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Compound Detail

CHEMBL5425250

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

Basic Information

ChEMBL ID CHEMBL5425250
Phase Preclinical
Structure Type MOL
InChI Key CMJYPZQQLQOFCI-SNVBAGLBSA-N
4
Targets
5
Activities
2
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

270.3
MW (Da)
2.42
ALogP
5
HBA
2
HBD
75.3
PSA (Ų)
0.88
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H18N4O
MW 270.34
Aromatic Rings 2
Heavy Atoms 20
NP-Likeness -0.42

Activity Summary

Kd 4 meas. best 7.5
IC50 1 meas. best 5.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Probable global transcription activator SNF2L2
CHEMBL2362979
Kd 7.5 7.5 32.0 1
Transcription activator BRG1
CHEMBL3085620
Kd 7.48 7.48 33.0 1
Protein polybromo-1
CHEMBL1795184
Kd 7.28 6.875 53.0 2
Nuclear receptor subfamily 1 group I member 2
CHEMBL3401
IC50 5.37 5.37 4300.0 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
37702400 10.1021/acs.jmedchem.3c01149 Retinoic acid receptor RXR-alpha 1
37702400 10.1021/acs.jmedchem.3c01149 Peroxisome proliferator-activated receptor delta 1
37702400 10.1021/acs.jmedchem.3c01149 Peroxisome proliferator-activated receptor gamma 1
37702400 10.1021/acs.jmedchem.3c01149 Retinoic acid receptor alpha 1

Data from ChEMBL 36 via Core Engine