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Compound Detail

CHEMBL2364626

RALIMETINIB
🧪 Phase II
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🧪 Phase II
CC(C)(C)Cn1c(N)nc2ccc(-c3[nH]c(C(C)(C)C)nc3-c3ccc(F)cc3)nc21

Basic Information

ChEMBL ID CHEMBL2364626
Name RALIMETINIB
Phase Phase II
Structure Type MOL
InChI Key XPPBBJCBDOEXDN-UHFFFAOYSA-N

Known Names

LSN-2322600 FREE BASE LSN2322600 FREE BASE Ly-2228820 LY2228820 LY22288220 Ralimetinib
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
6
Known Names
5
Indications
1
Mechanisms

Molecular Properties

420.5
MW (Da)
5.55
ALogP
5
HBA
2
HBD
85.4
PSA (Ų)
0.45
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Achiral
USAN Stem -tinib
USAN Year 2013

Extended Properties

Molecular Formula C24H29FN6
MW 420.54
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -1.14

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
MAP kinase p38 alpha inhibitor INHIBITOR Mitogen-activated protein kinase 14

Indications

Breast Neoplasms Fallopian Tube Neoplasms Glioblastoma Neoplasms Ovarian Neoplasms

Activity Summary

IC50 1 meas. best 6.06

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Middle East respiratory syndrome-related coronavirus
CHEMBL4296578
IC50 6.06 6.06 873.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Middle East respiratory syndrome-related coronavirus IC50 = 873.0 nM 6.06 Antiviral activity against MERS-CoV 34081439

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
- 10.6019/CHEMBL4651402 SARS-CoV-2 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1
34081439 10.1021/acs.jmedchem.1c00335 Middle East respiratory syndrome-related coronavirus 1

Data from ChEMBL 36 via Core Engine