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Compound Detail

CHEMBL298817

ALBACONAZOLE
🧪 Phase II
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🧪 Phase II
C[C@@H](n1cnc2cc(Cl)ccc2c1=O)[C@](O)(Cn1cncn1)c1ccc(F)cc1F

Basic Information

ChEMBL ID CHEMBL298817
Name ALBACONAZOLE
Phase Phase II
Structure Type MOL
InChI Key UHIXWHUVLCAJQL-MPBGBICISA-N

Known Names

Albaconazol Albaconazole UR-9825 W-0027 W0027
7
Targets
7
Activities
1
Assay Types
1
PK Parameters
20
Publications
5
Known Names
3
Indications
1
Mechanisms

Molecular Properties

431.8
MW (Da)
3.07
ALogP
7
HBA
1
HBD
85.8
PSA (Ų)
0.52
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer
USAN Stem -conazole
USAN Year 2008

Extended Properties

Molecular Formula C20H16ClF2N5O2
MW 431.83
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.30

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Lanosterol 14-alpha demethylase inhibitor INHIBITOR Lanosterol 14-alpha demethylase

Indications

Onychomycosis Vulvovaginitis Tinea Pedis

Activity Summary

IC50 7 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sterol 14-alpha demethylase
CHEMBL1075110
IC50 9.0 9.0 1.0 1
Cytochrome P450 3A4
CHEMBL340
IC50 7.4 7.4 40.0 1
Cytochrome P450 2C9
CHEMBL3397
IC50 4.98 4.98 10400.0 1
Cytochrome P450 2C19
CHEMBL3622
IC50 4.89 4.89 13000.0 1
Cytochrome P450 2D6
CHEMBL289
IC50 4.5 4.5 31700.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 4.46 4.46 34860.0 1
Cytochrome P450 1A2
CHEMBL3356
IC50 4.22 4.22 60300.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 2.9 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19635949 10.1128/aac.00565-09 Candida albicans 17
9599237 10.1021/jm9707277 Mus musculus 7
24564525 10.1021/jm4016284 Candida albicans 7
9599237 10.1021/jm9707277 Oryctolagus cuniculus 6
38598688 10.1021/acs.jmedchem.3c02188 [Candida] auris 6
24900660 10.1021/ml300429p Aspergillus fumigatus 6
9599237 10.1021/jm9707277 Rattus norvegicus 5
9599237 10.1021/jm9707277 Candida albicans 4
9599237 10.1021/jm9707277 NON-PROTEIN TARGET 4
18039919 10.1128/aac.01012-07 Sporothrix 4
38598688 10.1021/acs.jmedchem.3c02188 Candida albicans 4
31926784 10.1016/j.bmcl.2020.126951 Candida albicans 4
24900660 10.1021/ml300429p Candida albicans 4
18039919 10.1128/aac.01012-07 Sporothrix albicans 3
18039919 10.1128/aac.01012-07 Sporothrix globosa 3
18039919 10.1128/aac.01012-07 Sporothrix schenckii 3
18391027 10.1128/aac.00176-08 Fusarium verticillioides 3
24900660 10.1021/ml300429p Molecular identity unknown 3
24564525 10.1021/jm4016284 No relevant target 2
26310892 10.1016/j.ejmech.2015.08.023 Candida albicans 2

Data from ChEMBL 36 via Core Engine