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Compound Detail

CHEMBL5195936

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CC1(C)CC(Oc2ccc(-c3ccc(-c4ccnc(O)c4)cc3O)nn2)CC(C)(C)N1

Basic Information

ChEMBL ID CHEMBL5195936
Phase Preclinical
Structure Type MOL
InChI Key LBBBRWUUNXGXNH-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

420.5
MW (Da)
4.30
ALogP
7
HBA
3
HBD
100.4
PSA (Ų)
0.58
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H28N4O3
MW 420.51
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.46

Activity Summary

IC50 2 meas. best 7.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Huntingtin
CHEMBL5514
IC50 7.4 7.4 40.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Huntingtin IC50 = 40.0 nM 7.4 Inhibition of HTT (unknown origin) 35916496
Huntingtin IC50 = 40.0 nM 7.4 Inhibition of HTT (unknown origin) by HTS assay 36490325

Literature References

PubMed DOI Target Context # Activities
35916496 10.1021/acs.jmedchem.2c00875 Huntingtin 1
36490325 10.1021/acs.jmedchem.2c00799 Huntingtin 1

Data from ChEMBL 36 via Core Engine