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Compound Detail

CHEMBL4648548

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Cc1c(NCc2ccccc2N2CCN(C)CC2)cnn(C)c1=O

Basic Information

ChEMBL ID CHEMBL4648548
Phase Preclinical
Structure Type MOL
InChI Key HONYBLSJNSYWKQ-UHFFFAOYSA-N
4
Targets
5
Activities
2
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

327.4
MW (Da)
1.45
ALogP
6
HBA
1
HBD
53.4
PSA (Ų)
0.92
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H25N5O
MW 327.43
Aromatic Rings 2
Heavy Atoms 24
NP-Likeness -1.60

Activity Summary

Ki 4 meas. best 7.6
IC50 1 meas. best 6.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bromodomain-containing protein 7
CHEMBL3085622
Ki 7.6 7.6 25.1 1
Bromodomain-containing protein 9
CHEMBL3108640
Ki 7.4 7.4 39.8 1
Bromodomain-containing protein 9
CHEMBL3108640
IC50 6.7 6.7 199.5 1
Peregrin
CHEMBL3132741
Ki 6.6 6.6 251.2 1
Bromodomain-containing protein 4
CHEMBL1163125
Ki 4.6 4.6 25118.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32410449 10.1021/acs.jmedchem.0c00075 Bromodomain-containing protein 9 3
32410449 10.1021/acs.jmedchem.0c00075 Unchecked 3
32410449 10.1021/acs.jmedchem.0c00075 No relevant target 3
32410449 10.1021/acs.jmedchem.0c00075 Bromodomain-containing protein 4 2
32410449 10.1021/acs.jmedchem.0c00075 Bromodomain-containing protein 7 2
32410449 10.1021/acs.jmedchem.0c00075 Peregrin 1
32410449 10.1021/acs.jmedchem.0c00075 Transcription initiation factor TFIID subunit 1 1
32410449 10.1021/acs.jmedchem.0c00075 B-cell CLL/lymphoma 7 protein family member A 1
32410449 10.1021/acs.jmedchem.0c00075 B-cell CLL/lymphoma 7 protein family member B 1
32410449 10.1021/acs.jmedchem.0c00075 Protein polybromo-1 1
32410449 10.1021/acs.jmedchem.0c00075 Probable global transcription activator SNF2L2 1
32410449 10.1021/acs.jmedchem.0c00075 Transcription activator BRG1 1

Data from ChEMBL 36 via Core Engine