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Compound Detail

CHEMBL428685

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COC(=O)CCCC=C(c1cc(C)c(OC)c(C(=O)OC)c1)c1cc(C)c(OC)c(C(=O)OC)c1

Basic Information

ChEMBL ID CHEMBL428685
Phase Preclinical
Structure Type MOL
InChI Key NAAQTQYXSPNHPJ-UHFFFAOYSA-N
3
Targets
5
Activities
2
Assay Types
2
PK Parameters
13
Publications
0
Known Names

Molecular Properties

484.6
MW (Da)
4.67
ALogP
8
HBA
0
HBD
97.4
PSA (Ų)
0.27
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H32O8
MW 484.55
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness 0.23

Activity Summary

EC50 4 meas. best 6.6
IC50 1 meas. best 6.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus 1
CHEMBL378
EC50 6.6 6.2 250.0 3
Human immunodeficiency virus type 1 (RF/HAT ISOLATE)
CHEMBL613498
EC50 6.6 6.6 250.0 1
Human immunodeficiency virus type 1 reverse transcriptase
CHEMBL247
IC50 6.0 6.0 1000.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.715 hr Rattus norvegicus
T1/2 0.01267 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11708913 10.1021/jm010212m CEM-SS 2
17579385 10.1021/jm070236e Human immunodeficiency virus 1 2
11708913 10.1021/jm010212m Human immunodeficiency virus type 1 reverse transcriptase 1
11708913 10.1021/jm010212m Human immunodeficiency virus type 1 (RF/HAT ISOLATE) 1
15163195 10.1021/jm049916x Human immunodeficiency virus 1 1
15163195 10.1021/jm049916x Human immunodeficiency virus 2 1
15163195 10.1021/jm049916x MT4 1
15163195 10.1021/jm049916x Rattus norvegicus 1
17579385 10.1021/jm070236e Human immunodeficiency virus type 1 reverse transcriptase 1
17579385 10.1021/jm070236e Human immunodeficiency virus 2 1
17579385 10.1021/jm070236e CEM-SS 1
17579385 10.1021/jm070236e MT4 1
17579385 10.1021/jm070236e Plasma 1

Data from ChEMBL 36 via Core Engine