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Compound Detail

CHEMBL4086958

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Cc1cc2c(cc1N1C(=O)c3cccc4c(Br)ccc(c34)C1=O)n(C)c(=O)n2C

Basic Information

ChEMBL ID CHEMBL4086958
Phase Preclinical
Structure Type MOL
InChI Key YDDKRKCQSIKAJD-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

450.3
MW (Da)
3.90
ALogP
5
HBA
0
HBD
64.3
PSA (Ų)
0.41
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H16BrN3O3
MW 450.29
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -0.99

Activity Summary

IC50 3 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Transcription initiation factor TFIID subunit 1
CHEMBL3217390
IC50 8.4 8.4 4.0 1
Bromodomain-containing protein 1
CHEMBL2176774
IC50 7.29 7.29 51.0 1
Peregrin
CHEMBL3132741
IC50 6.23 6.23 591.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28402630 10.1021/acs.jmedchem.7b00306 Bromodomain-containing protein 4 2
28402630 10.1021/acs.jmedchem.7b00306 Transcription initiation factor TFIID subunit 1 1
28402630 10.1021/acs.jmedchem.7b00306 Bromodomain-containing protein 1 1
28402630 10.1021/acs.jmedchem.7b00306 Peregrin 1

Data from ChEMBL 36 via Core Engine