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Compound Detail

CHEMBL4856376

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Cc1cc2c(C3CCOCC3)cnc(NC3CCN(CCCN)CC3)c2[nH]c1=O

Basic Information

ChEMBL ID CHEMBL4856376
Phase Preclinical
Structure Type MOL
InChI Key PYSGTFPWZDWYFN-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

399.5
MW (Da)
2.35
ALogP
6
HBA
3
HBD
96.3
PSA (Ų)
0.69
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 C22H33N5O2
MW 399.54
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -0.81

Activity Summary

IC50 3 meas. best 6.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Transcription initiation factor TFIID subunit 1
CHEMBL3217390
IC50 6.4 6.4 398.1 1
ATPase family AAA domain-containing protein 2
CHEMBL2150837
IC50 4.9 4.9 12589.2 1
Bromodomain-containing protein 4
CHEMBL1163125
IC50 4.8 4.8 15848.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34413961 10.1021/acsmedchemlett.1c00294 Unchecked 2
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

Data from ChEMBL 36 via Core Engine