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Compound Detail

CHEMBL278935

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O=C(Nc1ccccc1C(=O)N[C@@H](Cc1ccccc1)C[C@H](O)[C@H](Cc1ccccc1)NC(=O)OCc1cncs1)OCc1ccccn1

Basic Information

ChEMBL ID CHEMBL278935
Phase Preclinical
Structure Type MOL
InChI Key WXJFTRVJBDTLCM-RQBSCEBTSA-N
2
Targets
2
Activities
2
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

679.8
MW (Da)
5.92
ALogP
9
HBA
4
HBD
151.8
PSA (Ų)
0.11
QED
2
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C37H37N5O6S
MW 679.80
Aromatic Rings 5
Heavy Atoms 49
NP-Likeness -0.60

Activity Summary

EC50 1 meas. best 6.7
Ki 1 meas. best 10.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 protease
CHEMBL243
Ki 10.52 10.52 0.0 1
CCRF-CEM
CHEMBL382
EC50 6.7 6.7 200.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 30.0 % Rattus norvegicus
T1/2 8.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9934467 10.1016/s0960-894x(98)00657-x Rattus norvegicus 2
9934467 10.1016/s0960-894x(98)00657-x Human immunodeficiency virus type 1 protease 1
9934467 10.1016/s0960-894x(98)00657-x CCRF-CEM 1
9934467 10.1016/s0960-894x(98)00657-x Unchecked 1

Data from ChEMBL 36 via Core Engine