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Compound Detail

CHEMBL1257065

STILONIUM IODIDE
🧪 Phase II
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🧪 Phase II
CC[N+](CC)(CC)CCOc1ccc(/C=C/c2ccccc2)cc1.[I-]

Basic Information

ChEMBL ID CHEMBL1257065
Name STILONIUM IODIDE
Phase Phase II
Structure Type MOL
InChI Key RDTKUZXIHMTSJO-UEIGIMKUSA-M
Parent Compound CHEMBL191491
Active Moiety CHEMBL191491

Known Names

Elvetil Iodure de stilonium Ioduro de estilonio M.G. 624 MG-624 Stilonium iodide
12
Targets
31
Activities
2
Assay Types
0
PK Parameters
20
Publications
6
Known Names

Molecular Properties

324.5
MW (Da)
5.11
ALogP
1
HBA
0
HBD
9.2
PSA (Ų)
0.46
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Achiral
USAN Stem -ium; -onium
USAN Year 1981

Extended Properties

Molecular Formula C22H30INO
MW 451.39
Aromatic Rings 2
Heavy Atoms 24
NP-Likeness -0.12

Activity Summary

IC50 24 meas. best 8.7
Ki 7 meas. best 8.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuronal acetylcholine receptor subunit alpha-7
CHEMBL2492
IC50 8.7 6.972 2.0 5
Neuronal acetylcholine receptor; alpha4/beta2
CHEMBL1907589
Ki 8.24 8.24 5.7 1
Neuronal acetylcholine receptor; alpha9/alpha10
CHEMBL2109238
IC50 8.18 8.06 6.7 3
Neuronal acetylcholine receptor subunit alpha-7
CHEMBL2492
Ki 6.98 6.98 104.0 3
Neuronal acetylcholine receptor subunit alpha-7
CHEMBL5169123
IC50 6.96 6.96 109.0 2
Plasmodium falciparum
CHEMBL364
IC50 6.4 6.0714 398.1 7
Neuronal acetylcholine receptor; alpha3/beta4
CHEMBL1907594
Ki 6.36 6.36 433.0 2
DNA dC->dU-editing enzyme APOBEC-3A
CHEMBL1741179
IC50 5.63 5.63 2330.0 1
DNA dC->dU-editing enzyme APOBEC-3G
CHEMBL1741217
IC50 5.59 5.59 2570.0 1
U-87 MG
CHEMBL614247
IC50 5.36 5.36 4400.0 1
A549
CHEMBL392
IC50 5.33 5.33 4700.0 1
Carboxy-terminal domain RNA polymerase II polypeptide A small phosphatase 1
CHEMBL1795098
IC50 4.69 4.69 20224.0 1
Astrocyte
CHEMBL5314311
IC50 4.33 4.33 47000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neuronal acetylcholine receptor subunit alpha-7 IC50 = 1.99 nM 8.7 Antagonist activity at human alpha7 nAChR expressed in Xenopus laevis oocytes as... 35834819
Neuronal acetylcholine receptor; alpha4/beta2 Ki = 5.7 nM 8.24 Displacement of [3H]-epibatidine from human alpha4beta2 nAChR expressed in HEK29... 35834819
Neuronal acetylcholine receptor; alpha9/alpha10 IC50 = 6.68 nM 8.18 Antagonist activity at human alpha9alpha10 nAChR expressed in Xenopus laevis ooc... 35834819
Neuronal acetylcholine receptor; alpha9/alpha10 IC50 = 10.0 nM 8.0 Antagonist activity at human alpha9alpha10 nACHR expressed in xenopous laevis oo... 30403486
Neuronal acetylcholine receptor; alpha9/alpha10 IC50 = 10.0 nM 8.0 Antagonist activity at human alpha9alpha10 nAChR expressed in Xenopus laevis ooc... 36526469
Neuronal acetylcholine receptor subunit alpha-7 IC50 = 41.0 nM 7.39 Antagonist activity at human alpha7 nACHR expressed in xenopous laevis oocyte as... 30403486
Neuronal acetylcholine receptor subunit alpha-7 IC50 = 41.0 nM 7.39 Antagonist activity at human alpha7 nAChR expressed in Xenopus laevis oocytes 36526469
Neuronal acetylcholine receptor subunit alpha-7 Ki = 104.0 nM 6.98 Displacement of [125I]alpha-Bungarotoxin from human alpha7 nAChR expressed in hu... 36526469
Neuronal acetylcholine receptor subunit alpha-7 Ki = 104.0 nM 6.98 Displacement of [125I]alpha-bungarotoxin from human alpha7 nAChR expressed in SH... 35834819
Neuronal acetylcholine receptor subunit alpha-7 Ki = 104.0 nM 6.98 Displacement of [125I]-alpha-bungarotoxin from human alpha7 nAChR expressed in h... 30403486
Neuronal acetylcholine receptor subunit alpha-7 IC50 = 109.0 nM 6.96 Antagonist activity at chick alpha7 nAChR expressed in stage VI oocytes assessed... 35834819
Neuronal acetylcholine receptor subunit alpha-7 IC50 = 109.0 nM 6.96 Antagonist activity at chicken alpha7 nAChR expressed in Xenopus laevis oocytes 36526469
Plasmodium falciparum IC50 = 398.11 nM 6.4 Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR gr... 19734910
Neuronal acetylcholine receptor; alpha3/beta4 Ki = 433.0 nM 6.36 Displacement of [3H]-Epibatidine from alpha3beta4 nAChR (unknown origin) express... 36526469
Neuronal acetylcholine receptor; alpha3/beta4 Ki = 433.0 nM 6.36 Displacement of [3H]-epibatidine from human alpha3beta4 nAChR expressed in SH-EP... 35834819
Plasmodium falciparum IC50 = 501.19 nM 6.3 Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 794.33 nM 6.1 Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 794.33 nM 6.1 Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 1000.0 nM 6.0 Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 1258.93 nM 5.9 Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR g... 19734910

Literature References

PubMed DOI Target Context # Activities
30403486 10.1021/acs.jmedchem.8b01052 ADMET 11
- 10.6019/CHEMBL5303304 HEK-293T 10
19734910 10.1038/nchembio.215 Plasmodium falciparum 7
36526469 10.1021/acs.jmedchem.2c01256 Neuronal acetylcholine receptor subunit alpha-7 6
- 10.6019/CHEMBL5303304 Fibroblast 6
- 10.6019/CHEMBL5303304 U2OS 5
30403486 10.1021/acs.jmedchem.8b01052 U-87 MG 4
35834819 10.1021/acs.jmedchem.2c00746 Neuronal acetylcholine receptor subunit alpha-7 4
30403486 10.1021/acs.jmedchem.8b01052 Neuronal acetylcholine receptor subunit alpha-7 2
36526469 10.1021/acs.jmedchem.2c01256 Neuronal acetylcholine receptor; alpha9/alpha10 2
35834819 10.1021/acs.jmedchem.2c00746 Neuronal acetylcholine receptor; alpha9/alpha10 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1
35834819 10.1021/acs.jmedchem.2c00746 Neuronal acetylcholine receptor; alpha3/beta4 1
- 10.6019/CHEMBL5665443 Uracil-DNA glycosylase 1
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 1
30403486 10.1021/acs.jmedchem.8b01052 Astrocyte 1
30403486 10.1021/acs.jmedchem.8b01052 SH-SY5Y 1
30403486 10.1021/acs.jmedchem.8b01052 A549 1
30403486 10.1021/acs.jmedchem.8b01052 Neuronal acetylcholine receptor; alpha9/alpha10 1

Data from ChEMBL 36 via Core Engine