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Compound Detail

CHEMBL406117

GUSPERIMUS
🧪 Phase III
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🧪 Phase III
N=C(N)NCCCCCCC(=O)NC(O)C(=O)NCCCCNCCCN

Basic Information

ChEMBL ID CHEMBL406117
Name GUSPERIMUS
Phase Phase III
Structure Type MOL
InChI Key IDINUJSAMVOPCM-UHFFFAOYSA-N

Known Names

Gusperimus
3
Targets
8
Activities
3
Assay Types
0
PK Parameters
20
Publications
1
Known Names
2
Indications

Molecular Properties

387.5
MW (Da)
-1.31
ALogP
6
HBA
8
HBD
178.4
PSA (Ų)
0.07
QED
1
Ro5 Violations
17
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Racemic

Flags

Natural Product
USAN Stem -imus
USAN Year 1993

Extended Properties

Molecular Formula C17H37N7O3
MW 387.53
Aromatic Rings 0
Heavy Atoms 27
NP-Likeness 0.24

Indications

Granulomatosis with Polyangiitis Immune System Diseases

ATC Classification

L04AA19
gusperimus
Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Level 2: IMMUNOSUPPRESSANTS

Activity Summary

IC50 5 meas. best 6.83
Kd 2 meas. best 5.4
Ki 1 meas. best 7.09

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MDA-MB-231
CHEMBL400
Ki 7.09 7.09 81.0 1
Plasmodium falciparum
CHEMBL364
IC50 6.83 6.83 148.0 1
Unchecked
CHEMBL612545
Kd 5.4 5.4 4000.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17194705 10.1074/jbc.m610251200 Plasmodium falciparum 12
15646539 10.1016/s0399-8320(04)95062-2 Unchecked 11
15646539 10.1016/s0399-8320(04)95062-2 NON-PROTEIN TARGET 8
17194705 10.1074/jbc.m610251200 Unchecked 4
37468498 10.1038/s41467-023-40064-9 Nuclear receptor subfamily 1 group I member 2 3
37468498 10.1038/s41467-023-40064-9 Cannabinoid receptor 1 2
37468498 10.1038/s41467-023-40064-9 Muscarinic acetylcholine receptor M2 2
37468498 10.1038/s41467-023-40064-9 Gamma-aminobutyric acid receptor subunit alpha-1 2
37468498 10.1038/s41467-023-40064-9 Alpha-2A adrenergic receptor 2
37468498 10.1038/s41467-023-40064-9 Progesterone receptor 2
37468498 10.1038/s41467-023-40064-9 Beta-2 adrenergic receptor 2
37468498 10.1038/s41467-023-40064-9 Beta-1 adrenergic receptor 2
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 1A 2
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 2B 2
9925733 10.1021/jm980431g Mus musculus 2
32686940 10.1021/acs.jmedchem.0c00530 Mus musculus 2
18164205 10.1016/j.bmc.2007.12.014 Unchecked 2
37468498 10.1038/s41467-023-40064-9 Alpha-1A adrenergic receptor 2
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 2A 2
37468498 10.1038/s41467-023-40064-9 Androgen receptor 2

Data from ChEMBL 36 via Core Engine