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Compound Detail

CHEMBL203631

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CO[C@H]1CC[C@H](C(=O)Nc2cc(-c3ccnc(Nc4ccc(F)cc4)c3)ccn2)CC1

Basic Information

ChEMBL ID CHEMBL203631
Phase Preclinical
Structure Type MOL
InChI Key ACGBFWCBVIXTPZ-OQIWPSSASA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

420.5
MW (Da)
5.17
ALogP
5
HBA
2
HBD
76.1
PSA (Ų)
0.58
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H25FN4O2
MW 420.49
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.12

Activity Summary

IC50 2 meas. best 6.63

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 10
CHEMBL2637
IC50 6.63 6.63 235.0 1
Mitogen-activated protein kinase 8
CHEMBL2276
IC50 5.89 5.89 1280.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mitogen-activated protein kinase 10 IC50 = 235.0 nM 6.63 Inhibition of JNK3 16337120
Mitogen-activated protein kinase 8 IC50 = 1280.0 nM 5.89 Inhibition of JNK1 16337120

Literature References

PubMed DOI Target Context # Activities
16337120 10.1016/j.bmcl.2005.11.039 Mitogen-activated protein kinase 10 1
16337120 10.1016/j.bmcl.2005.11.039 Mitogen-activated protein kinase 8 1
16337120 10.1016/j.bmcl.2005.11.039 Mitogen-activated protein kinase 14 1

Data from ChEMBL 36 via Core Engine