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Compound Detail

CHEMBL224516

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CCC1(c2ccc(CNc3ccccc3)cc2)Oc2ccccc2-n2cccc2C1=O

Basic Information

ChEMBL ID CHEMBL224516
Phase Preclinical
Structure Type MOL
InChI Key JNJMKXNEZVZYHV-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

408.5
MW (Da)
5.97
ALogP
4
HBA
1
HBD
43.3
PSA (Ų)
0.44
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H24N2O2
MW 408.50
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -0.49

Activity Summary

IC50 3 meas. best 7.05
EC50 1 meas. best 6.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.05 7.05 90.0 1
Human immunodeficiency virus 1
CHEMBL378
EC50 6.12 6.12 750.0 1
Human immunodeficiency virus type 1 reverse transcriptase
CHEMBL247
IC50 5.92 5.76 1200.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16279773 10.1021/jm050257d Human immunodeficiency virus type 1 reverse transcriptase 5
16279773 10.1021/jm050257d Unchecked 2
16279773 10.1021/jm050257d C8166 1
16279773 10.1021/jm050257d Human immunodeficiency virus 1 1
16279773 10.1021/jm050257d NSO 1
16279773 10.1021/jm050257d Daudi 1
16279773 10.1021/jm050257d NIH3T3 1
16279773 10.1021/jm050257d ADMET 1

Data from ChEMBL 36 via Core Engine