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Compound Detail

CHEMBL4441150

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Cc1nc(C(=O)N[C@H]2CC[C@H](O)CC2)c(C)c(-c2ccc(Cl)cc2)c1[C@H](OC(C)(C)C)C(=O)O

Basic Information

ChEMBL ID CHEMBL4441150
Phase Preclinical
Structure Type MOL
InChI Key OGDSMJIMRNCQEM-YDHSSHFGSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

489.0
MW (Da)
4.99
ALogP
5
HBA
3
HBD
108.8
PSA (Ų)
0.53
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H33ClN2O5
MW 489.01
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -0.37

Activity Summary

EC50 1 meas. best 6.03

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
EC50 6.03 6.03 930.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 5.0 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked EC50 = 930.0 nM 6.03 Inhibition of HIV NL4.3 integrase T124/T125 double mutant assessed as reduction ... 27563405

Literature References

PubMed DOI Target Context # Activities
27563405 10.1021/acsmedchemlett.6b00194 ADMET 1
27563405 10.1021/acsmedchemlett.6b00194 Unchecked 1

Data from ChEMBL 36 via Core Engine