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Compound Detail

CHEMBL2165299

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Cc1cc(CCC#N)cc(C)c1Oc1cc(Nc2ccc(C#N)cc2)c(N)cc1CO

Basic Information

ChEMBL ID CHEMBL2165299
Phase Preclinical
Structure Type MOL
InChI Key KUSZBGKKJFSGBE-UHFFFAOYSA-N
1
Targets
4
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

412.5
MW (Da)
5.24
ALogP
6
HBA
3
HBD
115.1
PSA (Ų)
0.46
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H24N4O2
MW 412.49
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.50

Activity Summary

EC50 4 meas. best 9.41

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus 1
CHEMBL378
EC50 9.41 8.79 0.4 4

Pharmacokinetic Data

Parameter Value Units Species
CL 330.0 mL.min-1.g-1 Homo sapiens
T1/2 0.3483 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22856541 10.1021/jm3007678 Human immunodeficiency virus 1 7
22856541 10.1021/jm3007678 No relevant target 3
22856541 10.1021/jm3007678 Liver microsomes 2
22856541 10.1021/jm3007678 Unchecked 1
22856541 10.1021/jm3007678 ADMET 1

Data from ChEMBL 36 via Core Engine