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Compound Detail

CHEMBL4566599

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C=CCCn1cc(-c2cnc(OC)c(C(=O)N3CCOCC3)c2)c2cc[nH]c2c1=O

Basic Information

ChEMBL ID CHEMBL4566599
Phase Preclinical
Structure Type MOL
InChI Key IPQLFXYRKFCCRJ-UHFFFAOYSA-N
4
Targets
6
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

408.5
MW (Da)
2.45
ALogP
6
HBA
1
HBD
89.5
PSA (Ų)
0.63
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H24N4O4
MW 408.46
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.98

Activity Summary

IC50 6 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Transcription initiation factor TFIID subunit 1
CHEMBL3217390
IC50 8.15 6.655 7.0 2
Chromatin remodeling regulator CECR2
CHEMBL3108639
IC50 6.0 6.0 1000.0 1
Bromodomain-containing protein 9
CHEMBL3108640
IC50 5.77 5.77 1700.0 1
Bromodomain-containing protein 4
CHEMBL1163125
IC50 5.07 5.045 8600.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30289257 10.1021/acs.jmedchem.8b01225 Transcription initiation factor TFIID subunit 1 2
30289257 10.1021/acs.jmedchem.8b01225 Bromodomain-containing protein 4 2
30289257 10.1021/acs.jmedchem.8b01225 Bromodomain-containing protein 9 1
30289257 10.1021/acs.jmedchem.8b01225 Chromatin remodeling regulator CECR2 1

Data from ChEMBL 36 via Core Engine