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Compound Detail

CHEMBL4084253

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CN1C[C@H](Nc2cnn(C)c(=O)c2Cl)C[C@H](c2ccccc2)C1

Basic Information

ChEMBL ID CHEMBL4084253
Phase Preclinical
Structure Type MOL
InChI Key ZJYJXUJUQQPMJB-UONOGXRCSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

332.8
MW (Da)
2.33
ALogP
5
HBA
1
HBD
50.2
PSA (Ų)
0.94
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H21ClN4O
MW 332.84
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness -0.99

Activity Summary

IC50 2 meas. best 7.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone acetyltransferase KAT2B
CHEMBL5500
IC50 7.1 7.1 79.4 1
Bromodomain-containing protein 9
CHEMBL3108640
IC50 4.5 4.5 31622.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28002667 10.1021/acs.jmedchem.6b01566 No relevant target 1
28002667 10.1021/acs.jmedchem.6b01566 Histone acetyltransferase KAT2B 1
28002667 10.1021/acs.jmedchem.6b01566 Bromodomain-containing protein 4 1
28002667 10.1021/acs.jmedchem.6b01566 Bromodomain-containing protein 9 1

Data from ChEMBL 36 via Core Engine