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Compound Detail

CHEMBL1522313

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COc1ccccc1C(=O)Nc1cc2c(cc1N1CCCCC1)n(C)c(=O)n2C

Basic Information

ChEMBL ID CHEMBL1522313
Phase Preclinical
Structure Type MOL
InChI Key LTUGYAOMCKNTGG-UHFFFAOYSA-N
4
Targets
6
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

394.5
MW (Da)
3.13
ALogP
6
HBA
1
HBD
68.5
PSA (Ų)
0.74
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H26N4O3
MW 394.48
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.37

Activity Summary

IC50 6 meas. best 7.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.23 7.23 59.0 1
Peregrin
CHEMBL3132741
IC50 7.1 6.37 79.4 3
Bromodomain-containing protein 4
CHEMBL1163125
IC50 5.5 5.5 3162.3 1
Bromodomain-containing protein 1
CHEMBL2176774
IC50 5.1 5.1 7943.3 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25408830 10.1021/ml5002932 Peregrin 3
25408830 10.1021/ml5002932 Bromodomain-containing protein 4 2
- 10.6019/CHEMBL5724709 Fibroblast 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
32787077 10.1021/acs.jmedchem.0c01183 NAD-dependent protein deacylase sirtuin-6 2
- 10.6019/CHEMBL5724709 U2OS 2
- 10.6019/CHEMBL5724709 HEK-293T 2
37552884 10.1021/acs.jmedchem.3c00671 Unchecked 2
- 10.6019/CHEMBL5724796 Bromodomain-containing protein 4 1
- 10.6019/CHEMBL5724796 Glycogen synthase kinase-3 beta 1
- 10.6019/CHEMBL5724796 Cyclin-dependent kinase 2 1
- 10.6019/CHEMBL5724796 Casein kinase I isoform delta 1
37552884 10.1021/acs.jmedchem.3c00671 PC-3 1
37552884 10.1021/acs.jmedchem.3c00671 LNCaP 1
37552884 10.1021/acs.jmedchem.3c00671 Bromodomain-containing protein 9 1
37552884 10.1021/acs.jmedchem.3c00671 Bromodomain-containing protein 7 1
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1
25408830 10.1021/ml5002932 Bromodomain and PHD finger-containing protein 3 1
25408830 10.1021/ml5002932 Bromodomain-containing protein 1 1
25408830 10.1021/ml5002932 ADMET 1

Data from ChEMBL 36 via Core Engine