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Compound Detail

CHEMBL4861244

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Cc1cc(/C=C/C#N)cc(C)c1Oc1nc(Nc2ccc(CC#N)cc2)nc2c1CCCC2

Basic Information

ChEMBL ID CHEMBL4861244
Phase Preclinical
Structure Type MOL
InChI Key OEHQJRHTJFMGGP-AATRIKPKSA-N
2
Targets
6
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

435.5
MW (Da)
6.11
ALogP
6
HBA
1
HBD
94.6
PSA (Ų)
0.47
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H25N5O
MW 435.53
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.74

Activity Summary

EC50 5 meas. best 7.89
IC50 1 meas. best 7.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus 1
CHEMBL378
EC50 7.89 7.232 12.9 5
Human immunodeficiency virus type 1 reverse transcriptase
CHEMBL247
IC50 7.31 7.31 49.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34496571 10.1021/acs.jmedchem.1c00987 Human immunodeficiency virus 1 8
34496571 10.1021/acs.jmedchem.1c00987 ADMET 2
34496571 10.1021/acs.jmedchem.1c00987 MT4 1
34496571 10.1021/acs.jmedchem.1c00987 Human immunodeficiency virus type 1 reverse transcriptase 1
34496571 10.1021/acs.jmedchem.1c00987 Human immunodeficiency virus 2 1

Data from ChEMBL 36 via Core Engine