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Compound Detail

CHEMBL4862754

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Cc1cc2c(C3=CCOCC3)cnc(NC3CCN(CCC(N)=O)CC3)c2[nH]c1=O

Basic Information

ChEMBL ID CHEMBL4862754
Phase Preclinical
Structure Type MOL
InChI Key MFZXSNYAQBIVDS-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

411.5
MW (Da)
1.79
ALogP
6
HBA
3
HBD
113.3
PSA (Ų)
0.67
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 C22H29N5O3
MW 411.51
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -0.76

Activity Summary

IC50 1 meas. best 5.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bromodomain-containing protein 4
CHEMBL1163125
IC50 5.2 5.2 6309.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Bromodomain-containing protein 4 IC50 = 6309.57 nM 5.2 Inhibition of BRD4 BD1 (unknown origin) by TR-FRET assay 34413961

Literature References

PubMed DOI Target Context # Activities
34413961 10.1021/acsmedchemlett.1c00294 No relevant target 2
34413961 10.1021/acsmedchemlett.1c00294 Transcription initiation factor TFIID subunit 1 1
34413961 10.1021/acsmedchemlett.1c00294 Bromodomain-containing protein 4 1
34413961 10.1021/acsmedchemlett.1c00294 ATPase family AAA domain-containing protein 2 1
34413961 10.1021/acsmedchemlett.1c00294 ADMET 1
34413961 10.1021/acsmedchemlett.1c00294 Unchecked 1

Data from ChEMBL 36 via Core Engine