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Compound Detail

CHEMBL4460783

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C=CCn1cc(-c2cccc(C(=O)N(C)C)c2)c2cc[nH]c2c1=O

Basic Information

ChEMBL ID CHEMBL4460783
Phase Preclinical
Structure Type MOL
InChI Key SPSRAFOXVSNAJA-UHFFFAOYSA-N
4
Targets
6
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

321.4
MW (Da)
2.88
ALogP
3
HBA
1
HBD
58.1
PSA (Ų)
0.75
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 C19H19N3O2
MW 321.38
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.06

Activity Summary

IC50 6 meas. best 6.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Chromatin remodeling regulator CECR2
CHEMBL3108639
IC50 6.77 6.77 170.0 1
Bromodomain-containing protein 9
CHEMBL3108640
IC50 6.54 6.54 290.0 1
Transcription initiation factor TFIID subunit 1
CHEMBL3217390
IC50 6.41 6.26 390.0 2
Bromodomain-containing protein 4
CHEMBL1163125
IC50 5.82 5.51 1500.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27219867 10.1021/acs.jmedchem.6b00264 Unchecked 6
27219867 10.1021/acs.jmedchem.6b00264 Chromatin remodeling regulator CECR2 5
27219867 10.1021/acs.jmedchem.6b00264 Transcription initiation factor TFIID subunit 1 2
27219867 10.1021/acs.jmedchem.6b00264 Bromodomain-containing protein 4 2
27219867 10.1021/acs.jmedchem.6b00264 Bromodomain-containing protein 9 1
27219867 10.1021/acs.jmedchem.6b00264 Peregrin 1
27219867 10.1021/acs.jmedchem.6b00264 CREB-binding protein 1

Data from ChEMBL 36 via Core Engine