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Compound Detail

CHEMBL4790365

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Nc1nnc(-c2ccccc2O)cc1N1CCC[C@@H](O)C1

Basic Information

ChEMBL ID CHEMBL4790365
Phase Preclinical
Structure Type MOL
InChI Key VUGYKDOKOLKKRA-SNVBAGLBSA-N
3
Targets
6
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

286.3
MW (Da)
1.39
ALogP
6
HBA
3
HBD
95.5
PSA (Ų)
0.77
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H18N4O2
MW 286.33
Aromatic Rings 2
Heavy Atoms 21
NP-Likeness -0.40

Activity Summary

Kd 6 meas. best 7.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Probable global transcription activator SNF2L2
CHEMBL2362979
Kd 7.15 7.15 71.0 1
Transcription activator BRG1
CHEMBL3085620
Kd 7.0 7.0 100.0 1
Protein polybromo-1
CHEMBL1795184
Kd 6.62 6.3025 238.0 4

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33216538 10.1021/acs.jmedchem.0c01242 Protein polybromo-1 10
33216538 10.1021/acs.jmedchem.0c01242 MDA-MB-231 2
33216538 10.1021/acs.jmedchem.0c01242 MCF7 2
33216538 10.1021/acs.jmedchem.0c01242 HT-29 2
33216538 10.1021/acs.jmedchem.0c01242 HCT-116 2
33216538 10.1021/acs.jmedchem.0c01242 Transcription activator BRG1 2
33216538 10.1021/acs.jmedchem.0c01242 Probable global transcription activator SNF2L2 2
33216538 10.1021/acs.jmedchem.0c01242 Unchecked 1
33216538 10.1021/acs.jmedchem.0c01242 Panel NCI-60 (60 carcinoma cell lines) 1

Data from ChEMBL 36 via Core Engine