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Compound Detail

CHEMBL7264

ATEVIRDINE SULPHATE
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CCNc1cccnc1N1CCN(C(=O)c2cc3cc(OC)ccc3[nH]2)CC1.CS(=O)(=O)O

Basic Information

ChEMBL ID CHEMBL7264
Name ATEVIRDINE SULPHATE
Phase Preclinical
Structure Type MOL
InChI Key HKPKBPALSLUFFM-UHFFFAOYSA-N
Parent Compound CHEMBL280527
Active Moiety CHEMBL280527
1
Targets
3
Activities
1
Assay Types
14
PK Parameters
13
Publications
0
Known Names

Molecular Properties

379.5
MW (Da)
2.97
ALogP
5
HBA
2
HBD
73.5
PSA (Ų)
0.71
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H29N5O5S
MW 475.57
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.50

Activity Summary

IC50 3 meas. best 5.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 reverse transcriptase
CHEMBL247
IC50 5.64 5.52 2300.0 3

Pharmacokinetic Data

Parameter Value Units Species
CL 13.0 mL.min-1.kg-1 Rattus norvegicus
Cmax 16000.0 nM Canis lupus familiaris
Cmax 4600.0 nM Rattus norvegicus
Cmax 4600.0 nM Rattus norvegicus
Cmax 16000.0 nM Canis lupus familiaris
F 50.0 % Canis lupus familiaris
F 62.0 % Rattus norvegicus
F 75.0 % Rattus norvegicus
F 62.0 % Rattus norvegicus
F 50.0 % Canis lupus familiaris
Tmax 1.0 hr Canis lupus familiaris
Tmax 0.5 hr Rattus norvegicus
Tmax 0.5 hr Rattus norvegicus
Tmax 1.0 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30516990 10.1021/acs.jmedchem.8b00843 ADMET 6
7512142 10.1021/jm00033a018 Rattus norvegicus 4
7512142 10.1021/jm00033a018 Canis familiaris 3
8809165 10.1021/jm960158n Human immunodeficiency virus type 1 reverse transcriptase 3
7512142 10.1021/jm00033a018 MT2 2
7512142 10.1021/jm00033a018 Unchecked 2
8809165 10.1021/jm960158n Rattus norvegicus 2
- 10.1016/0960-894X(95)00311-G Human immunodeficiency virus type 1 reverse transcriptase 2
7512142 10.1021/jm00033a018 Human immunodeficiency virus type 1 reverse transcriptase 1
7512142 10.1021/jm00033a018 Human immunodeficiency virus 1 1
- 10.1016/0960-894X(95)00311-G Human immunodeficiency virus 1 1
30516990 10.1021/acs.jmedchem.8b00843 Human immunodeficiency virus type 1 reverse transcriptase 1
30516990 10.1021/acs.jmedchem.8b00843 No relevant target 1

Data from ChEMBL 36 via Core Engine