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Compound Detail

CHEMBL5409404

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CC(C)[C@H]1CCCN1c1cc(-c2ccccc2O)nnc1N

Basic Information

ChEMBL ID CHEMBL5409404
Phase Preclinical
Structure Type MOL
InChI Key FQZVWWGALUEODH-CQSZACIVSA-N
4
Targets
5
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

298.4
MW (Da)
3.06
ALogP
5
HBA
2
HBD
75.3
PSA (Ų)
0.91
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H22N4O
MW 298.39
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness 0.04

Activity Summary

Kd 4 meas. best 8.22
EC50 1 meas. best 6.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein polybromo-1
CHEMBL1795184
Kd 8.22 7.97 6.0 2
Probable global transcription activator SNF2L2
CHEMBL2362979
Kd 7.89 7.89 13.0 1
Transcription activator BRG1
CHEMBL3085620
Kd 7.7 7.7 20.0 1
Nuclear receptor subfamily 1 group I member 2
CHEMBL3401
EC50 6.85 6.85 140.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
37702400 10.1021/acs.jmedchem.3c01149 Protein polybromo-1 2
37702400 10.1021/acs.jmedchem.3c01149 Probable global transcription activator SNF2L2 1
37702400 10.1021/acs.jmedchem.3c01149 Transcription activator BRG1 1
37702400 10.1021/acs.jmedchem.3c01149 Nuclear receptor subfamily 1 group I member 2 1
37702400 10.1021/acs.jmedchem.3c01149 Oxysterols receptor LXR-alpha 1
37702400 10.1021/acs.jmedchem.3c01149 Oxysterols receptor LXR-beta 1

Data from ChEMBL 36 via Core Engine