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Compound Detail

CHEMBL3585461

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Cc1cc2c(-c3cncc(COC(N)=O)c3)cnc(NC3CCNCC3)c2[nH]c1=O

Basic Information

ChEMBL ID CHEMBL3585461
Phase Preclinical
Structure Type MOL
InChI Key MUEIFQPTBPDFDJ-UHFFFAOYSA-N
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

408.5
MW (Da)
2.05
ALogP
7
HBA
4
HBD
135.0
PSA (Ų)
0.51
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 C21H24N6O3
MW 408.46
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.44

Activity Summary

IC50 5 meas. best 6.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Transcription initiation factor TFIID subunit 1
CHEMBL3217390
IC50 6.8 6.8 158.5 1
Bromodomain-containing protein 4
CHEMBL1163125
IC50 5.9 5.9 1258.9 2
ATPase family AAA domain-containing protein 2
CHEMBL2150837
IC50 5.8 5.8 1584.9 2

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
26155854 10.1021/acs.jmedchem.5b00772 ATPase family AAA domain-containing protein 2 1
26155854 10.1021/acs.jmedchem.5b00772 Bromodomain-containing protein 4 1
26155854 10.1021/acs.jmedchem.5b00772 No relevant target 1
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