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Compound Detail

CHEMBL4475046

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COC(CNc1ncnc2c1ccn2[C@@H]1O[C@H]([C@H](O)c2ccc(Cl)cc2)[C@@H](O)[C@H]1O)OC

Basic Information

ChEMBL ID CHEMBL4475046
Phase Preclinical
Structure Type MOL
InChI Key SFXBSODSUAZMSY-NAIAOIPJSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

464.9
MW (Da)
1.47
ALogP
10
HBA
4
HBD
131.1
PSA (Ų)
0.37
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H25ClN4O6
MW 464.91
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness 0.17

Activity Summary

IC50 1 meas. best 6.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
PRMT5/MEP50 complex
CHEMBL3137261
IC50 6.75 6.75 177.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
PRMT5/MEP50 complex IC50 = 177.0 nM 6.75 Inhibition of human recombinant PRMT5/MEP50 expressed in baculovirus infected Hi... 31312404

Literature References

PubMed DOI Target Context # Activities
31312404 10.1021/acsmedchemlett.9b00074 PRMT5/MEP50 complex 1
31312404 10.1021/acsmedchemlett.9b00074 Protein arginine N-methyltransferase 5 1
31312404 10.1021/acsmedchemlett.9b00074 Granta-519 1

Data from ChEMBL 36 via Core Engine