8 IC50 = 3.0 nM 8.52 Inhibition of Tpl2 kinase by ELISA 16973359

Literature References

PubMed DOI Target Context # Activities
16973359 10.1016/j.bmcl.2006.08.102 Mitogen-activated protein kinase kinase kinase 8 1
16973359 10.1016/j.bmcl.2006.08.102 Monocyte 1
16973359 10.1016/j.bmcl.2006.08.102 Blood 1

Data from ChEMBL 36 via Core Engine