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Compound Detail

CHEMBL4065116

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COc1cc(C#N)ccc1S(=O)(=O)Nc1ccc2c(c1)cc(C(C)C)c(=O)n2C

Basic Information

ChEMBL ID CHEMBL4065116
Phase Preclinical
Structure Type MOL
InChI Key WRCBUWZHGOJKHN-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

411.5
MW (Da)
3.34
ALogP
6
HBA
1
HBD
101.2
PSA (Ų)
0.69
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H21N3O4S
MW 411.48
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.53

Activity Summary

IC50 4 meas. best 6.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Peregrin
CHEMBL3132741
IC50 6.77 6.77 170.0 1
Bromodomain-containing protein 1
CHEMBL2176774
IC50 5.48 5.48 3300.0 1
Bromodomain and PHD finger-containing protein 3
CHEMBL3108644
IC50 5.34 5.34 4600.0 1
Bromodomain-containing protein 9
CHEMBL3108640
IC50 5.03 5.03 9300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28714688 10.1021/acs.jmedchem.7b00611 Bromodomain-containing protein 9 1
28714688 10.1021/acs.jmedchem.7b00611 Bromodomain and PHD finger-containing protein 3 1
28714688 10.1021/acs.jmedchem.7b00611 Bromodomain-containing protein 1 1
28714688 10.1021/acs.jmedchem.7b00611 Peregrin 1

Data from ChEMBL 36 via Core Engine