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Compound Detail

CHEMBL467894

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CCN1/C(=C/C=C/C2=[N+](CC)c3ccccc3C2(C)C)C(C)(C)c2ccccc21.[I-]

Basic Information

ChEMBL ID CHEMBL467894
Phase Preclinical
Structure Type MOL
InChI Key LGRNGKUSEZTBMB-UHFFFAOYSA-M
Parent Compound CHEMBL1186511
Active Moiety CHEMBL1186511
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

385.6
MW (Da)
6.34
ALogP
1
HBA
0
HBD
6.2
PSA (Ų)
0.56
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H33IN2
MW 512.48
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -0.07

Activity Summary

IC50 2 meas. best 6.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.01 6.01 980.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 980.0 nM 6.01 Inhibition of His-tagged human recombinant 2N4R tau protein aggregation assessed... 19432420

Literature References

PubMed DOI Target Context # Activities
25559100 10.1021/jm501452j Protein arginine N-methyltransferase 1 3
19432420 10.1021/jm900116d Unchecked 1
22749641 10.1016/j.ejmech.2012.06.017 Protein arginine N-methyltransferase 1 1

Data from ChEMBL 36 via Core Engine