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Compound Detail

CHEMBL273481

MUSCIMOL
Phase I
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Phase I

Basic Information

ChEMBL ID CHEMBL273481
Name MUSCIMOL
Phase Phase I
Structure Type MOL
InChI Key ZJQHPWUVQPJPQT-UHFFFAOYSA-N

Known Names

Agarin Muscimol NSC-333569 Pantherine
10
Targets
52
Activities
4
Assay Types
0
PK Parameters
20
Publications
4
Known Names
2
Indications

Molecular Properties

114.1
MW (Da)
-0.16
ALogP
4
HBA
2
HBD
72.3
PSA (Ų)
0.53
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Achiral

Flags

Natural Product

Extended Properties

Molecular Formula C4H6N2O2
MW 114.10
Aromatic Rings 1
Heavy Atoms 8
NP-Likeness -0.57

Indications

Epilepsy Parkinson Disease

Activity Summary

EC50 32 meas. best 7.27
IC50 12 meas. best 8.7
Ki 5 meas. best 8.59
Kd 3 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; anion channel
CHEMBL2093872
IC50 8.7 7.79 2.0 3
Unchecked
CHEMBL612545
Ki 8.59 8.37 2.6 2
GABA-A receptor; anion channel
CHEMBL1907607
IC50 8.52 8.2814 3.0 7
GABA-A receptor; anion channel
CHEMBL1907607
Ki 8.4 8.4 4.0 1
GABA-A receptor; anion channel
CHEMBL2093872
Ki 8.22 8.09 6.0 2
Gamma-aminobutyric acid receptor subunit gamma-1
CHEMBL296
IC50 8.22 8.22 6.0 1
Unchecked
CHEMBL612545
Kd 7.82 7.82 15.2 1
Unchecked
CHEMBL612545
EC50 7.27 6.1275 53.7 12
GABA A receptor alpha-3/beta-2/gamma-2
CHEMBL2111339
EC50 6.68 6.675 210.0 4
GABA A receptor alpha-2/beta-2/gamma-2
CHEMBL2111413
EC50 6.39 6.39 407.4 4
GABA-A receptor; alpha-1/beta-2/gamma-2
CHEMBL2095172
EC50 6.27 6.27 537.0 4
Gamma-aminobutyric acid receptor subunit rho-1
CHEMBL3561
EC50 6.16 6.0217 691.8 6
Gamma-aminobutyric acid receptor subunit rho-2
CHEMBL2375
Kd 5.85 5.85 1400.0 1
Gamma-aminobutyric acid receptor subunit rho-1
CHEMBL3561
Kd 5.64 5.64 2300.0 1
GABA-A receptor; agonist GABA site
CHEMBL2109244
EC50 4.57 4.57 27000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
GABA-A receptor; anion channel IC50 = 2.0 nM 8.7 Binding affinity in vivo for gamma-aminobutyric-acid A receptor measured by its ... 1331456
Unchecked Ki = 2.6 nM 8.59 Displacement of [3H]GABA from GABAA receptor 8496700
GABA-A receptor; anion channel IC50 = 3.0 nM 8.52 Displacement of [3H]- muscimol in cerebral tissue of male rats 2991521
GABA-A receptor; anion channel IC50 = 3.2 nM 8.49 Displacement of [3H]gamma-aminobutyric acid from sodium-independent Gamma-aminob... 7420361
GABA-A receptor; anion channel Ki = 4.0 nM 8.4 Displacement of [3H]gamma-amino butyric acid from Gamma-aminobutyric acid (GABA-... 7392039
GABA-A receptor; anion channel IC50 = 5.0 nM 8.3 In vitro inhibition of [3H]THIP binding to Gamma-aminobutyric acid receptor in r... 2999396
GABA-A receptor; anion channel Ki = 6.0 nM 8.22 Displacement of [3H]muscimol from GABAA receptor in SPRD rat brain synaptic memb... 25038482
GABA-A receptor; anion channel IC50 = 6.0 nM 8.22 In vitro inhibition of [3H]P4S binding to Gamma-aminobutyric acid receptor of ra... 2999396
Gamma-aminobutyric acid receptor subunit gamma-1 IC50 = 6.0 nM 8.22 In vitro inhibition of [3H]GABA binding to Gamma-aminobutyric acid receptor of r... 2999396
GABA-A receptor; anion channel IC50 = 6.0 nM 8.22 Inhibition against Gamma-aminobutyric acid A (GABA-A) receptor 11150163
GABA-A receptor; anion channel IC50 = 6.0 nM 8.22 Affinity for GGABA-A receptor alpha by inhibiting binding of [3H]muscimol to rat... 12036354
Unchecked Ki = 7.0 nM 8.15 Displacement of [3H]muscimol from GABAA receptor in rat synaptic membrane after ... 23294161
GABA-A receptor; anion channel IC50 = 10.0 nM 8.0 Displacement of [3H]GABA from Gamma-aminobutyric acid A receptor ofrat brain mem... 3031294
GABA-A receptor; anion channel Ki = 11.0 nM 7.96 Displacement of [3H]gamma-amino butyric acid from Gamma-aminobutyric acid (GABA-... 7392039
Unchecked Kd = 15.2 nM 7.82 Binding affinity to mouse brain GABAA receptor by Scatchard analysis 23886812
GABA-A receptor; anion channel IC50 = 16.0 nM 7.8 Percent inhibition against GABAA receptor alpha at a compound concentration of 1... 16250647
Unchecked EC50 = 54.0 nM 7.27 Agonist activity at human GABAA alpha5beta2gamma2S receptor expressed in TSA201 ... 23294161
Unchecked EC50 = 54.0 nM 7.27 Agonist activity at human GABAAalpha5beta2gamma2S receptor expressed in tsA-201c... 25038482
Unchecked EC50 = 53.7 nM 7.27 Agonist activity at human GABAAalpha5beta2gamma2S receptor expressed in tsA-201c... 25038482
Unchecked EC50 = 53.7 nM 7.27 Agonist activity at human GABAA alpha5beta2gamma2S receptor expressed in TSA201 ... 23294161

