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Compound Detail

CHEMBL190279

ALFAXALONE
🧪 Phase II
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🧪 Phase II
CC(=O)[C@H]1CC[C@H]2[C@@H]3CC[C@H]4C[C@H](O)CC[C@]4(C)[C@H]3C(=O)C[C@]12C

Basic Information

ChEMBL ID CHEMBL190279
Name ALFAXALONE
Phase Phase II
Structure Type MOL
InChI Key DUHUCHOQIDJXAT-OLVMNOGESA-N

Known Names

Alfaxalona Alfaxalone Alphaxolone GR 2/234 GR-2/234 Phaxan
7
Targets
14
Activities
2
Assay Types
0
PK Parameters
20
Publications
6
Known Names

Molecular Properties

332.5
MW (Da)
3.77
ALogP
3
HBA
1
HBD
54.4
PSA (Ų)
0.79
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer

Flags

Natural Product

Extended Properties

Molecular Formula C21H32O3
MW 332.48
Aromatic Rings 0
Heavy Atoms 24
NP-Likeness 2.36

ATC Classification

N01AX05
alfaxalone
Level 1: NERVOUS SYSTEM
Level 2: ANESTHETICS

Activity Summary

EC50 8 meas. best 6.35
IC50 6 meas. best 6.65

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.65 5.59 226.0 3
GABA-A receptor; anion channel
CHEMBL1907607
IC50 6.52 6.3867 300.0 3
GABA-A receptor; alpha-1/beta-3/gamma-2
CHEMBL2094121
EC50 6.35 6.35 450.0 1
GABA-A receptor; alpha-1/beta-2/gamma-2
CHEMBL2095172
EC50 6.3 5.98 500.0 2
Xenopus laevis
CHEMBL613478
EC50 5.95 5.605 1120.0 2
Anura
CHEMBL613477
EC50 5.72 5.72 1900.0 1
GABA A receptor alpha-2/beta-2/gamma-2
CHEMBL2111413
EC50 5.7 5.7 2000.0 1
Unchecked
CHEMBL612545
EC50 5.34 5.34 4600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 226.0 nM 6.65 Displacement of [35S]TBPS from GABA-A receptor picrotoxin binding site in rat br... 20875742
GABA-A receptor; anion channel IC50 = 300.0 nM 6.52 Inhibition of [35S]TBPS binding to GABA-A receptor in rat cerebral cortex. 9599235
GABA-A receptor; anion channel IC50 = 423.0 nM 6.37 Inhibition of binding of tert-butyl bicyclophosphorothionate ([35 S]TBPS) at Gam... 11063608
GABA-A receptor; alpha-1/beta-3/gamma-2 EC50 = 450.0 nM 6.35 Displacement of [3H]muscimol from human GABAA receptor alpha1beta3gamma2 express... 28505538
GABA-A receptor; alpha-1/beta-2/gamma-2 EC50 = 500.0 nM 6.3 Positive allosteric modulation of human GABAA receptor alpha1beta2gamma2L expres... 28505538
GABA-A receptor; anion channel IC50 = 538.0 nM 6.27 The concentration required to inhibit 50% of binding of [35S]TBPS to Gamma-amino... 9171876
Unchecked IC50 = 900.0 nM 6.05 Displacement of [3H]ethynylpropylbicycloorthobenzoate from GABAA receptor from r... 19497738
Xenopus laevis EC50 = 1120.0 nM 5.95 Anesthetic effect on prelimb-bud stage of Xenopus laevis tadpole assessed as los... 20875742
Anura EC50 = 1900.0 nM 5.72 Anesthetic activity in tadpole assessed as loss of righting reflexes 28505538
GABA A receptor alpha-2/beta-2/gamma-2 EC50 = 2000.0 nM 5.7 Effective concentration against GABA-evoked chloride currents mediated by human ... 15801854
GABA-A receptor; alpha-1/beta-2/gamma-2 EC50 = 2200.0 nM 5.66 Positive allosteric modulation of human GABAA receptor alpha1beta2gamma2L expres... 28505538
Unchecked EC50 = 4600.0 nM 5.34 Stimulation of [3H]flunitrazepam binding to GABA type A receptor in mouse primar... 23421641
Xenopus laevis EC50 = 5480.0 nM 5.26 Anesthetic effect on prelimb-bud stage of Xenopus laevis tadpole assessed as los... 20875742
Unchecked IC50 = 86000.0 nM 4.07 Displacement of [3H]ethynylpropylbicycloorthobenzoate from GABA receptor from ra... 19497738

Literature References

PubMed DOI Target Context # Activities
20875742 10.1016/j.bmcl.2010.09.008 Unchecked 6
28505538 10.1016/j.ejmech.2017.04.043 GABA-A receptor; alpha-1/beta-3/gamma-2 5
24328079 10.1021/jm401577c Mus musculus 5
20875742 10.1016/j.bmcl.2010.09.008 Xenopus laevis 4
21504158 10.1021/jm2002487 Mus musculus 4
28505538 10.1016/j.ejmech.2017.04.043 GABA-A receptor; alpha-1/beta-2/gamma-2 3
19497738 10.1016/j.bmcl.2009.05.065 Unchecked 3
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
- 10.6019/CHEMBL4651402 SARS-CoV-2 2
28505538 10.1016/j.ejmech.2017.04.043 Anura 2
23421641 10.1021/jm3016365 Unchecked 2
15801854 10.1021/jm049120y GABA A receptor alpha-2/beta-2/gamma-2 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
9171876 10.1021/jm960733n GABA-A receptor; anion channel 2
9171876 10.1021/jm960733n Mus musculus 2
17417631 10.1038/nchembio873 Unchecked 1
9171876 10.1021/jm960733n ADMET 1
11063608 10.1021/jm000977e Mus musculus 1
38318365 10.1016/j.isci.2024.108907 Deoxynucleoside triphosphate triphosphohydrolase SAMHD1 1
11063608 10.1021/jm000977e GABA-A receptor; anion channel 1

Data from ChEMBL 36 via Core Engine