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Compound Detail

CHEMBL2236589

20, RDS-2163
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CCOC(=O)/C(O)=C/C(=O)c1cn(Cc2ccccc2OC)c2ccccc2c1=O

Basic Information

ChEMBL ID CHEMBL2236589
Name 20, RDS-2163
Phase Preclinical
Structure Type MOL
InChI Key LEPPLGGMAAQLEL-NDENLUEZSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

407.4
MW (Da)
3.25
ALogP
7
HBA
1
HBD
94.8
PSA (Ų)
0.28
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H21NO6
MW 407.42
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.58

Activity Summary

IC50 2 meas. best 5.85
EC50 1 meas. best 5.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 integrase
CHEMBL3471
IC50 5.85 5.85 1400.0 1
Human immunodeficiency virus 1
CHEMBL378
EC50 5.58 5.58 2600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25961960 10.1021/acs.jmedchem.5b00159 Human immunodeficiency virus type 1 integrase 2
- 10.1007/s00044-011-9593-5 Human immunodeficiency virus type 1 integrase 1
25961960 10.1021/acs.jmedchem.5b00159 Human immunodeficiency virus type 1 reverse transcriptase 1
25961960 10.1021/acs.jmedchem.5b00159 Human immunodeficiency virus 1 1
25961960 10.1021/acs.jmedchem.5b00159 HeLa 1
25961960 10.1021/acs.jmedchem.5b00159 Unchecked 1

Data from ChEMBL 36 via Core Engine