Literature References

PubMed DOI Target Context # Activities
17655213 10.1021/jm070447j Unchecked 9
- 10.6019/CHEMBL4495565 SARS-CoV-2 4
25038482 10.1016/j.ejmech.2014.07.039 Gamma-aminobutyric acid receptor subunit rho-1 3
2536440 10.1021/jm00122a025 Mus musculus 3
23294161 10.1021/jm301473k Unchecked 3
25038482 10.1016/j.ejmech.2014.07.039 GABA A receptor alpha-2/beta-2/gamma-2 3
25038482 10.1016/j.ejmech.2014.07.039 GABA A receptor alpha-3/beta-2/gamma-2 3
- 10.1039/C5MD00442J Unchecked 3
7392039 10.1021/jm00180a029 Mus musculus 3
25038482 10.1016/j.ejmech.2014.07.039 Unchecked 3
23294161 10.1021/jm301473k GABA A receptor alpha-2/beta-2/gamma-2 2
7392039 10.1021/jm00180a029 GABA-A receptor; anion channel 2
1331456 10.1021/jm00100a015 GABA-A receptor; anion channel 2
7420361 10.1021/jm00184a017 GABA-A receptor; anion channel 2
25038482 10.1016/j.ejmech.2014.07.039 GABA-A receptor; alpha-1/beta-2/gamma-2 2
423190 10.1021/jm00187a022 Mus musculus 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
8496700 10.1021/np50094a001 Unchecked 2
23294161 10.1021/jm301473k GABA-A receptor; alpha-1/beta-2/gamma-2 2
23294161 10.1021/jm301473k Gamma-aminobutyric acid receptor subunit rho-1 2

Data from ChEMBL 36 via Core Engine